Semi-synthetic opioids like oxycodone, hydrocodone and hydromorphone are derived from them.
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"Thus, the reported semi-synthetic organism is likely to be just the first of a new form of semi-synthetic life that is able to access a broad range of forms and functions not available to natural organisms."Maybe. [Nature]
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Hydrocodone and oxycodone are semi-synthetic opioids, manufactured in labs with natural and synthetic ingredients.
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Overdoses linked to natural and semi-synthetic opioids like oxycodone and morphine are higher in rural counties.
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Deaths from natural and semi-synthetic opioids rose by 2.6 percent, and methadone deaths declined by 9.1 percent.
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Moving to the moon, surrounded by aristocrats, to take care of spoiled cats and semi-synthetic pigs to butcher.
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Some, such as morphine, are made from the opium poppy; others, such as oxycodone, are semi-synthetic or synthetic.
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To make heroin or morphine and other semi-synthetic opioids like Oxycodone and hydrocodone, you first need to grow poppies.
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It is a powerful semi-synthetic opiate derived from the opium poppy and is used illicitly as a recreational drug.
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The use of those fibers, plus a semi-synthetic fiber called viscose, account for 23% of the raw materials used by the brands.
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And because cells cannot make their own X and Y without the addition of certain chemicals, the semi-synthetic organisms cannot live outside of a laboratory.
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And because cells cannot make their own X and Y without the addition of certain chemicals, the semi-synthetic organisms cannot live outside of a laboratory.
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Synthetic opioids are manmade drugs such as fentanyl, as opposed to semi-synthetic opioids such as hydrocodone and oxycodone, or natural opioids such as codeine and morphine.
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The pill was labeled "Watson 385," which typically indicates that it contained a lower-potency mix of acetaminophen and hydrocodone, a semi-synthetic opioid used for pain relief.
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Until about 2500 the rise in opioid deaths was driven by the abuse of legitimate painkillers, which are sometimes called "semi-synthetic" because they are derived from plants.
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This statistic — which is expected to rise, according to Canopy — refers to the making of semi-synthetic materials, such as rayon, which is made from cellulose that's extracted from wood pulp.
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Romesberg is aware that the creation of semi-synthetic organisms might raise concerns of hybrid life forms spreading beyond the lab, but the system they used makes such an escape unlikely.
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Deaths from so-called natural opioids, which include the prescription medications morphine and codeine, and semi-synthetic opioids, which include the prescription drugs oxycodone and hydrocodone, decreased 2.6% from 2014 to 2015.
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William Hanage, an epidemiologist at the Harvard School of Public Health, was among those showing that these genes conferred a resistance to amikacin, a semi-synthetic drug that did not exist before the 1970s.
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"Today's report shows significant increases across states in death rates from heroin and synthetic opioid deaths, coupled with continuing high numbers of fatal overdoses related to natural/semi-synthetic opioid deaths," the CDC said in a statement.
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Estimates suggest that the global harvest of opium poppies, from which natural and semi-synthetic opioid medications such as morphine and codeine are prepared, together with the chemicals for synthetic ones, should be enough to satisfy all the demand in the world.
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As the New Yorker noted, the painkiller has reportedly made Purdue as much as $35 billion over the years, while doctors and patients alike soon found that its only active ingredient, the semi-synthetic opioid oxycodone, often resulted in "debilitating" withdrawal symptoms upon cessation or even between doses.
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"The resulting semi-synthetic organism both encodes and retrieves increased information," report the authors this week in Nature, "and should serve as a platform for the creation of new life forms and functions," like new kinds of bacteria with specialized purposes (cleaning the environment, storing gifs...who knows) for example.
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Even full-scale computations have been achieved by semi-synthetic DNA computers.
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Semi-synthetic fibers are made from raw materials with naturally long-chain polymer structure and are only modified and partially degraded by chemical processes, in contrast to completely synthetic fibers such as nylon (polyamide) or dacron (polyester), which the chemist synthesizes from low-molecular weight compounds by polymerization (chain- building) reactions. The earliest semi-synthetic fiber is the cellulose regenerated fiber, rayon. Most semi-synthetic fibers are cellulose regenerated fibers.
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Semi-synthetic resilin-based hydrogels, which incorporate poly(ethylene glycols), have also been reported.
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Dihydroergotamine (DHE) is a semi-synthetic form of ergotamine approved in the US in 1946.
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Synthetic drugs are those which are primarily derived from inorganic substances. Semi-synthetic are a hybrid of both synthetic and natural drugs, however as both synthetic and semi-synthetic drugs undergo an array of chemical processes during production, their environmental impact are quite similar.
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Daunorubicin is also used as the starting material for semi- synthetic manufacturing of doxorubicin, epirubicin and idarubicin.
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Pentosan polysulfate (PPS) is a medication used for interstitial cystitis and osteoarthritis. It is a semi-synthetic polysulfated xylan.
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KT5720 is a kinase inhibitor with specificity towards protein kinase A. It is a semi-synthetic derivative of K252a and analog of staurosporine.
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Buprenorphine is a semi-synthetic analogue of thebaine and is fairly soluble in water, as its hydrochloride salt. It degrades in the presence of light.
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Injectable semi-synthetic cephalosporin antibiotic related to cefamandole, q.v. Cefonicid synthesis:D. A. Berges, ; idem, (1976, 1977 both to Smith Kline)., (1978, 1979 both to Smith Kline).
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A common form of antibiotic production in modern times is semi-synthetic. Semi-synthetic production of antibiotics is a combination of natural fermentation and laboratory work to maximize the antibiotic. Maximization can occur through efficacy of the drug itself, amount of antibiotics produced, and potency of the antibiotic being produced. Depending on the drug being produced and the ultimate usage of said antibiotic determines what one is attempting to produce.
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Floyd E. Romesberg is an American biotechnologist, biochemist, and geneticist formerly at Scripps Research in San Diego, California. He is known for leading the team that created the first Unnatural Base Pair (UBP), thus expanding the genetic alphabet of four letters to six in 2012, the first semi-synthetic organism in 2014, and the first functional semi-synthetic organism that can reproduce its genetic material in successive offspring, in 2017.
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Lurtotecan is a semi-synthetic analog of camptothecin with antineoplastic activity. Liposomal lurtotecan was in clinical trials as a treatment for topotecan-resistant ovarian cancer, but was discontinued.
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17-Dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG) is a chemical compound which is a semi-synthetic derivative of the antibiotic geldanamycin. It is being studied for the possibility of treating cancer.
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Flopristin is a semi-synthetic antibiotic of the streptogramin A class. It is a fluorinated derivative of pristinamycin IIB. Flopristin is one of the components of the experimental drug NXL103.
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Semi-synthetic (e.g., LSD) and synthetic drugs (e.g., DPT and 2C-B used by the Sangoma) have also been developed. Alexander Shulgin developed hundreds of entheogens in PiHKAL and TiHKAL.
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Artesunate is made from dihydroartemisinin (DHA) by reacting it with succinic acid anhydride in a basic medium. It is one of few semi-synthetic derivatives from artemisinin that is water-soluble.
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Telavancin (trade name Vibativ) is a bactericidal lipoglycopeptide for use in MRSA or other Gram-positive infections. Telavancin is a semi-synthetic derivative of vancomycin.Astellas, Inc. VIBATIV prescribing information, 9/2009.
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Opioids include opiates, an older term that refers to such drugs derived from opium, including morphine itself. Other opioids are semi-synthetic and synthetic drugs such as hydrocodone, oxycodone and fentanyl; antagonist drugs such as naloxone; and endogenous peptides such as the endorphins. The terms opiate and narcotic are sometimes encountered as synonyms for opioid. Opiate is properly limited to the natural alkaloids found in the resin of the opium poppy although some include semi-synthetic derivatives.
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There are also many synthetic sex steroids. Synthetic androgens are often referred to as anabolic steroids. Synthetic estrogens and progestins are used in methods of hormonal contraception. Ethinylestradiol is a semi- synthetic estrogen.
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Morphine is a precursor in the manufacture in a number of opioids such as dihydromorphine, hydromorphone, hydrocodone, and oxycodone as well as codeine, which itself has a large family of semi-synthetic derivatives.
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Semi-synthetic oils (also called "synthetic blends") are a mixture of mineral oil and synthetic oil, which are engineered to have many of the benefits of full synthetic oil without the cost. Motul introduced the first semi-synthetic motor oil in 1966.DELPHI history Lubricants that have synthetic base stocks even lower than 30% but with high-performance additives consisting of esters can also be considered synthetic lubricants. In general, the ratio of the synthetic base stock is used to define commodity codes among the customs declarations for tax purposes.
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In search for useful biological activity, several synthetic and semi-synthetic analogs have been prepared for study. Semi-synthetic analogs include salvinorin B ethoxymethyl ether and salvinorin B methoxymethyl ether. Fully synthetic analogs include herkinorin. Several derivates can be conveniently made from salvinorin B. Most derivatives are selective kappa opioid agonists as with salvinorin A, although some are even more potent, with the most potent compound 2-ethoxymethyl salvinorin B being ten times stronger than salvinorin A. Some derivatives, such as herkinorin, reduce kappa opioid action and instead act as mu opioid agonists.
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Sultamicillin is a mutual prodrug of ampicillin and sulbactam. Ampicillin, a semi-synthetic orally active broad spectrum antibiotic, is linked via a methylene group with a beta-lactamase inhibitor. Sultamicillin is chemically oxymethyl penicillinate sulfone ester of ampicillin.
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This ended a point of conflict in the early 1990s; many environmentalists, including Al Gore, had opposed the destructive harvesting of Pacific yew for paclitaxel cancer treatments. Docetaxel can then be obtained by semi-synthetic conversion from the precursors.
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The antibiotic is highly soluble in water and is acid-labile. A typical lab working concentration is 50 µg per ml. It is a semi-synthetic analogue of the naturally occurring benzyl- penicillin. Carbenicillin at high doses can cause bleeding.
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API Group II- and API Group III-type base stocks help to formulate more economic-type semi- synthetic lubricants. API Group I-, II-, II+-, and III-type mineral-base oil stocks are widely used in combination with additive packages, performance packages, and ester and/or API Group IV poly-alpha-olefins in order to formulate semi-synthetic-based lubricants. API Group III base oils are sometimes considered fully synthetic, but they are still classified as highest-top-level mineral-base stocks. A synthetic or synthesized material is one that is produced by combining or building individual units into a unified entity.
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Roxithromycin is a semi-synthetic macrolide antibiotic. It is used to treat respiratory tract, urinary and soft tissue infections. Roxithromycin is derived from erythromycin, containing the same 14-membered lactone ring. However, an N-oxime side chain is attached to the lactone ring.
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These compounds include vinblastine, vincristine, vindesine, and vinorelbine. Additional researched vinca alkaloids include vincaminol, vineridine, and vinburnine. Vinpocetine is a semi-synthetic derivative of vincamine (sometimes described as "a synthetic ethyl ester of apovincamine"). Minor vinca alkaloids include minovincine, methoxyminovincine, minovincinine, vincadifformine, desoxyvincaminol, and vincamajine.
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Ixabepilone is a semi-synthetic analog of epothilone B, a natural chemical compound produced by Sorangium cellulosum. Epothilone B itself could not be developed as a pharmaceutical drug because of poor metabolic stability and pharmacokinetics. Ixabepilone was designed through medicinal chemistry to improve upon these properties.
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6 There are alkaloids that do not have strong psychoactive effect themselves, but are precursors for semi-synthetic psychoactive drugs. For example, ephedrine and pseudoephedrine are used to produce methcathinone and methamphetamine.Veselovskaya, pp. 51–52 Thebaine is used in the synthesis of many painkillers such as oxycodone.
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Over the four decades he worked at M.I.T., Sheehan came to hold over 30 patents, including the invention of ampicillin, a commonly used semi- synthetic penicillin that is taken orally rather than by injection. His research covered not only penicillin, but also peptides, other antibiotics, alkaloids, and steroids.
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In addition, the nootropic agent vincamine is derived from Vinca minor. Vinorelbine, a newer semi-synthetic chemotherapeutic agent, is used in the treatment of non-small-cell lung cancer and is prepared either from the natural products leurosine or catharanthine and vindoline, in both cases by first preparing anhydrovinblastine.
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Their chemical modification permits the integration of cellular attachment sites and a certain control over degradation rates. Semi-synthetic hydrogels share characteristics of both classes. Indeed, they permit either the modification of the purified natural biopolymers or by coupling the synthetic component with integrin and/or growth factor binding sites.
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Compounds that are prepared by reaction of other compounds are known as "synthetic". They may be either compounds that already are found in plants or animals or those that do not occur naturally. Most polymers (a category that includes all plastics and rubbers) are organic synthetic or semi-synthetic compounds.
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Rohitukine (C16H19O5N), a chromane alkaloid, was first reported from Amoora rohituka (Roxb.) Wight & Arn. (Meliaceae) and then from D. binectariferum . Rohitukine exhibits both anti-inflammatory as well as immuno-modulatory properties besides acting as an anticancer compound. Rohitukine is an important precursor for the semi- synthetic derivative, flavopiridol (C21H20Cl NO5).
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Chloroeremomycin is a member of the glycopeptide family of antibiotics, such as vancomycin. The molecule is a non-ribosomal polypeptide that has been glycosylated. It is composed of seven amino acids and three saccharide units. Although chloroeremomycin has never been in clinical phases, oritavancin, a semi-synthetic derivative of chloroeremomycin, has been investigated.
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A 2012 review found that A. paniculata extracts could inhibit expression of several cytochrome C enzymes and thus interfere with metabolism of other pharmaceuticals. A 2019 review finds that A. paniculata compounds have poor solubility and relatively low potency, and that a semi-synthetic injectable derivative can cause sometimes life-threatening allergic reactions.
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Lexitropsins are members of a family of semi-synthetic DNA-binding ligands. They are structural analogs of the natural antibiotics netropsin and distamycin. Antibiotics of this group can bind in the minor groove of DNA with different sequence-selectivity. Lexitropsins form a complexes with DNA with stoichiometry 1:1 and 2:1.
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Bromocriptine is an ergot derivative, semi-synthetic. Bromocriptine is a D2 receptor agonist and D1 receptor antagonist with a binding affinity to D2 receptors of anterior pituitary cells, exclusively on lactotrophs. Bromocriptine stimulates Na+, K+-ATPase activity and/or cytosolic Ca2+ elevation and therefore reduction of prolactin which leads to no production of cAMP.
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This semi-synthetic approach has also facilitated experimentation with alternative acyl chain compositions. QS-21 is currently under clinical evaluation as an additive for various trial vaccines, including those for HIV, malaria and cancer. , it had been tested in more than 3000 patients in 60 clinical trials. It is a component of the Shingrix vaccine.
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Basic structure of a tetracycline chelating a metal (M)Tetracyclines are antibiotics that also exhibit MMP inhibitory activity. They chelate Zn2+ ion, thereby inhibiting MMP activity. It is believed that tetracyclines also effect MMP expression and proteolytic activity. Doxycycline Doxycycline is a semi-synthetic tetracycline that has been studied for dental and medical applications.
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Ethocybin (CEY-19; 4-phosphoryloxy-DET; 4-PO-DET) is a homologue of the mushroom alkaloid psilocybin, and a semi-synthetic psychedelic alkaloid of the tryptamine family. Effects of ethocybin are comparable to those of a shorter LSD or psilocybin, although intensity and duration vary depending on dosage, individual physiology, and set and setting.
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Zearalanone (ZAN) is a semi-synthetic mycoestrogen that is a derivative of zearalenone (ZEN). Zearalanone is extracted from medical herbs and edible herbs alone with other substance called aflatoxins in the same time by a specific immunoaffinity column. Zearalanone has six analog. They are ZEN, zearalanone, α-zeralanol, β-zeralanol, α-zearalenol, and β-zearalenol.
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The enzyme yields hydromorphone and hydrocodone, which are both valuable semi-synthetic opiate drugs. Hydromorphone is a powerful analgesic, which is shown to be more potent than morphine. Hydrocodone is a FDA-approved, mild analgesic and antitussive. Notably, morphine and codeine are natural products of the opiate biosynthetic pathway in opium poppy plant Papaver somniferum.
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Scientists from the company Amyris have developed a method for high-level production of artemisinin. One of the synthetic genes in this procedure is ADS from Artemisia annua. The semi-synthetic production of artemisinin by Amyris has the potential to lower the cost of antimalarial treatments thus making them more readily available to the developing world.
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In contrast the semi- synthetic mono-methyl ether, heterocodeine is a direct agonist. The 6,7,8,14 tetradehydro 3,6 methyl di-ether of morphine is thebaine. Heterocodeine is 6 times more potent than morphine due to having a substitution at the 6-hydroxy position, in a similar manner to 6-acetylmorphine. The drug methyldihydromorphine (dihydroheterocodeine) is a derivative of heterocodeine.
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Dreser brought the new drug to market as an analgesic and a cough treatment for tuberculosis, bronchitis, and asthma in 1898. Bayer ceased production in 1913, after heroin's addictive potential was recognized. Several semi-synthetic opioids were developed in Germany in the 1910s. The first, oxymorphone, was synthesized from thebaine, an opioid alkaloid in opium poppies, in 1914.
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O-Acetylpsilocin can be obtained by acetylation of psilocin under alkaline or strongly acidic conditions. It is, therefore, a semi-synthetic compound. It is believed to be a prodrug of psilocin; however, speculation exists that psilacetin itself also may be psychoactive. O-Acetylpsilocin is more resistant than psilocin to oxidation under basic conditions due to its acetoxy group.
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Orlistat is a semi-synthetic compound, which has a similar structure to lipstatin. They differ only in the saturation of the β-alkyl chain, where orlistat is saturated while lipstatin has two double bonds in the side chain.Christophe, A.B. and S. DeVriese, Fat Digestion and Absorption. The Role of Dietary Fat in Obesity and Therapy with Orlistat, ed.
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Topotecan is a semi-synthetic derivative of camptothecin. Camptothecin is a natural product extracted from the bark of the tree Camptotheca acuminata. Topoisomerase-I is a nuclear enzyme that relieves torsional strain in DNA by opening single strand breaks. Once topoisomerase-I creates a single strand break, the DNA can rotate in front of the advancing replication fork.
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Telithromycin is the first ketolide antibiotic to enter clinical use and is sold under the brand name of Ketek. It is used to treat community acquired pneumonia of mild to moderate severity. After significant safety concerns, the US Food and Drug Administration sharply curtailed the approved uses of the drug in early 2007. Telithromycin is a semi-synthetic erythromycin derivative.
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The original vinca alkaloids are natural products that include vincristine and vinblastine. Following the success of these drugs, semi-synthetic vinca alkaloids were produced: vinorelbine (used in the treatment of non-small-cell lung cancer), vindesine, and vinflunine. These drugs are cell cycle-specific. They bind to the tubulin molecules in S-phase and prevent proper microtubule formation required for M-phase.
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Prajmaline (Neo-gilurythmal) is a class Ia antiarrhythmic agent which has been available since the 1970s. Class Ia drugs increase the time one action potential lasts in the heart. Prajmaline is a semi-synthetic propyl derivative of ajmaline, with a higher bioavailability than its predecessor. It acts to stop arrhythmias of the heart through a frequency-dependent block of cardiac sodium channels.
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Zotarolimus (INN, codenamed ABT-578) is an immunosuppressant. It is a semi- synthetic derivative of sirolimus (rapamycin). It was designed for use in stents with phosphorylcholine as a carrier. Zotarolimus, or ABT-578, was originally used on Abbott's coronary stent platforms to reduce early inflammation and restenosis; however, Zotarolimus failed Abbott's primary endpoint to bring their stent/drug delivery system to market.
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This species is grown to produce thebaine, which is commercially converted to codeine and semi-synthetic opiates including hydrocodone, hydromorphone, oxycodone, and oxymorphone. Papaver bracteatum does not contain morphine, codeine or any other narcotic alkaloids in significant amounts. Oripavine has been reported in minute traces but would not exert a relevant activity.Von Lyle E. Craker, James E. Simon (Eds.) (1991).
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Dalfopristin is a semi-synthetic streptogramin antibiotic analogue of ostreogyrcin A (virginiamycin M, pristinamycin IIA, streptogramin A). The combination quinupristin/dalfopristin (marketed under the trade name Synercid) was brought to the market by Rhone-Poulenc Rorer Pharmaceuticals in 1999. Synercid (weight-to-weight ratio of 30% quinupristin to 70% dalfopristin) is used to treat infections by staphylococci and by vancomycin-resistant Enterococcus faecium.
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Midostaurin, sold under the brand name Rydapt, is a multi-targeted protein kinase inhibitor that has been investigated for the treatment of acute myeloid leukemia (AML), myelodysplastic syndrome (MDS) and advanced systemic mastocytosis. It is a semi-synthetic derivative of staurosporine, an alkaloid from the bacterium Streptomyces staurosporeus. The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.
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Taxanes are natural and semi-synthetic drugs. The first drug of their class, paclitaxel, was originally extracted from Taxus brevifolia, the Pacific yew. Now this drug and another in this class, docetaxel, are produced semi-synthetically from a chemical found in the bark of another yew tree, Taxus baccata. Podophyllotoxin is an antineoplastic lignan obtained primarily from the American mayapple (Podophyllum peltatum) and Himalayan mayapple (Sinopodophyllum hexandrum).
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Annual world production of ergot alkaloids has been estimated at 5,000–8,000 kg of all ergopeptines and 10,000–15,000 kg of lysergic acid, used primarily in the manufacture of semi- synthetic derivatives. Others, such as Lysergic acid diethylamide, better known as LSD, a fully synthetic derivative, and ergine, an natural derivative found in Argyreia nervosa, Ipomoea tricolor and related species, are known psychedelic substances.
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Compared with other ergot alkaloids, ergometrine has a greater selectivity in stimulating the uterus. LSD, a semi-synthetic psychedelic ergoline, is an agonist of 5-HT2A, 5-HT1A and to a lesser extent D2 receptors and has a powerful psychedelic effect. Some monoterpenoid indole alkaloids also interact with adrenoceptors. For example, ajmalicine is a selective antagonist of α1-adrenergic receptors and therefore has antihypertensive action.
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The uricosuric agent probenecid proved to be suitable. When probenecid and penicillin are administered together, probenecid competitively inhibits the excretion of penicillin, increasing penicillin's concentration and prolonging its activity. Eventually, the advent of mass- production techniques and semi-synthetic penicillins resolved the supply issues, so this use of probenecid declined. Probenecid is still useful, however, for certain infections requiring particularly high concentrations of penicillins.
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Although dihydrocodeine does have extremely active metabolites, in the form of dihydromorphine and dihydromorphine-6-glucuronide (one hundred times more potent), these metabolites are produced in such small amounts that they do not have clinically significant effects. Dihydrocodeine is also the original member and chemical base of a number of similar semi-synthetic opioids such as acetyldihydrocodeine, dihydrocodeinone enol acetate, dihydroisocodeine, nicocodeine, and nicodicodeine.
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Chronic pain medication is for alleviating long-lasting, ongoing pain. Morphine is the gold standard to which all narcotics are compared. Semi-synthetic derivatives of morphine such as hydromorphone (Dilaudid), oxymorphone (Numorphan, Opana), nicomorphine (Vilan), hydromorphinol and others vary in such ways as duration of action, side effect profile and milligramme potency. Fentanyl has the benefit of less histamine release and thus fewer side effects.
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There are several derivatives of helenaline known within the same sesquiterpene lactone group; pseudoguaianolides. Most of these derivatives occur naturally, such as the compound dihydrohelenalin, but there are also some semi-synthetic derivatives known, such as 2β-(S-glutathionyl)-2,3-dihydrohelenalin. In general, most derivatives are more toxic than helenalin itself. Among these, derivatives with the shortest ester groups are most likely to contain a higher toxicity.
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Modern technologies in genetic engineering and metabolic engineering enabled the production of these natural products in microorganisms. Complete biosynthesis of opiate compounds has been achieved in genetically tractable organisms Saccharomyces cerevisiae and Escherichia coli. Morphinone reductase was also successfully expressed in these two organisms. The enzyme represents a promising candidate for downstream modifications of opiate compounds, allowing the biosynthesis of valuable semi-synthetic opiate drugs in microorganisms.
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1938–39 Schiaparelli suit with large buttons sculpted by Alberto Giacometti Schiaparelli is one of the designers credited with offering the first clothes with visible zippers in 1930. Rather than being concealed, zippers became a key element of Schiaparelli's designs, visibly fastening necklines and running down sleeves and skirts.Secrest, p. 153, 154 She used chunky plastic zippers made from cellulose nitrate, the first semi-synthetic plastic fabric, and cellulose acetate.
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Obeticholic acid (abbreviated to OCA, trade name Ocaliva), is a semi-synthetic bile acid analogue which has the chemical structure 6α-ethyl-chenodeoxycholic acid. It is used as a drug to treat primary biliary cholangitis, and is undergoing development for several other liver diseases and related disorders. Intercept Pharmaceuticals Inc. hold the worldwide rights to develop OCA outside Japan and China, where it is licensed to Dainippon Sumitomo Pharma.
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Pivalic acid is prepared by hydrocarboxylation of isobutene via the Koch reaction: :(CH3)2C=CH2 \+ CO + H2O → (CH3)3CCO2H Such reactions require an acid catalyst such as hydrogen fluoride. tert-Butyl alcohol and isobutyl alcohol can also be used in place of isobutene. Globally, several million kilograms are produced annually. Pivalic acid is also economically recovered as a by-product from the production of semi-synthetic penicillins like ampicillin and amoxycillin.
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1,2,4-Trioxane itself has not been isolated or characterized, but rather only studied computationally. However, it constitutes an important structural element of some more complex organic compounds. The natural compound artemisinin, isolated from the sweet wormwood plant (Artemisia annua), and some semi-synthetic derivatives are important antimalarial drugs containing the 1,2,4-trioxane ring. Completely synthetic analogs containing the 1,2,4-trioxane ring are important potential improvements over the naturally derived artemisinins.
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2C-B is an entactogen commonly used at public places, like rave parties. Entheogens used by movements includes biota like peyote (Native American Church), extracts like ayahuasca (Santo Daime, União do Vegetal), the semi-synthetic drug LSD (Neo-American Church), and synthetic drugs like DPT (Temple of the True Inner Light) and 2C-B (Sangoma). Both Santo Daime and União do Vegetal now have members and churches throughout the world.
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Desomorphine is a semi-synthetic opioid commercialized by Roche, with powerful, fast-acting effects, such as sedation and analgesia. It was first discovered and patented by a German team working for Knoll in 1920DE Patent 414598C 'Verfahren zur Herstellung von Dihydrodesoxymorphin und Dihydrodesoxycodein' but wasn't generally recognized. It was later synthesized in 1932 by Lyndon Frederick Small. Small also successfully patented it in 1934 in the United States.
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There are several techniques to produce peptides chemically, generally it is by solid-phase protection chemistry. This means that any (protected) amino acid can be added into the nascent sequence. In November 2017, a team from the Scripps Research Institute reported having constructed a semi-synthetic E. coli bacteria genome using six different nucleic acids (versus four found in nature). The two extra 'letters' form a third, unnatural base pair.
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14-Methoxydihydromorphinone is a semi-synthetic opioid related to 14-methoxymetopon (14-MM), an opioid with a Ki of 0.15 nM, and 14-O-methyloxymorphone (14-OMO) with a Ki of 0.10 nM. By contrast, oxymorphone has a Ki of 0.97 nM and morphine one of 6.55 nM (all at mu receptors). This suggests that both 14-OMO and 14-MM have a higher mu/kappa selectivity than oxymorphone.
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Semi-synthetic bio-hybrid channels constructed by modifications of natural ion channels had been constructed. Leveraging modern synthetic organic chemistry, these allows pinpoint modifications of existing structures to either elucidate their transport mechanisms or to graft on new functionalities. center Gramicidin and alamethicin had been popular starting points for selective modifications. The above diagram illustrates one example, where a crown-ether was fixed across the mouth of the ion-passing portal.
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Semi-synthetic antibiotic related to penicillin. The relatively small chemical difference between ampicillin and benzylpenicillin not only allows for substantial oral activity but also results in a substantial broadening of antimicrobial spectrum so as to allow for use against many Gram-negative bacteria. Many devices have been employed in order to enhance still further the oral absorption of ampicillin. Bacampicillin is a prodrug of ampicillin designed for this purpose.
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Oripavine is an opiate and the major metabolite of thebaine. It is the parent compound from which a series of semi-synthetic opioids are derived, which includes the compounds etorphine and buprenorphine. Although its analgesic potency is comparable to morphine, it is not used clinically due to its severe toxicity and low therapeutic index. Due to its use in manufacture of strong opioids, oripavine is a controlled substance in some jurisdictions.
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It is now usually called Perkin's mauve, mauveine, or aniline purple. Earlier references to a mauve dye in 1856–1858 referred to a color produced using the semi-synthetic dye murexide or a mixture of natural dyes. Perkin was so successful in marketing his discovery to the dye industry that his biography by Simon Garfield is simply entitled Mauve. Between 1859 and 1861, mauve became a fashion must have.
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Both deficient and excess intake of a vitamin can potentially cause clinically significant illness, although excess intake of water-soluble vitamins is less likely to do so. Before 1935, the only source of vitamins was from food. If intake of vitamins was lacking, the result was vitamin deficiency and consequent deficiency diseases. Then, commercially produced tablets of yeast- extract vitamin B complex and semi-synthetic vitamin C became available.
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René Roy uses carbohydrate chemistry to develop neoglycoconjugates and polymers to treat disease related to glycoproteins such as bacterial infections and cancers. His synthesis of new glycan structures, among which glycopolymers, glycodendrimers, and glycodendrimersomes (terms that he first developed) enabled progress in the area of multivalent molecular recognition mechanisms. He is known for his work on semi-synthetic glycoconjugate vaccines. He has designed a breast cancer vaccine prototype.
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Chlorophyllin refers to any one of a group of closely related water-soluble salts that are semi-synthetic derivatives of chlorophyll, differing in the identity of the cations associated with the anion. Its most common form is a sodium/copper derivative used as a food additive and in alternative medicine. As a food coloring agent, copper complex chlorophyllin is known as natural green 3 and has the E number E141.
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1-Iodomorphine is a semi-synthetic narcotic analgesic formed by halogenation of the 1 position on the morphine carbon skeleton. Halogenated morphine derivatives were first synthesised in Germany, Austria/Austria-Hungary, the United Kingdom and the United States in the period 1890 to 1930. Use of this drug increased after 1945 for the below-mentioned research. It is a research chemical which is often prepared in the laboratory when it is needed.
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Arene- and cyclopentadienyl complexes are kinetically inert platforms for the design of new radiopharmaceuticals. Furthermore, there have been made studies utilizing exogenous semi-synthetic ligands; specifically to the dopamine transporter, observing increased resultant efficacy in regard to reward facilitating behavior (incentive salience) and habituation, namely with the phenyltropane compound [η6-(2β-carbomethoxy-3β-phenyl)tropane]tricarbonylchromium. Carbon monoxide releasing organometallic compounds are also actively investigated, due to the importance of carbon monoxide as a gasotransmitter.
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Synthetic drugs are produced from material that can't be found in nature and semi-synthetic drugs are made from both natural and synthetic materials such as methamphetamines and MDMA. Drug policy is a large determinant on how organisations produce drugs and thereby, how their processes affect the environment, thus prompting Government bodies to analyse the current drug policy."The Impact of Drug Policy on the Environment" (PDF). 2015. Retrieved 7 May 2019.
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The company commenced operations in 1988-89 with a single unit manufacturing semi-synthetic penicillin (SSP) in Puducherry. Aurobindo Pharma became a public company in 1992 and listed its shares in the Indian stock exchanges in 1995. Aurobindo Pharma also has a presence in key therapeutic segments such as neurosciences, cardiovascular, anti-retrovirals, anti-diabetics, gastroenterology and cephalosporins, among others. Aurobindo Pharma features among the top 10 companies in India in terms of consolidated revenues.
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Etorphine (M99) is a semi-synthetic opioid possessing an analgesic potency approximately 1,000–3,000 times that of morphine. It was first prepared in 1960 from oripavine, which does not generally occur in opium poppy extract but rather the related plants Papaver orientale and Papaver bracteatum. It was later reproduced in 1963 by a research group at MacFarlan Smith in Gorgie, Edinburgh, led by Kenneth Bentley. It can also be produced from thebaine.
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An example of semi- synthetic production involves the drug ampicillin. A beta lactam antibiotic just like penicillin, ampicillin was developed by adding an addition amino group (NH2) to the R group of penicillin. This additional amino group gives ampicillin a broader spectrum of use than penicillin. Methicillin is another derivative of penicillin and was discovered in the late 1950s, the key difference between penicillin and methicillin being the addition of two methoxy groups to the phenyl group.
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This noise is said to come from the cams due to incorrect valve setup (when setting valve clearance each cylinder must be set to TDC) or from age and use of incorrect oil grade. The correct oil grade is 5W-30 semi synthetic oil. Another reason is the large tappet clearance on the exhaust valve. This could of course be reduced to lower the noise level but the engine would then suffer from a rough idle and usually stalled.
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Since the discovery of cephalosporins P, N and C in 1948 there have been many studies describing the antibiotic action of cephalosporins and the possibility to synthesize derivatives. Hydrolysis of cephalosporin C, isolation of 7-aminocephalosporanic acid and the addition of side chains opened the possibility to produce various semi-synthetic cephalosporins. In 1962, cephalothin and cephaloridine were introduced. Cephaloridine was briefly popular because it tolerated intramuscularly and attained higher and more sustained levels in blood than cephalothin.
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Dually, one can view processes occurring in nature as information processing. Such processes include self-assembly, developmental processes, gene regulation networks, protein–protein interaction networks, biological transport (active transport, passive transport) networks, and gene assembly in unicellular organisms. Efforts to understand biological systems also include engineering of semi-synthetic organisms, and understanding the universe itself from the point of view of information processing. Indeed, the idea was even advanced that information is more fundamental than matter or energy.
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Heroin, the brand name for diacetylmorphine, is the first of several semi-synthetic opioids to be derived from morphine, a component of natural opium. Although it is derived from, rather than directly found in, natural opium, it is commonly referred to as an opiate. Heroin (diacetylmorphine) is a morphine prodrug; it is metabolized by the liver into morphine after administration. One of the major metabolites of heroin, 6-monoacetylmorphine (6-MAM), is also a morphine prodrug.
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Its reported anticancer mechanism is that it acts as a farnesyl transferase inhibitor. Dozens of semi-synthetic anticancer compounds have been made from dideoxyverticillin A. Dimeric derivatives are reported to have better anticancer activity. The enantioselective first total synthesis of (+)-11,11’-dideoxyverticillin A, the structure of which contains many sterically congested, contiguous stereogenic centers as well as acid- and base-labile and redox-sensitive functionality, was biosynthetically inspired and achieved with high levels of chemical sophistication.
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Rayon is a semi-synthetic fiber made by chemically reshaping cellulose. Cellulose extracted from bamboo is suitable for processing into viscose rayon (rayon is also made from cellulose from other sources). Bamboo leaves and the soft, inner pith from the hard bamboo trunk are extracted using a steaming process and then mechanically crushed to extract the cellulose. The viscose rayon process then treats the fibers with lye, and adds carbon disulfide to form sodium cellulose xanthate.
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Clindamycin phosphate is a water-soluble ester of the semi-synthetic antibiotic clindamycin, which is synthesized from lincomycin. Like the macrolide antibiotics, it acts as a bacteriostatic agent by interfering with the 50S subunit of the ribosome of Cutibacterium acnes, inhibiting bacterial protein synthesis and preventing bacteria from replicating. C. acnes plays a role in the development of acne. Benzoyl peroxide also kills C. acnes, but by releasing free radical oxygen species, thus oxidizing bacterial proteins.
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Artelinic acid (or its salt, artelinate) is an experimental drug that is being investigated as a treatment for malaria. It is a semi-synthetic derivative of the natural compound artemisinin. Artelinic acid has a lower rate of neurotoxicity than the related artemisinin derivatives arteether and artemether, but is three times more toxic than artesunate. At present, artelinic acid seems unlikely to enter routine clinical use, because it offers no clear benefits over the artemesinins already available (artesunate and artemether).
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NCPC currently produces over 430 kinds of antibiotics, semi-synthetic antibiotics, pharmaceutical intermediates, synthetic vitamins, biotechnology products, veterinary and neutraceuticals both in bulk and in finished products. NCPC sells bulk antibiotics , vitamins 10000 tons, antibiotic intermediates 7500 tons, powder for injection 1.8 billion vials, capsules 1.03 billion grains annually. The capacity of penicillin, streptomycin, 6-APA, amoxycillin, cefaradine, vitamin B100 are in the lead worldwide. NCPC's next development focus is on biotechnology products, bio-pesticides and animal products.
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Amyris joined partnership with IDRI (Infectious Disease Research Institute) in July, 2020 for a planned COVID-19 RNA (ribonucleic acid) vaccine technology program. The program combines IDRI's expertise in combating infectious diseases with Amyris' fermentation platform technology, with the goal to create semi- synthetic squalene-based adjuvants at scale. IDRI's RNA vaccine platform is expected to offer significant differentiated advantages over other RNA vaccines currently in development and will be further enhanced by a scalable Amyris adjuvant.
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In Europe, the drugs were predominantly purchased from websites, but in the US they were mainly sold in small independent stores such as gas stations and head shops. In the US, this often made them easier to obtain than cigarettes and alcohol. Bath salts have also been sold online in small packets. Hundreds of other designer drugs or "legal highs" have been reported, including artificial chemicals such as synthetic cannabis and semi-synthetic substances such as methylhexaneamine.
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Dihydroartemisinin (also known as dihydroqinghaosu, artenimol or DHA) is a drug used to treat malaria. Dihydroartemisinin is the active metabolite of all artemisinin compounds (artemisinin, artesunate, artemether, etc.) and is also available as a drug in itself. It is a semi-synthetic derivative of artemisinin and is widely used as an intermediate in the preparation of other artemisinin-derived antimalarial drugs. It is sold commercially in combination with piperaquine and has been shown to be equivalent to artemether/lumefantrine.
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Many inhibitors of Glucose-6-Phosphate Translocase of novel, semi-synthetic or natural origin are known and of medical importance. Genetic algorithms for synthesizing novel inhibitors of G6PT1 have been developed and utilized in drug discovery. Inhibitors of G6PT1 are the most studied as this subunit catalyzes the rate limiting step in glucose production through gluconeogenesis or glycogenolysis, and without its function these two processes could not occur. This inhibition holds great potential in drug development (discussed in "Medical and Disease Relevance").
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Production of antibiotics is a naturally occurring event, that thanks to advances in science can now be replicated and improved upon in laboratory settings. Due to the discovery of penicillin by Alexander Fleming, and the efforts of Florey and Chain in 1938, large-scale, pharmaceutical production of antibiotics has been made possible. As with the initial discovery of penicillin, most antibiotics have been discovered as a result of happenstance. Antibiotic production can be grouped into three methods: natural fermentation, semi-synthetic, and synthetic.
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The 3,6-diesters of morphine are drugs with more rapid and complete central nervous system penetration due to increased lipid solubility and other structural considerations. The prototype for this subgroup of semi-synthetic opiates is heroin and the group also includes dipropanoylmorphine, diacetyldihydromorphine, disalicylmorphine and others. Whilst this produces an enhanced "bang" when the drug is administered intravenously, it cannot be distinguished from morphine via other routes, although the different side effect profile, including lower incidence of nausea, is very apparent.
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Coex preserves the physical and chemical characteristics of the raw material to which is applied. The main features of Coex materials are comfort, hydrophilicity, antistatic properties, mechanical resistance and a great versatility in the textile sector, like all natural and semi-synthetic cellulosic fibers. This materials are resistant to moths, mildew and sunlight. The main feature of biopolymers Coex is the flame resistance, they work with fireproof action, creating a barrier to the flames and not simply delaying the fire.
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He pioneered the use of nucleotide analogs, synthesized at the beginning of his career, in muscle research and later for Ras-family GTPases, leading to the first ever structure determination of an unstable protein-substrate complex (Ras:GTP). Innovative use of semi-synthetic proteins led to an understanding of transport mechanisms of Rab GTPases and to resolution of a longstanding controversy concerning targeting of these proteins to membranes. His group discovered and characterized hitherto unrecognized covalent modifications of Rab proteins by bacteria.
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Earlier, the artificial strings of DNA did not encode for anything, but scientists speculated they could be designed to manufacture new proteins which could have industrial or pharmaceutical uses. Transcription of DNA containing unnatural base pair and translation of corresponding mRNA were actually achieved recently. On November 2017, the same team at the Scripps Research Institute that first introduced two extra nucleobases into bacterial DNA, reported having constructed a semi-synthetic E. coli bacteria able to make proteins using such DNA.
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Venter was featured in Time magazine's "The Top 10 Everything of 2008" article. Number three in 2008's Top 10 Scientific Discoveries was a piece outlining his work stitching together the 582,000 base pairs necessary to invent the genetic information for a whole new bacterium. On May 20, 2010, Venter announced the creation of first self-replicating semi-synthetic bacterial cell. In the June 2011 issue of Men's Journal, Venter was featured as the "Survival Skills" celebrity of the month.
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Scientists at Pfizer led by Lloyd Conover modified these compounds, which led to the invention of tetracycline itself, the first semi- synthetic antibiotic. Charlie Stephens' group at Pfizer worked on further analogs and created one with greatly improved stability and pharmacological efficacy: doxycycline. It was clinically developed in the early 1960s and approved by the FDA in 1967. As its patent grew near to expiring in the early 1970s, the patent became the subject of lawsuit between Pfizer and International RectifierPfizer, Inc. v.
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Methyldihydromorphine is a semi-synthetic opioid originally developed in Germany in 1936, controlled under both domestic law and UN conventions because of its possible potential for abuse. Methyldihydromorphine is related to heterocodeine and is not a synonym for dihydrocodeine or dihydroheterocodeine (6-methoxydihydromorphine). This compound is a derivative of hydromorphone It has been found to be 33 per cent the analgesic potency of morphine with a substantially longer duration of action. So far, little is currently known about this compound.
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Lincomycin is primarily isolated from fermentations of Streptomyces lincolnensis, while clindamycin is prepared semi-synthetically. While several hundred synthetic and semi-synthetic derivatives of lincosamides have been prepared, only lincomycin A and clindamycin are used in clinical practice due to issues with toxicity and low biological activity in other lincosamide antibiotics. Chemical synthesis of lincomycin A. Propylproline and methylthio-lincosamide are joined via a condensation reaction. This reaction forms N-demethyllincomycin A, which is methylated via S-adenosylmethionine to form lincomycin A.
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Julien, Robert M. See A Primer of Drug Action full citation above. Now, the term is used in a number of ways. Some people might define narcotics as substances that bind at opioid receptors (cellular membrane proteins activated by substances like heroin or morphine), while others refer to any illicit substance as a narcotic. From a U.S. legal perspective, narcotics refer to opium, opium derivatives, and their semi- synthetic substitutes,Narcotics Drug Addiction Help Rehabilitation Recovery Resource. Drug-rehab-referral.org.
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Pyritinol also called pyridoxine disulfide or pyrithioxine (European drug names Encephabol, Encefabol, Cerbon 6) is a semi-synthetic water-soluble analog of vitamin B6 (Pyridoxine HCl). It was produced in 1961 by Merck Laboratories by bonding 2 vitamin B6 compounds (pyridoxine) together with a disulfide bridge. Since the 1970s, it has been a prescription and OTC drug in several countries for cognitive disorders, rheumatoid arthritis, and learning disorders in children. Since the early 1990s it has been sold as a nootropic dietary supplement in the United States.
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RB-64 or 22-thiocyanatosalvinorin A is a semi-synthetic salvinorin derivative and a κ-opioid receptor (KOR) agonist which is used in scientific research. Its most remarkable property is its biased activity in signal transduction in favour of G protein versus β-arrestin-2, a phenomenon which is called functional selectivity or biased agonism. RB-64 has a bias factor of 96 and is analgesic with fewer of the prototypical side-effects associated with unbiased KOR agonists. The analgesia-like effect is long-lasting.
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Stauprimide is a semi-synthetic analog of the staurosporine family of indolocarbazoles. Stauprimide was first published in 1994 as part of an extensive structure-activity investigation to improve the selective inhibition of protein kinase C as a potential antitumor agent. More recently, stauprimide has been shown to increase the efficiency of the directed differentiation of mouse and human embryonic stem cells in synergy with defined extracellular signaling cues. Stauprimide interacts with NME2 (PUF) transcription factor to down-regulate c-Myc expression, leading to differentiation of stem cells.
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In 2010 Venter and colleagues created Mycoplasma mycoides strain JCVI-syn1.0 with a synthetic genome. Initially the synthetic construct did not work, so to pinpoint the error—which caused a delay of 3 months in the whole project—a series of semi-synthetic constructs were created. The cause of the failure was a single frameshift mutation in DnaA, a replication initiation factor. The purpose of constructing a cell with a synthetic genome was to test the methodology, as a step to creating modified genomes in the future.
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The physiological behavior of morphinans (naturally occurring and semi-synthetic derivatives) is thought to be associated with the aromatic A ring, the nitrogen-containing D ring and the "bridge" between these two rings formed by carbons 9, 10 and 11 of the core, with the D ring "above" the core (levorotatory). Small groups are usually found on morphinan derivatives at carbons 3 and 6. Many such derivatives have an epoxy group between carbons 4 and 5 (i.e., 4,5α-epoxy), thereby forming an E ring.
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Ukrain (; also called celandine) is the trademarked name of a semi-synthetic substance derived from the plant Chelidonium majus and promoted as a drug to treat cancer and viral infections, including HIV and hepatitis. It was created in 1978, by a Ukrainian chemist Vasyl Novytskyi (). Ukrain is named after the nation of Ukraine and is produced by the Austrian company Nowicky Pharma. According to the American Cancer Society and the Memorial Sloan-Kettering Cancer Center, there is no evidence that Ukrain is an effective cancer treatment.
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Dihydroartemisinin (also known as dihydroqinghaosu, artenimol or DHA) is a drug used to treat malaria. Dihydroartemisinin is the active metabolite of all artemisinin compounds (artemisinin, artesunate, artemether, etc.) and is also available as a drug in itself. It is a semi-synthetic derivative of artemisinin and is widely used as an intermediate in the preparation of other artemisinin-derived antimalarial drugs. Piperaquine is an antimalarial drug, a bisquinoline first made in the 1960s, and used extensively in China and Indochina as prophylaxis and treatment during the next 20 years.
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Scientists at the Italian drug company Achifar discovered rifabutin in 1975. (Eventually Archifar became part of Farmitalia Carlo Erba, a unit of the conglomerate Montedison which was subsequently bought by Pharmacia) This company's Adria Laboratories subsidiary filed for Food and Drug Administration (FDA) approval of rifabutin under the brand name Mycobutin in the early 1990s and the drug gained FDA approval in December 1992. Rifabutin is primarily bactericidal antibiotic drug used to treat tuberculosis. Its effect on bacteria is based on the DNA-dependent RNA polymerase blocking drug rifamycin S, a semi-synthetic derivative.
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Salvinorin B methoxymethyl ether (2-O-methoxymethylsalvinorin B) is a semi- synthetic analogue of the natural product salvinorin A used in scientific research. It has a longer duration of action of around 2–3 hours, compared to less than 30 minutes for salvinorin A, and has increased affinity and potency at the κ-opioid receptor. It is made from salvinorin B, which is most conveniently made from salvinorin A by deacetylation. The crystal structure reveals that the methoxy group overlaps with the acetyl group of salvinorin A, but with a different orientation.
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Vancomycin was isolated in 1953 and used clinically by 1958, while teicoplanin was discovered in 1978 and became clinically-available in 1984. . Telavancin is a semi-synthetic lipoglycopeptide derivative of vancomycin approved by FDA in 2009. Teicoplanin has historically been more widely-marketed - and thus more used - in Europe compared to the U.S. It has more fatty acid chains than vancomycin and is considered to be 50 to 100 times more lipophillic. Teicoplanin also has an increased half-life compared to vancomycin, as well as having better tissue penetration.
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Dihydrocodeine is a semi-synthetic opioid analgesic prescribed for pain or severe dyspnea, or as an antitussive, either alone or compounded with paracetamol (acetaminophen) (as in co-dydramol) or aspirin. It was developed in Germany in 1908 and first marketed in 1911. Commonly available as tablets, solutions, elixirs, and other oral forms, dihydrocodeine is also available in some countries as an injectable solution for deep subcutaneous and intra- muscular administration. As with codeine, intravenous administration should be avoided, as it could result in anaphylaxis and life-threatening pulmonary edema.
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The environmental impacts caused by the production of illicit drugs is an often neglected topic when analysing the effects of such substances. However, due to the clandestine nature of illicit drug production, its effects can be highly destructive yet difficult to detect and measure. The consequences differ depending upon the drug being produced but can be largely categorised into impacts caused by natural drugs or caused by synthetic/semi-synthetic drugs. Natural drugs refer to drugs which are primarily extracted from a natural source such as cocaine or cannabis.
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Opium concentrates using solvents other than acidifed or plain water are often but not necessarily called PSC. Poppies of the Norman and Przemko strains contain much higher amounts of thebaine and oripavine and have morphine concentrations down to under 1 per cent. versus up to 26 per cent in high-morphine strains. At least one manufacturer, Tasmanian Alkaloids, produces both high-morphine and high-thebaine/oripavine types of poppy straw concentrate; the latter is used by pharmaceutical manufacturers to make semi-synthetic and synthetic opioids such as oxycodone, etorphine, butorphanol and a number of others.
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Pyrethrins have shorter environmental persistence than synthetic pyrethroids because their chemical structure is more susceptible to the presence of UV light and changes in pH. They pose a toxic hazard normally not found in commercial pyrethroid to mammals and humans. While pyrethrum extract is composed of 6 esters which are insecticidal, the semi-synthetic pyrethroid is a composed of only one chemically active compound. As a result, the liver has to break down these additional chains first, which allows the toxicity levels to rise within the bloodstream, which can lead to hospitalization and even death.
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Heroin, the first semi-synthetic opioid, was first synthesized in 1874, but was not pursued until its rediscovery in 1897 by Felix Hoffmann at the Bayer pharmaceutical company in Elberfeld, Germany. From 1898 to 1910 heroin was marketed as a non-addictive morphine substitute and cough medicine for children. Because the lethal dose of heroin was viewed as a hundred times greater than its effective dose, heroin was advertised as a safer alternative to other opioids. By 1902, sales made up 5 percent of the company's profits, and "heroinism" had attracted media attention.
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Pentamorphone (14β-pentylaminomorphinone, RX-77989) is a semi-synthetic opiate derivative related to compounds such as morphine, hydromorphone and oxymorphone. Developed in 1984, it is a potent opioid analgesic several times stronger than fentanyl, and with a similarly fast onset of effects and short duration of action. It was found to produce relatively little respiratory depression compared to other potent opioid agonists, but its analgesic effects were somewhat disappointing in human trials, and while pentamorphone had some slight advantages over fentanyl these were not sufficient to warrant its introduction into clinical use.
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The Bentley compounds are a class of semi-synthetic opioids that were first synthesized by K. W. Bentley by Diels-Alder reaction of thebaine with various dienophiles. The compounds are also known as thevinols, orvinols, or bridged oripavine derivatives, due to the characteristic 6,14-endo-etheno- bridge and substitution at the 7α position. Buprenorphine and etorphine are perhaps the best known of the family, which was the first series of extremely potent μ-opioid agonists, with some compounds in the series having over many thousands of times the analgesic potency of morphine.
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The first modern example of polymer science is Henri Braconnot's work in the 1830s. Henri, along with Christian Schönbein and others, developed derivatives of the natural polymer cellulose, producing new, semi-synthetic materials, such as celluloid and cellulose acetate. The term "polymer" was coined in 1833 by Jöns Jakob Berzelius, though Berzelius did little that would be considered polymer science in the modern sense. In the 1840s, Friedrich Ludersdorf and Nathaniel Hayward independently discovered that adding sulfur to raw natural rubber (polyisoprene) helped prevent the material from becoming sticky.
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O-Acetylpsilocin (also known as psilacetin, 4-acetoxy-DMT, or 4-AcO-DMT) is a semi-synthetic psychoactive drug that has been suggested by David Nichols to be a potentially useful alternative to psilocybin for pharmacological studies, as they are both believed to be prodrugs of psilocin. However, some users report that O-acetylpsilocin's subjective effects differ from those of psilocybin and psilocin. It is the acetylated form of the psilocybin mushroom alkaloid psilocin and is a lower homolog of 4-AcO-MET, 4-AcO-DET, 4-AcO-MiPT and 4-AcO-DiPT.
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Vinblastine and vincristine , chemotherapy medications used to treat several types of cancers, are found in the plant and are biosynthesised from the coupling of the alkaloids catharanthine and vindoline. The newer semi-synthetic chemotherapeutic agent vinorelbine, used in the treatment of non-small-cell lung cancer, can be prepared either from vindoline and catharanthine or from the vinca alkaloid leurosine, in both cases via anhydrovinblastine. The insulin-stimulating vincoline has been isolated from the plant. Rosinidin is the pink anthocyanidin pigment found in the flowers of C. roseus.
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Benzylmorphine (Peronine) is a semi-synthetic opioid narcotic introduced to the international market in 1896 and that of the United States very shortly thereafter. It is much like codeine, containing a benzyl group attached to the morphine molecule just as the methyl group creates codeine and the ethyl group creates ethylmorphine or dionine (used as a generic name for that drug just as peronine is for benzylmorphine). It is about 90% as strong as codeine by weight. This drug, the benzyl ether of morphine, should not be confused with dibenzoylmorphine, an ester of morphine comparable to heroin.
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Bardoxolone methyl (also known as “RTA 402”, “CDDO-methyl ester”, and CDDO-Me) is an experimental and orally-bioavailable semi-synthetic triterpenoid, based on the scaffold of the natural product oleanolic acid. Pre-clinical studies indicate that the compound acts as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway. A phase 3 clinical trial evaluating bardoxolone methyl for the treatment of chronic kidney disease (CKD) was terminated in October 2012 after patients treated with the drug were found to have experienced a higher rate of heart-related adverse events, including heart failure, hospitalizations, and deaths.
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Dihydroetorphine was developed by K. W. Bentley at McFarlan-Smith in the 1960s and is a potent opioid analgesic used mainly in China. It is a derivative of the better-known opioid etorphine, a very potent veterinary painkiller and anesthetic medication used primarily for the sedation of large animals such as elephants, giraffes, and rhinos. Dihydroetorphine is a semi-synthetic opioid used mainly as a strong painkiller for humans. It is several thousand times stronger than morphine (between 1000x and 12000x more potent depending what method is used for comparison), although it is poorly absorbed when taken orally.
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Rivastigmine was developed by Marta Weinstock- Rosin of the Department of Pharmacology at the Hebrew University of Jerusalem and sold to Novartis by Yissum for commercial development. It is a semi- synthetic derivative of physostigmine. It has been available in capsule and liquid formulations since 1997.Novartis Pharmaceuticals Corporation "Exelon Product Insert" June 2006 In 2006, it became the first product approved globally for the treatment of mild to moderate dementia associated with Parkinson's disease;Approves the First Treatment for Dementia of Parkinson's Disease U.S. FDA News Release and in 2007 the rivastigmine transdermal patch became the first patch treatment for dementia.
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The chemical structure of cellulose with substitutions that characterize coex materials. Coex is a biopolymer with flame-retardant properties derived from the functionalization of cellulosic fibers such as cotton, linen, jute, cannabis, coconut, ramie, bamboo, raffia palm, stipa, abacà, sisal, nettle and kapok. The treatment effectiveness was also proven on wood and semi-synthetic fibers such as cellulose acetate, cellulose triacetate, viscose, modal, lyocell and cupro. The material is obtained by sulfation and phosphorylation reactions on glucan units linked to each other in position 1,4 and in particular on the secondary and tertiary hydroxyl groups of cellulosic biopolymer.
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The streptogramin antibiotics were identified almost 50 years ago, but have only recently found clinical use as a consequence of the increase in multidrug-resistant bacteria. They present poor solubility in aqueous solution, and this has limited their clinical use; however, the natural products still find use as feed additives in agriculture. Medicinal chemists at Rhône-Poulenc worked in the preparation of semi-synthetic, water-soluble, derivatives of pristinamycin IA (B type streptogramin) and pristinamycin IIA (A type streptogramin) giving rise to quinupristin and dalfopristin, respectively, which, when administered in a 3:7 ratio, comprise the 1999 FDA approved drug Synercid.
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The chemical structure of penicillin was first proposed by Edward Abraham in 1942. Dorothy Hodgkin determined the correct chemical structure of penicillin using X-ray crystallography at Oxford in 1945. In Kundl, Tyrol, Austria, in 1952, Hans Margreiter and Ernst Brandl of Biochemie (now Sandoz) developed the first acid-stable penicillin for oral administration, penicillin V. American chemist John C. Sheehan of the Massachusetts Institute of Technology completed the first chemical synthesis of penicillin in 1957. The second-generation semi- synthetic β-lactam antibiotic methicillin, designed to counter first- generation-resistant penicillinases, was introduced in the United Kingdom in 1959.
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Chronic toxicity in humans occurs most quickly through respiration into the lungs, or more slowly through absorption through the skin. Allergic reactions may occur after exposure, leading to itching and irritated skin as well as burning sensations. These types of reactions are rare because the allergenic component of pyrethrin in semi-synthetic phritoids has been removed. The metabolite compounds of pyrethrin are less toxic to mammals than their originators, and compounds are either broken down in the liver or gastrointestinal tract, or excreted through feces; no evidence of storage in tissues has been found [citation needed].
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When halogenated morphides and codides are used for research or industrial uses, they are often synthesised on-site. Chloromorphide is one of a series of opioids known as morphides and codides, which are important precursors and intermediates in the synthesis of semi-synthetic opioid analgesic drugs, especially those with additions, substitutions, or other modifications at the 7, 8, and/or 14 positions on the morphine carbon skeleton. Semisynthetics with changes at other positions can also be made from these compounds. The codeine analog of chloromorphide is α-chlorocodide (alphachlorcodide), an intermediate in one method of desomorphine synthesis which uses codeine as precursor.
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One of them, targeting the Haemophilus influenzae b (HIB) bacteria, has been designed jointly with the Cuban researcher Vincente Verez Bencomo to prevent lethal meningitis and pneumonia in developing countries. It is the first human semi-synthetic glycoconjugate vaccine approved and remains the only one. In use since 2004, more than 34 million doses have been distributed to children in several countries including Vietnam, Syria, Brazil, Venezuela and Angola, eradicating the infectious disease in Cuba. Rene Roy is a cofounder of Glycovax Pharma, a biotech company operating in Montreal, developing glycochemistry-based treatments against cancer and other disease with unmet medical needs.
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Household items made of various types of plastic Plastics are a wide range of synthetic or semi-synthetic organic compounds that are malleable and so can be molded into solid objects. Plasticity is the general property of all materials which can deform irreversibly without breaking but, in the class of moldable polymers, this occurs to such a degree that their actual name derives from this specific ability. Plastics are typically organic polymers of high molecular mass and often contain other substances. They are usually synthetic, most commonly derived from petrochemicals, however, an array of variants are made from renewable materials such as polylactic acid from corn or cellulosics from cotton linters.
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Teva has 21 API production facilities located in Israel, Hungary, Italy, the U.S., the Czech Republic, India, Mexico, Puerto Rico, Monaco, China and Croatia. TAPI's holds expertise in a variety of production technologies, including chemical synthesis, semi-synthetic fermentation, enzymatic synthesis, high potent manufacturing, plant extract technology, synthetic peptides, vitamin D derivatives and prostaglandins. Also, its advanced technology and expertise in the field of solid state particle technology enables it to meet specifications for particle size distribution (PSD), bulk density, specific surface area, polymorphism, as well as other characteristics. Teva's API facilities meet all applicable current Good Manufacturing Practices (cGMP) requirements under U.S., European, Japanese, and other applicable quality standards.
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Salvinorin A is one of several structurally related salvinorins found in the Salvia divinorum plant. Salvinorin A seems to be the only naturally occurring salvinorin that is psychoactive. Salvinorin A can be synthesized from salvinorin B by acetylation, and de-acetylated salvinorin A becomes analog to salvinorin B. Research has produced a number of semi-synthetic compounds. Most derivatives are selective kappa opioid agonists as with salvinorin A, although some are even more potent, with the most potent compound 2-methoxymethyl salvinorin B being ten times stronger than salvinorin A. Some derivatives, such as herkinorin, reduce kappa opioid action and instead act as mu opioid agonists.
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Prepared substances (as opposed to those that occur naturally in a consumable form, such as cannabis and psilocybin mushrooms) require reagents. Some drugs, like cocaine and morphine, are extracted from plant sources and refined with the aid of chemicals. Semi-synthetic drugs such as heroin are made starting from alkaloids extracted from plant sources which are the precursors for further synthesis. In the case of heroin, a mixture of alkaloids is extracted from the opium poppy (Papaver somniferum) by incising its seed capsule, whereupon a milky fluid (the opium 'latex') bleeds out of the incisions which is then left to dry out and scraped off the bulbs, yielding raw opium.
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Pethidine is the most widely used opioid in labour and delivery but has fallen out of favour in some countries such as the United States in favour of other opioids, due to its potential drug interactions (especially with serotonergics) and its neurotoxic metabolite, norpethidine. It is still commonly used in the United Kingdom and New Zealand, and was the preferred opioid in the United Kingdom for use during labour, but has been superseded somewhat by diamorphine (heroin) and other strong semi-synthetic opioids (e.g. hydromorphone) to avoid serotonin interactions since the mid-2000s. Pethidine is the preferred painkiller for diverticulitis, because it decreases intestinal intraluminal pressure.
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Capillary action through synthetic mesh is the result of the intermolecular attraction between moisture and semi-synthetic polymers, causing a current of thermionic energy through a specific pathway within a mesh material. The combination of the adhesive forces and the surface tension that arises from cohesion produces the characteristic upward curve in a fluid, such as water. Capillarity is the result of cohesion of water molecules and adhesion of those molecules to the solid material forming the void. As the edges of the material are brought closer together, such as in a very narrow path, the interaction causes the liquid to be drawn away from the original source.
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Plastic household items Eberhard Bosslet 2001 Biomorph sculptures "Stool Archipelago", "Island of Growth", "stump stools" are groups of sculptures made of fiberglass plastic on the basis of known organic forms. Dresden Conservation and restoration of objects made from plastics is an activity dedicated to the conservation of objects of historical and personal value made from plastics. When applied to cultural heritage this activity is generally undertaken by a conservator-restorer. Within museum collections there are a variety of artworks and artifacts that are composed of plastic material whether they are synthetic or semi-synthetic; these were created for a range of uses from artistic, to technical, to domestic use.
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A freshly-scored opium poppy seedpod bleeding latex. Morphine is the most abundant opiate found in opium, the dried latex extracted by shallowly scoring the unripe seedpods of the Papaver somniferum poppy. Morphine is generally 8–14% of the dry weight of opium, although specially bred cultivars reach 26% or produce little morphine at all (under 1%, perhaps down to 0.04%). The latter varieties, including the 'Przemko' and 'Norman' cultivars of the opium poppy, are used to produce two other alkaloids, thebaine and oripavine, which are used in the manufacture of semi-synthetic and synthetic opioids like oxycodone and etorphine and some other types of drugs.
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The Madagascan periwinkle Catharanthus roseus L. is the source for a number of important natural products, including catharanthine and vindoline and the vinca alkaloids it produces from them: leurosine and the chemotherapy agents vinblastine and vincristine, all of which can be obtained from the plant. The newer semi-synthetic chemotherapeutic agent vinorelbine, which is used in the treatment of non-small-cell lung cancer and is not known to occur naturally. However, it can be prepared either from vindoline and catharanthine or from leurosine, in both cases by synthesis of anhydrovinblastine. The leurosine pathway uses the Nugent–RajanBabu reagent in a highly chemoselective de- oxygenation of leurosine.
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The replacement of the ester group with an amide group at the C-16 resulted in the development of vindesine. Similarly replacement of the acetyl group at C-16 with L-trp-OC2H5, d-Ala(P)-(OC2H5)2, L-Ala(P)-(OC2H5)2 and I-Vla(P)-(OC2H5)2 gave rise to new analogues having anti- tubulin activity. Also it was found that the vindoline's indole methyl group is a useful position to functionalize potentially and develop new, potent vinblastine derivatives. A new series of semi-synthetic C-16 -spiro-oxazolidine-1,3-diones prepared from 17-deacetyl vinblastine showed good anti-tubulin activity and lower cytotoxicity.
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Morphinan has a phenanthrene core structure with the A ring remaining aromatic and the B and C rings being saturated, and an additional nitrogen-containing, six-membered, saturated ring, the D ring, being attached to carbons 9 and 13 of the core, and with the nitrogen being at position 17 of the composite. Of the major naturally occurring opiates of the morphinan type—morphine, codeine and thebaine—thebaine has no therapeutic properties (it causes seizures in mammals), but it provides a low-cost feedstock for the industrial production of at least four semi-synthetic opiate agonists, including hydrocodone, hydromorphone, oxycodone and oxymorphone, and, perhaps more significantly, the opioid antagonist naloxone.
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Docetaxel is of the chemotherapy drug class; taxane, and is a semi-synthetic analogue of paclitaxel (Taxol), an extract from the bark of the rare Pacific yew tree, Taxus brevifolia. Due to scarcity of paclitaxel, extensive research was carried out leading to the formulation of docetaxel – an esterified product of 10-deacetyl baccatin III, which is extracted from the renewable and more readily available leaves of the European yew tree. Docetaxel differs from paclitaxel at two positions in its chemical structure. It has a hydroxyl functional group on carbon 10, whereas paclitaxel has an acetate ester, and a tert-butyl carbamate ester exists on the phenylpropionate side chain instead of the benzamide in paclitaxel.
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Saridegib, also known as IPI-926, is an experimental drug candidate undergoing clinical trials for the treatment of various types of cancer, including hard- to-treat hematologic malignancies such as myelofibrosis and ligand-dependent tumors such as chondrosarcoma. IPI-926 exhibits its pharmacological effect by inhibition of the G protein-coupled receptor smoothened, a component of the hedgehog signaling pathway. Chemically, it is a semi-synthetic derivative of the alkaloid cyclopamine. The process begins with cyclopamine extracted from harvested Veratrum californicum which is taken through a series of alterations resulting in an analogue of the natural product cyclopamine, making IPI-926 the only compound in development/testing that is not fully synthetic.
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The Madagascan periwinkle Catharanthus roseus L. is the source for a number of important natural products, including catharanthine and vindoline and the vinca alkaloids it produces from them: leurosine and the chemotherapy agents vinblastine and vincristine, all of which can be obtained from the plant. The newer semi-synthetic chemotherapeutic agent vinorelbine is used in the treatment of non-small-cell lung cancer and is not known to occur naturally. However, it can be prepared either from vindoline and catharanthine or from leurosine, in both cases by synthesis of anhydrovinblastine, which "can be considered as the key intermediate for the synthesis of vinorelbine." The leurosine pathway uses the Nugent–RajanBabu reagent in a highly chemoselective de-oxygenation of leurosine.
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The payoff in the native chemical ligation method is that coupling long peptides by this technique is in many cases nearly quantitative and provides synthetic access to large peptides and proteins otherwise impossible to make, due to length or decoration by post- translational modification. Native chemical ligation forms the basis of modern chemical protein synthesis, and has been used to prepare numerous proteins and enzymes by total chemical synthesis. Polypeptide C-terminal thioesters produced by recombinant DNA techniques can be reacted with an N-terminal Cys containing polypeptide by the same native ligation chemistry to provide very large semi-synthetic proteins. Native chemical ligation of this kind using a recombinant polypeptide segment is known as Expressed Protein Ligation.
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Using a semi-synthetic approach, a diketide intermediate may be added either in vitro or in vivo to a DEBS complex in which the activity of the first KS has been deleted. This means that the diketide will load onto the second KS (in module 2 of DEBS) and be processed all the way to the end as normal. It has been shown that this second KS is fairly nonspecific and a large variety of synthetic diketides can be accepted and subsequently fully elongated and released. However, it has also been seen that this KS is not highly tolerant of structural changes at the C2 and C3 positions, especially if the stereochemistry is altered.
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Xiyanping (喜炎平) is an anti-inflammatory and antiviral preparation developed and licensed for use in China. It is a semi-synthetic injectable product derived from the active component of the plant Andrographis paniculata (Chuan Xin Lian, 穿心蓮), which is used in Traditional Chinese medicine. Xiyanping is primarily composed of 9-dehydro-17-hydro-andrographolide and sodium 9-dehydro-17-hydro-andrographolide-19-yl sulfate. It is used mainly in the treatment of hand, foot and mouth disease, diarrhea, upper respiratory tract infections and viral pneumonia,Sun SG, Shi YF, Yan H, Li Y, Wang R, Wang SH, Sun XD. Xiyanping Injection in Treatment of Viral Pneumonia in Children: A Meta-analysis of Random Control Trials.
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Heroin, a powerful opioid and narcotic The term narcotic (, from ancient Greek ναρκῶ narkō, "to make numb") originally referred medically to any psychoactive compound with sleep-inducing properties, and euphoric properties as well. In the United States, it has since become associated with opiates and opioids, commonly morphine and heroin, as well as derivatives of many of the compounds found within raw opium latex. The primary three are morphine, codeine, and thebaine (while thebaine itself is only very mildly psychoactive, it is a crucial precursor in the vast majority of semi-synthetic opioids, such as oxycodone or hydrocodone). Legally speaking, the term "narcotic" may be imprecisely defined and typically has negative connotations.
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Bacterial cell wall synthesis and the role of PBPs in its synthesis is a very good target for drugs of selective toxicity because the metabolic pathways and enzymes are unique to bacteria. Resistance to antibiotics has come about through overproduction of PBPs and formation of PBPs that have low affinity for penicillins (among other mechanisms such as lactamase production). These experiments change the structure of PBP by adding different amino acids into the protein, allowing for new discovery of how the drug interacts with the protein. Research on PBPs has led to the discovery of new semi-synthetic β-lactams, wherein altering the side-chains on the original penicillin molecule has increased the affinity of PBPs for penicillin, and, thus, increased effectiveness in bacteria with developing resistance.
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The R&D; group at teva api consists of a team of over 760 top scientists located in 7 development centers worldwide: A large center in Israel (synthetic products and peptides), a large center in Hungary (fermentation and semi-synthetic products), and a facility in India and additional sites in Italy, Croatia, Mexico and the Czech Republic (development of high potency API). teva api's R&D; focuses on the development of processes for the manufacturing of API, including intermediates, chemical and biological (fermentation), which are of interest to the generic drug industry, as well as Teva's proprietary drugs. The API R&D; division also seeks methods to continuously reduce API production costs, enabling teva api to improve its cost structure.
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Earliest uses of Ephedra spp. (mahuang) for specific illnesses date back to 5000 BC. Ephedrine and isomers were already isolated in 1881 from Ephedra dystachia and characterized by the Japanese organic chemist Nagai Nagayoshi of the 19th century. His work to access Ephedra drug materials to isolate a pure pharmaceutical substance, and the systematic production of semi-synthetic derivatives thereof is relevant still today as the three species Ephedra sinica, Ephedra vulgaris and to a lesser extent Ephedra equisetina are commercially grown in Mainland China as a source for natural ephedrines and isomers for use in pharmacy. E. sinica and E. vulgaris usually carry six optically active phenylethylamines, mostly ephedrine and pseudoephedrine with minor amounts of norephedrine, norpseudoephedrine as well as the three methylated analogs.
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The oil-base stock can be petroleum, castor oil, semi-synthetic or synthetic oil and is mixed (or metered by injection) with petrol/gasoline at a volumetric fuel-to-oil ratio ranging from 16:1 to as low as 100:1. To avoid the high emissions and oily deposits on spark plugs, modern two-strokes, especially for small engines such as garden equipment and chainsaws, may now demand a synthetic oil and can suffer from oiling problems otherwise. Engine original equipment manufacturers (OEMs) introduced pre- injection systems (sometimes known as "auto-lube") to engines to operate from a 32:1 to 100:1 ratio. Oils must meet or exceed the following typical specifications: TC-W3TM, NMMA, [API] TC, JASO FC, ISO-L-EGC.
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Heroin-assisted treatment (HAT), or diamorphine assisted treatment, refers to the prescribing of semi-synthetic heroin to opiate addicts who do not benefit from or cannot tolerate treatment with one of the established drugs used in opiate replacement therapy like methadone or buprenorphine (brand name Subutex). For this group of patients, heroin- assisted treatment has proven superior in improving their social and health situation. It has also been shown to save money, as it significantly reduces costs incurred by trials, incarceration, health interventions and delinquency. It has also drastically reduced overdose deaths in the countries utilizing it, as patients take their dose in a controlled, professionally supervised setting, and Narcan (naloxone) is on hand in the case of an accidental overdose.
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René Roy (born November 4, 1952) is a Canadian organic chemist from Quebec, specializing in glycobiology and carbohydrate chemistry. He is professor emeritus, Department of chemistry, at the Université du Québec à Montréal (UQAM) and associate professor at the Institut National de la Recherche Scientifique (INRS) – Institut Armand-Frappier (IAF). He is the founder and former director of PharmaQAM, a biopharmaceutical research center based at UQAM, focusing on the discovery of new bioactive molecules, their mechanism of action and the vectorization of drugs. He is a pioneer in the development of synthetic glycoconjugate vaccines both for human and veterinary health, having co-developed the first and sole marketed semi-synthetic vaccine for human use, preventing bacterial meningitis and pneumonia in developing countries.
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Plastics have become an integral component of life and many plastic objects have become staple icons or objects worth preserving for the future. Although relatively new material for museum collections, plastics having originated in the 19th century, they are deteriorating at an alarming rate, risking the loss not only of the objects themselves, but through their deterioration processes they place objects within their vicinity at risk too. Plastics are made of synthetic, semi-synthetic and organic material, all of which are susceptible to degradation, with their respective off-gassing being harmful to the objects nearby in museum collections. Recent changes in plastic manufacturing, as a result of environmental concerns, towards biodegradable plastics, have a potentially negative effect upon the long term stability of such objects within museum collections.
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Some purpose-developed strains of poppy now produce opium that is up to 26% morphine by weight. A rough rule of thumb to determine the morphine content of pulverised dried poppy straw is to divide the percentage expected for the strain or crop via the latex method by eight or an empirically determined factor, which is often in the range of 5 to 15. The Norman strain of P. Somniferum, also developed in Tasmania, produces down to 0.04% morphine but with much higher amounts of thebaine and oripavine, which can be used to synthesise semi-synthetic opioids as well as other drugs like stimulants, emetics, opioid antagonists, anticholinergics, and smooth-muscle agents. In the 1950s and 1960s, Hungary supplied nearly 60% of Europe's total medication-purpose morphine production.
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Chemical structure and expected channel forming mechanism for the first attempt at preparing a synthetic ion channel While semi-synthetic ion channels, often based on modified peptidic channels like gramicidin, had been prepared since the 1970s, the first attempt to prepare a synthetic ion channel was made in 1982 using a substituted β-cyclodextrin. Inspired by gramicidin, this molecule was designed to be a barrel-shaped entity spanning a single leaflet of a bilayer membrane, becoming "active" only when two molecules in opposite leaflets come together in an end-to-end fashion. While the compound does induce ion-fluxes in vesicles, the data does not unambiguously show channel formation (as opposed to other transport mechanisms; see Mechanism). Na+ transport by such channels was first reported by two groups of investigators in 1989–1990.
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Terramycin, an early antibiotic developed by Pfizer in Kent, synthesised by American chemist Robert Burns Woodward, and led to the common antibiotic doxycycline William Harvey of Folkestone, in Kent, discovered the circulation of blood. The Lilly Research Centre in Windlesham, Berkshire, part of Eli Lilly, developed Olanzapine in 1996 (for bipolar disorder, selling around $5bn worldwide annually). Beecham Research Laboratories at Brockham Park in 1959 discovered meticillin (or methicillin), the first semi-synthetic penicillin (beta-lactamase stable), deriving from their discovery in 1958 of 6-APA, the core constituent; the team, led by Prof George Rolinson, won the Mullard Award in 1971. Bipyridine compounds (Paraquat-Gramoxone and Diquat) were discovered for herbicide use in 1954 by William Boon at ICI's Plant Protection division at Jealott's Hill, being released onto the market in 1958.
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Chemical changes to the morphine molecule yield other euphorigenics such as dihydromorphine, hydromorphone (Dilaudid, Hydal), and oxymorphone (Numorphan, Opana), as well as the latter three's methylated equivalents dihydrocodeine, hydrocodone, and oxycodone, respectively; in addition to heroin, there are dipropanoylmorphine, diacetyldihydromorphine, and other members of the 3,6 morphine diester category like nicomorphine and other similar semi-synthetic opiates like desomorphine, hydromorphinol, etc. used clinically in many countries of the world but in many cases also produced illicitly in rare instances. In general, non-medical use of morphine entails taking more than prescribed or outside of medical supervision, injecting oral formulations, mixing it with unapproved potentiators such as alcohol, cocaine, and the like, or defeating the extended-release mechanism by chewing the tablets or turning into a powder for snorting or preparing injectables. The latter method can be as time-consuming and involved as traditional methods of smoking opium.
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Steroid saponins, for example, in Dioscorea wild yam the sapogenin diosgenin—in form of its glycoside dioscin—is an important starting material for production of semi-synthetic glucocorticoids and other steroid hormones such as progesterone. The ginsenosides are triterpene glycosides and Ginseng saponins from Panax Ginseng C. A. Meyer, (Chinese ginseng) and Panax quinquefolius (American Ginseng). In general, the use of the term saponin in organic chemistry is discouraged, because many plant constituents can produce foam, and many triterpene-glycosides are amphipolar under certain conditions, acting as a surfactant. More modern uses of saponins in biotechnology are as adjuvants in vaccines: Quil A and its derivative QS-21, isolated from the bark of Quillaja saponaria Molina, to stimulate both the Th1 immune response and the production of cytotoxic T-lymphocytes (CTLs) against exogenous antigens make them ideal for use in subunit vaccines and vaccines directed against intracellular pathogens as well as for therapeutic cancer vaccines but with the aforementioned side-effect of hemolysis.
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In 1973, Griffin wrote and self-published the book World Without Cancer and released it as a video; its second edition appeared in 1997. In the book and the video, Griffin asserts that cancer is a metabolic disease like a vitamin deficiency facilitated by the insufficient dietary consumption of amygdalin. He contends that "eliminating cancer through a nondrug therapy has not been accepted because of the hidden economic and power agendas of those who dominate the medical establishment" and he wrote, "at the very top of the world's economic and political pyramid of power there is a grouping of financial, political, and industrial interests that, by the very nature of their goals, are the natural enemies of the nutritional approaches to health." Since the 1970s, the use of laetrile (a semi-synthetic version of amygdalin) to treat cancer has been identified in the scientific literature as a canonical example of quackery and has never been shown to be effective in the treatment or prevention of cancer.
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Herkinorin is an opioid analgesic that is an analogue of the natural product Salvinorin A. It was discovered in 2005 during structure-activity relationship studies into neoclerodane diterpenes, the family of chemical compounds of which Salvinorin A is a member. Unlike Salvinorin A which is a selective κ-opioid agonist with no significant μ-opioid receptor affinity, herkinorin is a μ-opioid agonist with more than 100x higher μ-opioid affinity and 50x lower κ-opioid affinity compared to Salvinorin A. Herkinorin is a semi-synthetic compound, made from Salvinorin B, which is most conveniently made from Salvinorin A by deacetylation, as while both Salvinorin A and Salvinorin B are found in the plant Salvia divinorum, Salvinorin A is present in larger quantities. A study in primates showed it to act as both a peripherally active μ and κ agonist with a fast onset of action. The study did not find any evidence of central activity in primates and questions whether herkinorin's effects are due entirely to peripheral binding.
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