Someone in eating disorder recovery may refer to their "disordered eating" because they'd prefer not to be defined as an anorectic or a bulimic (quite understandably).
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Etolorex is an anorectic of the amphetamine class. It was never marketed.
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Levopropylhexedrine is also used as an anorectic under the brand name Eventin.
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Cloforex (Oberex) is an anorectic of the amphetamine class. It is a prodrug to chlorphentermine.
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Oxifentorex (INN) is an amphetamine described as an anorectic which does not appear to have ever been marketed.
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Picilorex (INN; brand name Roxenan) is an anorectic which is no longer marketed. It is a monoamine reuptake inhibitor.
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Fenisorex (INN, USAN, BAN) is an amphetamine-like anorectic drug which does not appear to have ever been marketed.
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Several studies have shown acute peripheral administration of PYY3-36 inhibits feeding of rodents and primates. Other studies on Y2R-knockout mice have shown no anorectic effect on them. These findings indicate PYY3-36 has an anorectic (losing appetite) effect, which is suggested to be mediated by Y2R. PYY-knockout female mice increase in body weight and fat mass.
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Acridorex (INN; BS 7573a) is an amphetamine which was investigated as an anorectic but does not appear to have ever been marketed.
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G-130 (GP-130, 2-Phenyl-5,5-dimethyltetrahydro-1,4-oxazine) \- Diethanolamine Derivatives. is a drug with stimulant and anorectic effects, related to phenmetrazine.
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The 5-HT2c receptor agonist Fenfluramine (market names Pondimin, Ponderax and Adifax) was discovered in 1972 as a result of research performed to identify anorectic compounds lacking the effects of psycho-stimulants and sympathomimetic agents (such as amphetamines). Prior to the discovery of fenfluramine, amphetamines were the primary form of anorectic drugs available, however the side effects made them difficult to use. Fenfluramine's anorectic effect is achieved through an increase in serotonin levels, imparting a sensation of fullness, which leads to a lower intake of food. Fenfluramine was sold as a racemic mixture of two enantiomers, dexfenfluramine and levofenfluramine.
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Morforex (INN; Bo 637), also referable to as N-morpholinoethylamphetamine, is an anorectic which was never marketed. It produces amphetamine as an active metabolite.
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Flucetorex (INN) is an amphetamine, which was investigated as an anorectic, but does not appear to have ever been marketed. It is related to fenfluramine.
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3-Benzhydrylmorpholine was developed by American Home Products in the 1950s, and is a drug with stimulant and anorectic effects, related to both pipradrol and phenmetrazine.
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SKF-38,393 is a synthetic compound of the benzazepine chemical class which acts as a selective D1/D5 receptor partial agonist. It has stimulant and anorectic effects.
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While accepting her award for Video of the Year, presented by legendary singer and actress Cher, Lady Gaga wore a dress made entirely from cuts of raw meat. The dress bore a resemblance to an artwork, Vanitas: Flesh Dress for an Albino Anorectic, created by Canadian artist Jana Sterbak in 1987.Vanitas: Flesh Dress for an Albino Anorectic – Collections – Walker Art Center . Collections.walkerart.org. Retrieved on 2013-08-25.
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Galnon is a drug which acts as a selective, non-peptide agonist at the galanin receptors GALR. It has anticonvulsant, anxiolytic, anorectic and amnestic effects in animal studies.
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NNC 38-1049 is a histamine antagonist selective for the H3 subtype. It has anorectic effects in animal studies and is being researched as a potential treatment for obesity.
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Levophacetoperane (Lidépran, Phacétoperane) is a psychostimulant developed by Rhône-Poulenc in the 1950s. The drug has been used as an antidepressant and anorectic. It is the reverse ester of methylphenidate.
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Dexfenfluramine, marketed as dexfenfluramine hydrochloride under the name Redux, is a serotonergic anorectic drug: it reduces appetite by increasing the amount of extracellular serotonin in the brain.Stuart Ira Fox. Human Physiology. Twelfth Edition.
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GW-803430 (GW-3430) is a drug used in scientific research and is a selective non-peptide antagonist at the melanin concentrating hormone receptor MCH1. In animal studies it has anxiolytic, antidepressant and anorectic effects.
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Obestatin is a hormone that is produced in specialized epithelial cells of the stomach and small intestine of several mammals including humans. Obestatin was originally identified as an anorectic peptide, but its effect on food intake remains controversial.
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2-Phenyl-3,6-dimethylmorpholine is a drug with stimulant and anorectic effects, related to phenmetrazine. Based on what is known from other phenylmorpholines with similar structure, it likely acts as a serotonin reuptake inhibitor and may produce antidepressant-like effects.
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VER-3323 is a drug which acts as a selective agonist for both the 5-HT2B and 5-HT2C serotonin receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT2A. It has potent anorectic effects in animal studies.
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Pentorex (Modatrop), also known as phenpentermine or α,β-dimethylamphetamine, is a stimulant drug related to phentermine which is used as an anorectic to assist with weight loss. It also acts as a diuretic. Pentorex was developed by Nordmark in the 1960s.
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RDS-127 is a drug which is used in scientific research. It acts as a D2-like receptor agonist and also has some serotonin and adrenergic agonist effects, as well as some anticholinergic action, and produces both anorectic and pro- sexual effects in animal studies.
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2-Phenyl-3,5-dimethylmorpholine is a drug with stimulant and anorectic effects, related to phenmetrazine. Based on what is known from other phenylmorpholines with similar structure, it likely acts as a norepinephrine- dopamine releasing agent and may produce effects similar or slightly different to phenmetrazine.
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The meat she used in Vanitas: Flesh Dress for an Albino Anorectic (1987) has emotional and symbolic value implying death in relation to the piece being worn as a dress by a woman. The network of relations among the materials defines what she calls ‘states of being’ between freedom and restraint. Her work has Surrealist affinities that acknowledge experiences of uncanny and unconscious desires that go beyond reason. She doubles the self in her art through objects that are worn on the body (like Vanitas: Flesh Dress for an Albino Anorectic (1987)) or suggest a presence, and they convey a sense of otherness through a psychic state of being.
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SNAP-94847 is a drug used in scientific research, which is a selective, non- peptide antagonist at the melanin concentrating hormone receptor MCH1. In animal studies it has been shown to produce both anxiolytic and antidepressant effects, and also reduces food consumption suggesting a possible anorectic effect.
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FG-7142 (ZK-31906) is a drug which acts as a partial inverse agonist at the benzodiazepine allosteric site of the GABAA receptor. It has anorectic, anxiogenic and pro-convulsant effects. It also increases release of acetylcholine and noradrenaline, and improves memory retention in animal studies.
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Levopropylhexedrine (Eventin) is a psychostimulant used as an anorectic in Germany and patented by Smith Kline & French in 1947.US 2454746 Cyclohexylalkylamines It has also been used in the anticonvulsant preparation barbexaclone in combination with phenobarbital to offset sedation. Levopropylhexedrine is the S-enantiomer of propylhexedrine.
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4-methylaminorex can be smoked, insufflated or taken orally. As an anorectic, the ED50 is 8.8 mg/kg in rats for the (±)-cis isomers. The (±)-trans isomers are slightly more potent at 7.0 mg/kg. As a recreational drug, the effective dosage ranges from 5 to 25 mg.
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Phenmetrazine was first patented in Germany in 1952 by Boehringer-Ingelheim, with some pharmacological data published in 1954. It was the result of a search by Thomä and Wick for an anorectic drug without the side-effects of amphetamine. Phenmetrazine was introduced into clinical use in 1954 in Europe.
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Its structure incorporates the backbone of amphetamine, the prototypical CNS stimulant which, like phenmetrazine, is a releasing agent of dopamine and norepinephrine. The molecule also loosely resembles ethcathinone, the active metabolite of popular anorectic amfepramone (diethylpropion). Unlike phenmetrazine, ethcathinone (and therefore amfepramone as well) are mostly selective as noradrenaline releasing agents.
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The Anorectic Behavior Observation Scale (ABOS) is a thirty-item diagnostic questionnaire devised to be answered by the parents, spouse or other family member of an individual suspected of having an eating disorder. It was developed by Vandereyken et al. in 1992. The questions address three factors: unusual eating behavior, bulimic-type behavior and hyperactivity.
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An anorectic or anorexic is a drug which reduces appetite, resulting in lower food consumption, leading to weight loss. By contrast, an appetite stimulant is referred to as orexigenic. The term is (from the Greek ἀν- (an-) = "without" and ὄρεξις (órexis) = "appetite"), and such drugs are also known as anorexigenic, anorexiant, or appetite suppressant.
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ORG-37684 is a drug developed by Organon, which acts as a potent and selective agonist for the 5-HT2 receptor family, with highest affinity at 5-HT2C and lowest at 5-HT2B subtypes. It has anorectic effects in animal studies and has been researched as a potential weight loss drug for use in humans.
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SKF-77,434 is a drug which acts as a selective dopamine D1 receptor partial agonist, and has stimulant and anorectic effects. Unlike other D1 agonists with higher efficacy such as SKF-81,297 and 6-Br-APB, SKF-77,434 does not maintain self-administration in animal studies, and so has been researched as a potential treatment for cocaine addiction.
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Cyclazodone has not been evaluated by the United States Food and Drug Administration for use in humans as a nootropic, anorectic, or stimulant and thus safety information on Cyclazodone is lacking. However, in studies relating to the therapeutic uses of Cyclazodone, it was noted that Cyclazodone exhibited less cardiotoxic and hepatotoxic effects than D-Amphetamine in studies on mice.
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Indorenate (TR-3369), is a tryptamine derivative which acts as an agonist at the 5-HT1A, 5-HT1B and 5-HT2C serotonin receptors. It has anxiolytic, antihypertensive and anorectic effects, predominantly through action at 5-HT1A, but with some contribution from the 5-HT1B and 5-HT2C subtypes, and possibly some other non-serotonergic targets also.
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Rimonabant (also known as SR141716; trade names Acomplia, Zimulti) is an anorectic antiobesity drug that was first approved in Europe in 2006 but was withdrawn worldwide in 2008 due to serious psychiatric side effects; it was never approved in the United States. Rimonabant is an inverse agonist for the cannabinoid receptor CB1 and was the first drug approved in that class.
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These were specified to be the two rare conditions of narcolepsy and hyperactivity with the third permitted indication being for appetite suppression among obese patients. However, usage of amphetamines as anorectic agents will only be indicated for short-term obesity treatment not to exceed a few weeks.Pep Pill Makers Accused By F.D.A., The New York Times, August 6, 1970, Page 1.
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Taranabant (codenamed MK-0364) is a cannabinoid receptor type 1 inverse agonist that was investigated as a potential treatment for obesity due to its anorectic effects. It was discovered by Merck & Co. In October 2008, Merck has stopped its phase III clinical trials with the drugs due to high level of central nervous system side effects, mainly depression and anxiety.
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Rimonabant (also known as SR141716; trade names Acomplia and Zimulti) was an anorectic antiobesity medication that was first approved in Europe in 2006 but was withdrawn worldwide in 2008 due to serious psychiatric side effects; it was never approved in the United States. Rimonabant is an inverse agonist for the cannabinoid receptor CB1 and was the first medication approved in that class.
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Tiflorex, formerly known as flutiorex, is a stimulant amphetamine. Its most pronounced effect is in suppression of appetite; it has little effect on pulse rate, sleep, or mood. It was found to be twice as potent an anorectic as fenfluramine. SL 72.340-d was cited to be 4x the anorectant potency of fenfluramine (ED50=1.4 mg/kg vs 5.6 mg/kg).
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YM-348 is an indazole derivative drug which acts as a potent and selective 5-HT2C receptor agonist, with an EC50 of 1nM and 15x selectivity over 5-HT2A, although it only has moderate selectivity of 3x over the closely related 5-HT2B receptor. It has thermogenic and anorectic effects in animal studies, making it potentially useful for the treatment of obesity.
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A-372159 is a drug which acts as a potent and selective partial agonist for the 5HT2C receptor, with more than 100x selectivity over the closely related 5-HT2B receptor and a Ki of 3nM. It has been found to produce anorectic effects in animal studies and produced significant weight loss in rats with no development of tolerance or serious side effects.
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It was discovered in 1962 by Edward John Hurlburt, and was quickly found in 1963 to have an anorectic effect in rats. It was introduced as a prescription appetite suppressant in Germany, Switzerland and Austria in 1965, but was withdrawn in 1972 after it was found to cause pulmonary hypertension in approximately 0.2% of patients, and was linked to a number of deaths.
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A-68930 is a synthetic compound that acts as a selective dopamine receptor D1 agonist. It is orally active and has antidepressant and anorectic effects in animals, producing wakefulness and tachycardia, but without stimulant effects, instead producing sedation. The difference in effects between A-68930 and other D1 agonists such as SKF-82958 may be due to their differing effects on the related D5 receptor.
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Cyclazodone is a centrally acting stimulant drug developed by American Cyanamid Company in the 1960s. The drug is related to other drugs such as pemoline and thozalinone. It displayed a favorable therapeutic index and margin of safety in comparison to Pemoline and other N-lower-alkyl-substituted Pemoline derivatives. The patents concluded that Cyclazodone possessed properties efficacious in reducing fatigue and as a potential anorectic.
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Phendimetrazine functions as a prodrug to phenmetrazine; approximately 30 percent of an oral dose is converted into it. Phendimetrazine can essentially be thought of as an extended-release formulation of phenmetrazine with less potential for abuse. Phendimetrazine is an anorectic drug which acts as a norepinephrine-dopamine releasing agent (NDRA). As an amphetamine congener, its structure incorporates the backbone of methamphetamine, a potent CNS stimulant.
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A-423,579 is one of a range of histamine antagonists developed by Abbott Laboratories which are selective for the H3 subtype, and have stimulant and anorectic effects in animal studies making them potentially useful treatments for obesity. A-423,579 has improved characteristics over earlier drugs in the series with both high efficacy and low toxicity in studies on mice, and is currently in clinical development.
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Several selective ligands for the melanocortin receptors are known, and some synthetic compounds have been investigated as potential tanning, anti-obesity and aphrodisiac drugs, with tanning effects mainly from stimulation of MC1, while anorectic and aphrodisiac effects appear to involve both MC3 and MC4. MC1, MC3 and MC4 are widely expressed in the brain, and are also thought to be responsible for effects on mood and cognition.
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Secretin and its receptor are found in discrete nuclei of the hypothalamus, including the paraventricular nucleus and the arcuate nucleus, which are the primary brain sites for regulating body energy homeostasis. It was found that both central and peripheral injection of Sct reduce food intake in mouse, indicating an anorectic role of the peptide. This function of the peptide is mediated by the central melanocortin system.
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Lu AA-33810 is a drug developed by Lundbeck, which acts as a potent and highly selective antagonist for the Neuropeptide Y receptor Y5, with a Ki of 1.5nM and around 3300x selectivity over the related Y1, Y2 and Y4 receptors. In animal studies it produced anorectic, antidepressant and anxiolytic effects, and further research is now being conducted into its possible medical application in the treatment of eating disorders.
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The sites of action in the brain include the medial habenula, interpeduncular nucleus, dorsolateral tegmentum and basolateral amygdala. It has also been shown to produce anorectic effects in obese rats, most likely due to the same actions on the reward system which underlie its anti-addictive effects against drug addiction. 18-MC is in the early stages of human testing by the California-based drug development company Savant HWP.
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Thozalinone (USAN) (brand name Stimsen; former developmental code name CL-39808) is a psychostimulant that has been used as an antidepressant in Europe. It has also been trialed as an anorectic. Thozalinone is described as a "dopaminergic stimulant", and likely acts via inducing the release of dopamine and to a minimal extent norepinephrine; similar to analogue pemoline, it is seemingly devoid of abuse potential unlike common psychostimulants that increase catecholamines.
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By inhibiting the rewarding effects of cocaine, CART has a potential use in treating cocaine addiction. CART peptides are inhibitors of food intake (anorectic) and closely associated with leptin and neuropeptide Y, two important food intake regulators. CART hypoactivity in the hypothalamus of depressed animals is associated with hyperphagia and weight gain. CART is thought to play a key role in the opioid mesolimbic dopamine circuit that modulates natural reward processes.
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Aminorex (Menocil, Apiquel, aminoxaphen, aminoxafen, McN-742) is a weight loss (anorectic) stimulant drug. It was withdrawn from the market after it was found to cause pulmonary hypertension. In the U.S., it is an illegal Schedule I drug, meaning it has high abuse potential, no accepted medical use, and a poor safety profile. Aminorex, in the 2-amino-5-aryl oxazoline class, was developed by McNeil Laboratories in 1962.
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Benfluorex, sold under the brand name Mediator, is an anorectic and hypolipidemic agent that is structurally related to fenfluramine (a substituted amphetamine). It may improve glycemic control and decrease insulin resistance in people with poorly controlled type-2 diabetes. It was on the market between 1976 and 2009, and is thought to have caused between 500 and 2,000 deaths. It was patented and manufactured by the French pharmaceutical company Servier.
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NGD-4715 is a drug developed by Neurogen, which acts as a selective, non- peptide antagonist at the melanin concentrating hormone receptor MCH1. In animal models it has anxiolytic, antidepressant, and anorectic effects, and it has successfully passed Phase I clinical trials in humans. Neurogen was acquired by Ligand Pharmaceuticals in August, 2009, and NGD-4715 was not listed among its key assets. All four laboratories were closed and sold, and no employees were retained.
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Velneperit (S-2367) is a drug developed by Shionogi, which acts as a potent and selective antagonist for the Neuropeptide Y receptor Y5. It has anorectic effects and was developed as a possible treatment for obesity, but was discontinued from further development after disappointing results in Phase II clinical trials. However it was still considered a successful proof of concept of the potential of Y5 receptor antagonists as possible anti-obesity agents in future.
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Obocell was indicated for the treatment of obesity, with the therapeutic anorectic effect being achieved by consuming the medication 30 to 60 minutes prior to each meal. The manufacturer recommended dosage was 1 or 2 tablets to be taken with a full glass of water three times daily. Nicel, the company's brand name formulation of high-viscosity methylcellulose, was an additional third active ingredient present within the Obocell-TF formulation as 160mg Nicel per tablet.
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PNU-22394 is a drug which acts as an agonist at serotonin 5-HT2 receptors, with strongest binding affinity for 5-HT2A and 5-HT2C and slightly weaker at 5-HT2B, although it is only a full agonist at 5-HT2C, but partial agonist at 5-HT2A and 5-HT2B. It has anorectic effects in both animal studies and human trials, along with "Pro-Cognitive Properties", although it has never been developed for medical use.
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A range of selective ligands for the GHS-R receptor are now available and are being developed for several clinical applications. GHS-R agonists have appetite-stimulating and growth hormone-releasing effects, and are likely to be useful for the treatment of muscle wasting and frailty associated with old-age and degenerative diseases. On the other hand, GHS-R antagonists have anorectic effects and are likely to be useful for the treatment of obesity.
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Dilated pupils (mydriasis) are prominent during khat consumption, reflecting the sympathomimetic effects of the drug, which are also reflected in increased heart rate and blood pressure. Long-term use can precipitate permanent tooth darkening (of a greenish tinge), susceptibility to ulcers, and diminished sex drive. Khat is an effective anorectic, causing loss of appetite. It is unclear if the consumption of khat directly affects the mental health of the user or not.
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Amfecloral (INN), also known as amphecloral (USAN), is a stimulant drug of the phenethylamine and amphetamine chemical classes that was used as an appetite suppressant under the trade name Acutran, but is now no longer marketed. It was classified as an anorectic drug with little to no stimulant activity in a 1970 review. The British Pharmacopoeia Commission approved the name in 1970. The raw ingredients used in manufacturing it were d-amphetamine and chloral hydrate.
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However, salmon RIA appears to allow interspecies assessment of plasma lep levels. This only confirms that more comprehensive studies are needed for conclusive data interpretation. Studies on rainbow trout also implicated Lep as an anorectic hormone as in mammals. Injection of rainbow trout with recombinant trout leptin (rt-leptin) resulted in a significantly reduced appetite over two days that coincided with a decrease in hypothalamic mRNA expression of neuropeptide Y (npy) and increase of pomc mRNAs, respectively.
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Formetorex (INN), also known as formetamide or N-formylamphetamine, is a substituted amphetamine described as an anorectic which does not appear to have ever been marketed. Formetorex is also an intermediate in the production of amphetamine by the "Leuckart reaction." It is also commonly found as an impurity in clandestine labs where this synthesis method is used. Due to the simplicity of the Leuckart reaction, it is the most popular synthetic route employed for the illicit manufacture of amphetamines.
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The package insert contains the following boxed warning, as do all thyroid hormones: > Drugs with thyroid hormone activity, alone or together with other > therapeutic agents, have been used for the treatment of obesity. In > euthyroid patients, doses within the range of daily hormonal requirements > are ineffective for weight reduction. Larger doses may produce serious or > even life-threatening manifestations of toxicity, particularly when given in > association with sympathomimetic amines such as those used for their > anorectic effects.
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In Print. Giacomo, D., & Weissmark, M. (1985). An "Overweight" anorectic family. Journal of Systemic Therapies, 4 (1), 61-68.In Print. Giacomo, D., & Weissmark, M. (1986). Systemic practice. Family process, 25 (4), 483-512.In Print. Giacomo, D., & Weissmark, M. (1987). Toward a generative theory of the therapeutic field. Family process, 26 (4), 437-459.In Print. Weissmark, M., & Giacomo, D. (1995). Measuring therapeutic interactions: clinical and research applications. Psychiatry: Interpersonal and Biological Processes, 58, 173-188.
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Clortermine (Voranil) was developed by Ciba in the 1960s and is an anorectic drug of the amphetamine class. It is the 2-chloro analogue of the better known appetite suppressant phentermine, and is the 2-chloro positional isomer of chlorphentermine. Clortermine produces very low rates of self-administration in animals similarly to chlorphentermine, and as a result it likely does not act on dopamine. Instead, it may act as a serotonin and/or norepinephrine releasing agent.
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6-Br-APB is a synthetic compound that acts as a selective D1 agonist, with the (R)-enantiomer being a potent full agonist, while the (S) enantiomer retains its D1 selectivity but is a weak partial agonist. (R)-6-Br-APB and similar D1-selective full agonists like SKF-81,297 and SKF-82,958 produce characteristic anorectic effects, stereotyped behaviour and self- administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine.
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Vabicaserin (codenamed SCA-136) was a novel antipsychotic and anorectic under development by Wyeth. As of 2010 it is no longer in clinical trials for the treatment of psychosis. It was also under investigation as an antidepressant but this indication appears to have been dropped as well. Vabicaserin acts as a selective 5-HT2C receptor full agonist (Ki = 3 nM; EC50 = 8 nM; IA = 100% (relative to 5-HT)) and 5-HT2B receptor antagonist (IC50 = 29 nM).
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It lacks any reinforcing or hallucinogenic effects, produces dysphoric, depressive, and anxiogenic effects in rodents and humans, and can induce panic attacks in individuals susceptible to them. It also worsens obsessive–compulsive symptoms in people with the disorder. mCPP is known to induce headaches in humans and has been used for testing potential antimigraine medications. It has potent anorectic effects and has encouraged the development of selective 5-HT2C receptor agonists for the treatment of obesity as well.
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Further studies suggest that consumption of comfort food is triggered in men by positive emotions, and by negative ones in women. The stress effect is particularly pronounced among college-aged women, with only 33% reporting healthy eating choices during times of emotional stress. For women specifically, these psychological patterns may be maladaptive. A therapeutic use of these findings includes offering comfort foods or "happy hour" beverages to anorectic geriatric patients whose health and quality of life otherwise decreases with reduced oral intake.
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SNAP-7941 is a drug used in scientific research, which is a selective, non- peptide antagonist at the melanin concentrating hormone receptor MCH1. In initial animal studies it had promising anxiolytic, antidepressant and anorectic effects, but subsequent trial results were disappointing, and the main significance of SNAP-7941 is as the lead compound from which more potent and selective antagonists such as SNAP-94847 were developed, although it continues to be used for research into the function of the MCH1 receptor.
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Thus, reduction in PYY sensitivity may not be one of the causes of obesity, in contrast to the reduction of leptin sensitivity. The anorectic effect of PYY could possibly be a future obesity drug. The consumption of protein boosts PYY levels, so some benefit was observed in experimental subjects in reducing hunger and promoting weight loss. This could partially explain the weight-loss experienced with high-protein diets, but the high thermic effect of protein appears to be the leading cause.
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Cocaethylene is largely considered a recreational drug in and of itself, with stimulant, euphoriant, anorectic, sympathomimetic, and local anesthetic properties. The monoamine neurotransmitters serotonin, norepinephrine, and dopamine play important roles in cocaethylene's action in the brain. Cocaethylene increases the levels of serotonergic, noradrenergic, and dopaminergic neurotransmission in the brain by inhibiting the action of the serotonin transporter, norepinephrine transporter, and dopamine transporter. These pharmacological properties make cocaethylene a serotonin- norepinephrine-dopamine reuptake inhibitor (SNDRI; also known as a "triple reuptake inhibitor").
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Ciclazindol (WY-23409) is an antidepressant and anorectic drug of the tetracyclic chemical class that was developed in the mid to late 1970s, but was never marketed. It acts as a norepinephrine reuptake inhibitor, and to a lesser extent as a dopamine reuptake inhibitor. Ciclazindol has no effects on the SERT, 5-HT receptors, mACh receptors, or α-adrenergic receptors, and has only weak affinity for the H1 receptor. As suggested by its local anesthetic properties, ciclazindol may also inhibit sodium channels.
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Levofenfluramine (INN), or (−)-3-trifluoromethyl-N-ethylamphetamine, also known as (−)-fenfluramine or (R)-fenfluramine, is a drug of the amphetamine family that, itself (i.e., in enantiopure form), was never marketed. It is the levorotatory enantiomer of fenfluramine, the racemic form of the compound, whereas the dextrorotatory enantiomer is dexfenfluramine. Both fenfluramine and dexfenfluramine are anorectic agents that have been used clinically in the treatment of obesity (and hence, levofenfluramine has been as well since it is a component of fenfluramine).
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In the late 1960s, non-selective serotonin receptor antagonists demonstrated a relationship between serotonin receptors and food intake. Later, animal studies showed that serotonin receptor agonists might act as a mediator of satiety. Serotonin has been implicated as a critical factor in the short-term regulation of food intake and in promoting loss of weight associated with hyperphagia. Studies using pharmacological and genetic tools demonstrated that the 5-HT2C receptor subtype was one of the principal mediators through which serotonin exerts its anorectic effects in rodents.
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SKF-82,958 is a synthetic compound of the benzazepine class that acts as a D1/D5 receptor full agonist. SKF-82,958 and similar D1-like-selective full agonists like SKF-81,297 and 6-Br-APB produce characteristic anorectic effects, hyperactivity and self-administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine. SKF-82,958 was also subsequently found to act as an agonist of ERα with negligible activity at ERβ, making it a subtype-selective estrogen.
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This is a list of aminorex analogues. Aminorex itself is a stimulant drug with a 5-phenyl-2-amino-oxazoline structure. It was developed in the 1960s as an anorectic,Meschino JA, Poos GI. 2-amino-5,6-dihydro-4H-1,3-oxazines and a process for their preparation. US Patent 3115494, 1961Poos GI. 2-amino-5-aryloxazoline products. US Patent 3161650, 1962 but withdrawn from sale after it was discovered that extended use produced pulmonary hypertension, often followed by heart failure, which resulted in a number of deaths.
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SB-334867 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX1, with around 50x selectivity for OX1 over OX2 receptors. It has been shown to produce sedative and anorectic effects in animals, and has been useful in characterising the orexinergic regulation of brain systems involved with appetite and sleep, as well as other physiological processes. The hydrochloride salt of SB-334867 has been demonstrated to be hydrolytically unstable, both in solution and as the solid.
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TDIQ (also known as 6,7-methylenedioxy-1,2,3,4-tetrahydroisoquinoline or MDTHIQ) is a drug used in scientific research, which has anxiolytic and anorectic effects in animals. It has an unusual effects profile in animals, with the effects generalising to cocaine and partially to MDMA and ephedrine, but the effects did not generalise to amphetamine and TDIQ does not have any stimulant effects. It is thought these effects are mediated via a partial agonist action at Alpha-2 adrenergic receptors, and TDIQ has been suggested as a possible drug for the treatment of cocaine dependence.
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Phenylpropanolamine (PPA; Accutrim; β-hydroxyamphetamine), also known as the stereoisomers norephedrine and norpseudoephedrine, is a psychoactive drug of the phenethylamine and amphetamine chemical classes that is used as a stimulant, decongestant, and anorectic agent. It is commonly used in prescription and over-the-counter cough and cold preparations. In veterinary medicine, it is used to control urinary incontinence in dogs under trade names Propalin and Proin. In the United States, PPA is no longer sold without a prescription due to a proposed increased risk of stroke in younger women.
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Sibutramine (Reductil or Meridia) is an anorectic or appetite suppressant, reducing the desire to eat. Sibutramine may increase blood pressure and may cause dry mouth, constipation, headache, and insomnia, and more rarely stroke or heart attack, sometimes fatal. In the past, it was noted by the US that Meridia was a harmless medication for fighting obesity. The US District Court of the Northern District of Ohio rejected 113 cases complaining about the negative effects of the medication, stating that the clients lacked supporting facts and that the representatives involved were not qualified enough.
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4-Methylamphetamine (4-MA; PAL-313; Aptrol; p-TAP) is a stimulant and anorectic drug of the phenethylamine and amphetamine chemical classes. In vitro, it acts as a potent and balanced serotonin, norepinephrine, and dopamine releasing agent with Ki affinity values of 53.4nM, 22.2nM, and 44.1nM at the serotonin, norepinephrine, and dopamine transporters, respectively. However, more recent in vivo studies that involved performing microdialysis on rats showed a different trend. These studies showed that 4-methylamphetamine is much more potent at elevating serotonin (~18 x baseline) relative to dopamine (~5 x baseline).
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CART is an anorectic peptide and is widely expressed in both the central and peripheral nervous systems, particularly concentrated in the hypothalamus. CART is also expressed outside of the nervous system in pituitary endocrine cells, adrenomedullary cells, islet somatostatin cells, and in rat antral gastrin cells. Other structures and pathways associated with CART expression include the mesolimbic pathway (linking the ventral tegmental area to the nucleus accumbens) and amygdala. CART is also found in a subset of retinal ganglion cells (RGCs), the primary afferent neurons in the retina.
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Fenfluramine, a related drug, had been withdrawn from the market in 1997 after reports of heart valve disease, pulmonary hypertension, and development of cardiac fibrosis. This side effect is mediated by the metabolite norfenfluramine on 5HT2B receptors of heart valves, leading to a characteristic pattern of heart failure following proliferation of cardiac fibroblasts on the tricuspid valve. Both fenfluramine and benfluorex form norfenfluramine as a metabolite. This side effect led to the withdrawal of fenfluramine as an anorectic drug worldwide, and later to the withdrawal of benfluorex in Europe.
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Surinabant (SR147778) is a cannabinoid receptor type 1 antagonist developed by Sanofi-Aventis. It is being investigated as a potential treatment for nicotine addiction, to assist smoking cessation. It may also be developed as an anorectic drug to assist with weight loss, however there are already several CB1 antagonists or inverse agonists on the market or under development for this application, so surinabant is at present mainly being developed as an anti-smoking drug, with possible application in the treatment of other addictive disorders such as alcoholism. Other potential applications such as treatment of ADHD have also been proposed.
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Evidence from physiological, pharmacological and neuroimaging studies suggest serotonin (also called 5-HT) may play a role in anorexia. While acutely ill, metabolic changes may produce a number of biological findings in people with anorexia that are not necessarily causative of the anorexic behavior. For example, abnormal hormonal responses to challenges with serotonergic agents have been observed during acute illness, but not recovery. Nevertheless, increased cerebrospinal fluid concentrations of 5-hydroxyindoleacetic acid (a metabolite of serotonin), and changes in anorectic behavior in response to acute tryptophan depletion (tryptophan is a metabolic precursor to serotonin) support a role in anorexia.
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Leptin also reduces appetite in response to feeding, but obese people develop a resistance to leptin. Obese people secrete less PYY than non-obese people, and attempts to use PYY directly as a weight-loss drug have met with some success. Researchers noted the caloric intake during a buffet lunch offered two hours after the infusion of PYY was decreased by 30% in obese subjects (P<0.001) and 31% in lean subjects (P<0.001). While some studies have shown obese persons have lower circulating level of PYY postprandially, other studies have reported they have normal sensitivity to the anorectic effect of PYY3-36.
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A-77636 is a synthetic drug which acts as a selective D1 receptor full agonist. It has nootropic, anorectic, rewarding and antiparkinsonian effects in animal studies, but its high potency and long duration of action causes D1 receptor downregulation and tachyphylaxis, and unlike other D1 full agonists such as SKF-82,958, it does not produce place preference in animals. A-77636 partially substituted for cocaine in animal studies, and has been suggested for use as a possible substitute drug in treating addiction, but it is better known for its use in studying the role of D1 receptors in the brain.
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Norfenfluramine, or 3-trifluoromethylamphetamine, is a never-marketed drug of the amphetamine family that behaves as a serotonin and norepinephrine releasing agent and potent 5-HT2A, 5-HT2B, and 5-HT2C agonist. The action of norfenfluramine on 5-HT2B receptors on heart valves leads to a characteristic pattern of heart failure following proliferation of cardiac fibroblasts on the tricuspid valve, known as cardiac fibrosis. This side effect led to the withdrawal of fenfluramine as an anorectic agent worldwide, and to the withdrawal of benfluorex in Europe, as both fenfluramine and benfluorex form norfenfluramine as an active metabolite. It is a human TAAR1 agonist.
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The hypothalamus responds to the hormone leptin, which signals the feeling of fullness after eating, and nonylphenol has been shown to both increase and decrease eating behavior by interfering with leptin signaling in the midbrain. Nonylphenol has been shown mimic the action of leptin on neuropeptide Y and anorectic POMC neurons, which has an anti-obesity effect by decreasing eating behavior. This was seen when estrogen or estrogen mimics were injected into the ventromedial hypothalamus. On the other hand, nonylphenol has been shown to increase food intake and have obesity enhancing properties by lowering the expression of these anorexigenic neurons in the brain.
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8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT1A receptor. It was one of the first major 5-HT1A receptor full agonists to be discovered. Originally believed to be selective for the 5-HT1A receptor, 8-OH-DPAT was later found to act as a 5-HT7 receptor agonist and serotonin reuptake inhibitor/releasing agent as well. In animal studies, 8-OH-DPAT has been shown to possess antidepressant, anxiolytic, serenic, anorectic, antiemetic, hypothermic, hypotensive, bradycardic, hyperventilative, and analgesic effects.
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The chemical structure of MDMA or "ecstasy" Amphetamines have an effect on norepinephrine levels similar to that of cocaine in that they both increase NE levels in the brain. Amphetamine-like drugs are substrates for monoamine transporters, include NET, that cause a reversal in the direction of neurotransmitter transport. Amphetamines cause a large accumulation of extracellular NE. High levels of NE in the brain account for most of the profound effects of amphetamines, including alertness and anorectic, locomotor and sympathomimetic effects. However, the effects that amphetamines have on the brain are slower but last longer than the effects cocaine has on the brain.
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BIBP-3226 is a drug used in scientific research which acts as a potent and selective antagonist for both the Neuropeptide Y receptor Y1 and also the neuropeptide FF receptor. It was the first non-peptide antagonist developed for the Y1 receptor and has been widely used to help determine its functions in the body. Activation of Y1 is thought to be involved in functions such as regulation of appetite and anxiety, and BIBP-3226 has anxiogenic and anorectic effects, as well as blocking the Y1-mediated corticotropin releasing hormone release. It has also been used as a lead compound to develop a number of newer more potent Y1 antagonists.
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Epidemics of fatal pulmonary hypertension and heart valve damage associated with pharmaceutical anorectic agents have led to the withdrawal of products from the market. This was the case with aminorex in the 1960s, and again in the 1990s with fenfluramine (see: Fen-phen). Likewise, association of the related appetite suppressant phenylpropanolamine with hemorrhagic stroke led the Food and Drug Administration (FDA) to request its withdrawal from the market in the United States in 2000, and similar concerns regarding ephedrine resulted in an FDA ban on its inclusion in dietary supplements in 2004. A Federal judge later overturned this ban in 2005 during a challenge by supplement maker Nutraceuticals.
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Ibipinabant (SLV319, BMS-646,256) is a drug used in scientific research which acts as a potent and highly selective CB1 antagonist. It has potent anorectic effects in animals, and was researched for the treatment of obesity, although CB1 antagonists as a class have now fallen out of favour as potential anorectics following the problems seen with rimonabant, and so ibipinabant is now only used for laboratory research, especially structure-activity relationship studies into novel CB1 antagonists. SLV330, which is a structural analogue of Ibipinabant, was reported active in animal models related to the regulation of memory, cognition, as well as in addictive behavior. An atom- efficient synthesis of ibipinabant has been reported.
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Methylenedioxypyrovalerone has no record of FDA approved medical use. It has been shown to produce robust reinforcing effects and compulsive self- administration in rats, though this had already been provisionally established by a number of documented cases of misuse and addiction in humans before the animal tests were carried out. MDPV is the 3,4-methylenedioxy ring-substituted analog of the compound pyrovalerone, developed in the 1960s, which has been used for the treatment of chronic fatigue and as an anorectic, but caused problems of abuse and dependence. Other drugs with a similar chemical structure include α-pyrrolidinopropiophenone (α-PPP), 4'-methyl-α- pyrrolidinopropiophenone (M-α-PPP), 3',4'-methylenedioxy-α- pyrrolidinopropiophenone (MDPPP) and 1-phenyl-2-(1-pyrrolidinyl)-1-pentanone (α-PVP).
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Its fresh leaves and tops are chewed or, less frequently, dried and consumed as tea, to achieve a state of euphoria and stimulation; it also has anorectic (appetite-reducing) side effects. The leaves or the soft part of the stem can be chewed with either chewing gum or fried peanuts to make it easier to chew. In recent years, however, improved roads, off-road motor vehicles, and air transportation have increased the global distribution of this perishable commodity, and as a result, the plant has been reported in England, Wales, Rome, Amsterdam, Canada, Israel, Australia, New Zealand, and the United States. In the US, freshly packed khat leaves are sold on the markets of New York, Los Angeles, Boston, and Dallas, where the demand is highest.
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Medifoxamine (Cledial, Gerdaxyl) is an antidepressant that appears to act as an SDRI as well as a 5-HT2 receptor antagonist. Sibutramine (Reductil, Meridia, Siredia, Sibutrex) is a withdrawn anorectic that itself as a molecule in vitro is an SNDRI but preferentially an SDRI, with 18.3- and 5.8-fold preference for inhibiting the reuptake of serotonin and dopamine over norepinephrine, respectively. However, the metabolites of sibutramine are substantially more potent and possess different ratios of monoamine reuptake inhibition in comparison, and sibutramine appears to be acting in vivo mainly as a prodrug to them; accordingly, it was found to act as an SNRI (73% and 54% for norepinephrine and serotonin reuptake inhibition, respectively) in human volunteers with only very weak inhibition of dopamine reuptake (16%).
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The young Elisabeth shortly after becoming Austrian Empress (by , 1855) After enjoying an informal and unstructured childhood, Elisabeth, who was shy and introverted by nature, and more so among the stifling formality of Habsburg court life, had difficulty adapting to the Hofburg and its rigid protocols and strict etiquette. Within a few weeks, Elisabeth started to display health problems: she had fits of coughing and became anxious and frightened whenever she had to descend a narrow steep staircase.Vandereycken, Walter & Van Deth, Ron, "The Anorectic Empress: Elisabeth of Austria", History Today, Vol. 46, April 1996 She was surprised to find she was pregnant and gave birth to her first child, a daughter, Archduchess Sophie of Austria (1855–1857), just ten months after her wedding.
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Pyrovalerone (Centroton, 4-Methyl-β-keto-prolintane, Thymergix, O-2371)US Patent 3314970 is a psychoactive drug with stimulant effects via acting as a norepinephrine-dopamine reuptake inhibitor (NDRI), and is used for the clinical treatment of chronic fatigue or lethargy and as an anorectic or appetite suppressant for weight loss purposes. It was developed in the late 1960s and has since been used in France and several other European countries, and although pyrovalerone is still occasionally prescribed, it is used infrequently due to problems with abuse and dependence. It is closely related on a structural level to a number of other stimulants, such as MDPV and prolintane (Promotil, Katovit). Side effects of pyrovalerone include anorexia or loss of appetite, anxiety, fragmented sleep or insomnia, and trembling, shaking, or muscle tremors.
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European regulators required a major warning of pulmonary hypertension risks. In 1996, a 30-year-old woman developed heart problems after a month of using fenfluramine/phentermine; when she died in February 1997, the Boston Herald devoted a front-page article to her. Later that year, in August 1997, a paper in the New England Journal of Medicine (NEJM) from the Mayo Clinic discussed clinical findings in 24 people who had taken fen-phen. The authors noted that their findings suggested a possible correlation between mitral valve dysfunction and the use of these anorectic agents. The FDA alerted medical doctors that it had received nine additional reports of the same type, and requested all health care professionals to report any such cases to the agency’s MedWatch program, or to their respective pharmaceutical manufacturers.
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A potential explanation as to why levofenfluramine is not similarly an effective anorectic is that it has also been found to behave as a dopamine receptor antagonist, which, as dopamine antagonists like atypical antipsychotics are associated with causing increased appetite and weight gain—effects that their actions on dopamine receptors have been implicated in playing a role in the development of, is an action that could in theory cancel out the hypothetical serotonergically-mediated appetite suppressant effects of the compound. However, this is speculation and has not been proven. Levonorfenfluramine, an active metabolite of levofenfluramine, is also a fairly potent serotonin releasing agent (with a potency of approximately 1/2 that of norfenfluramine and 1/6th that of dexfenfluramine) and, similarly to dexnorfenfluramine, is a 5-HT2B and 5-HT2C receptor agonist, as well as a somewhat less potent norepinephrine reuptake inhibitor (about 1/2 that of its efficacy as a serotonin releaser). As such, likely contributes significantly to the biological activity—though not necessarily appetite suppressant effects—of not only levofenfluramine but of racemic fenfluramine as well.
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