Substituted Aminorex
This is a list of aminorex analogues, also known as substituted 2-amino-5-aryloxazolines. Aminorex itself is a stimulant drug with a 5-phenyl-2-amino-oxazoline structure. It was developed in the 1960s as an anorectic, but withdrawn from sale after it was discovered that extended use produced pulmonary hypertension, often followed by heart failure, which resulted in a number of deaths. A designer drug analogue 4-methylaminorex appeared on the illicit market in the late 1980s but did not attract significant popularity due to its steep dose-response curve and tendency to produce seizures. Pemoline, the 4-keto derivative of aminorex, had been discovered several years earlier, and derivatives of this type appeared to be effective stimulants with comparatively low toxicity. Pemoline was sold for around 25 years as a therapy for ADHD and relief of fatigue, before being withdrawn from the market in 2005 because of rare but serious cases of liver failure. More recently in around 2014 another ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Aminorex
Aminorex, sold under the brand names Menocil and Apiquel among others, is a weight loss (anorectic) stimulant drug. It was withdrawn from the market after it was found to cause pulmonary hypertension (PPH). In the United States, aminorex is a Schedule I controlled substance. Aminorex, in the 2-amino-5-aryloxazoline group, was developed by McNeil Laboratories in 1962. It is closely related to 4-methylaminorex (4-MAR). Aminorex has been shown to have locomotor-stimulant effects, lying midway between dextroamphetamine and methamphetamine. Aminorex effects have been attributed to the release of catecholamines. It can be produced as a metabolite of the deworming medication levamisole, which is sometimes used as a cutting agent of illicitly produced cocaine. Pharmacology Pharmacodynamics Aminorex is a serotonin–norepinephrine–dopamine releasing agent (SNDRA). Its values for induction of monoamine release are 26.4nM for norepinephrine, 49.4nM for dopamine, and 193nM fo ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Cyclazodone
Cyclazodone is a centrally acting stimulant Stimulants (also known as central nervous system stimulants, or psychostimulants, or colloquially as uppers) are a class of drugs that increase alertness. They are used for various purposes, such as enhancing attention, motivation, cognition, ... 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. Structural congeners of pemoline have been described as "excitants with unique properties distinguishing them from the sympathomimetic amines" whilst displaying less stimulatory activity and toxicity compared to amphetamine. It is included under the World Anti-Doping Agency prohibited list. Sa ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Cyclazodone Structure
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. Structural congeners of pemoline have been described as "excitants with unique properties distinguishing them from the sympathomimetic amines" whilst displaying less stimulatory activity and toxicity compared to amphetamine. It is included under the World Anti-Doping Agency prohibited list. Safety 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 is lacking. However, in studies relating to the therapeutic uses of cyclazodone, ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Fenozolone
Fenozolone (Ordinator) was developed by Laboratoires Dausse in the 1960s and is a psychostimulant related to pemoline. See also * 4-Methylaminorex * Aminorex * Clominorex * Cyclazodone * Fluminorex * Pemoline * Thozalinone Thozalinone (United States Adopted Name, 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 clinical trial, trialed as an anorectic. Thozal ... References Stimulants Aminorexes Norepinephrine-dopamine releasing agents Oxazolones Phenyl compounds {{psychoactive-stub ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Thozalinone
Thozalinone (United States Adopted Name, 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 clinical trial, trialed as an anorectic. Thozalinone is described as a "dopaminergic stimulant", and likely acts via inducing the releasing agent, release of dopamine and to a minimal extent norepinephrine; similar to chemical analogue, analogue pemoline, it is reportedly devoid of abuse potential unlike other dopaminergic psychostimulants. Synthesis Sodium hydride is used as a strong base to abstract the alcohol proton in ethyl mandelate [774-40-3] (1); addition of the oxyanion to dimethylcyanamide [1467-79-4] gives the intermediate (2). Intramolecular cyclization then occurs giving Thozalinone (3). Notes *In treatment of Parkinsonism: W. D. Gray, C. E. Edward, (1972 to Am. Cyanamid). *Pharmacological studies: See also * Fenozolone References {{Monoamine releasing a ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Pemoline Structure 2
Pemoline, formerly sold under the brand name Cylert among others, is a stimulant medication which was used in the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy,- it has since been discontinued in most countries due to rare but serious liver toxicity. The medication was taken by mouth. Common side effects include insomnia, decreased appetite, abdominal pain, irritability, and headaches, while rare cases of serious liver damage requiring liver transplantation or causing death have been reported. As a stimulant, Pemoline acts as a selective dopamine reuptake inhibitor and releasing agent via indirect agonism of dopamine receptors. In addition, it shows little activity with respect to norepinephrine, thus minimal to no cardiovascular or sympathomimetic effects in comparison to many other stimulants. Pemoline was first synthesized in 1913, but its stimulant activity was not discovered until the 1930s, nor used for ADHD until 1975. Between 1997 and 2005 ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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2C-B-aminorex
2C-B-aminorex (2C-B-AR) is a recreational designer drug with psychedelic effects. It is a substituted aminorex derivative which was first identified in Sweden in June 2019. Structurally, it is a hybrid of 4-bromo-2,5-dimethoxyphenethylamine (2C-B) and aminorex. See also * 2C-B * 2C-B-morpholine * 2C-B-PP * BOB (psychedelic) * 4,4'-DMAR * 4'-Fluoro-4-methylaminorex * 4B-MAR * 4C-MAR * List of aminorex analogues This is a list of aminorex analogues, also known as substituted 2-amino-5-aryloxazolines. Aminorex itself is a stimulant drug with a 5-phenyl-2-amino-oxazoline structure. It was developed in the 1960s as an anorectic, but withdrawn from sale after ... References 2,5-Dimethoxyphenethylamines Aminorexes Bromoarenes Designer drugs Psychedelic phenethylamines {{hallucinogen-stub ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |