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Aminorexes
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 It was developed in the 1960s as an anorectic, but withdrawn from sale after it was discovered that extended use produced pulmonary hypertension, often followed by heart failure, which resulted in a number of deaths.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 Pemoline was sold for around 25 years as a therapy for ADHD and relief of fatigue, before being withdrawn from the market in 2005 because of rare but serious cases of liver failure.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] |
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 It was withdrawn from the market after it was found to cause pulmonary hypertension (PPH).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] |
Clominorex
Clominorex is a centrally acting sympathomimetic which is related to other drugs such as aminorex and pemoline. It was developed as an appetite suppressant by McNeil Laboratories in the 1950s. See also * 4C-MAR * 4-Methylaminorex * Aminorex * Cyclazodone * Fenozolone * 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 4-Chlorophenyl compounds Norepinephrine-dopamine releasing agents {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluminorex
Fluminorex is a centrally acting sympathomimetic which is related to other drugs such as aminorex and pemoline. It was developed as an appetite suppressant by McNeil Laboratories in the 1950s. Synthesis 2-amino-1- -(trifluoromethyl)phenylthanol 76-02-3(1) cyanogen bromide 06-68-3(2) See also * 4'-Fluoro-4-methylaminorex * 4-Methylaminorex * Aminorex * Clominorex * Cyclazodone * Fenozolone * 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 Trifluoromethyl compounds Norepinephrine-dopamine releasing agents {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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] |
4,4'-dimethylaminorex
4,4'-Dimethylaminorex (abbreviated as 4,4'-DMAR), sometimes referred to by the street name "Serotoni", is a psychostimulant and entactogen designer drug related to aminorex, 4-methylaminorex, and pemoline. It was first detected in the Netherlands in December 2012, and has been sold as a designer drug around Europe since mid-2013. 4,4'-DMAR had been linked to at least 31 deaths in Hungary, Poland, and the UK by February 2014, mostly when consumed in combination with other drugs. Nineteen deaths linked to 4,4'-DMAR were reported in Northern Ireland in the same time period. Pharmacology Pharmacodynamics 4,4'-DMAR is a monoamine releasing agent (MRA) and acts specifically as a highly potent and well-balanced serotonin-norepinephrine-dopamine releasing agent (SNDRA), with EC50 values for serotonin, norepinephrine, and dopamine release of 18.5nM, 26.9nM, and 8.6nM, respectively. It also interacts with the vesicular monoamine transporter 2 (VMAT2) with similar potency as MDMA. In ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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] |
Pemoline
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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] |
4-methylaminorex
4-Methylaminorex (4-MAR, 4-MAX) is a stimulant drug of the 2-amino-5-aryloxazoline group that was first synthesized in 1960 by McNeil Laboratories. It is also known by its street name "U4Euh" ("Euphoria"). It is banned in many countries as a stimulant. 4-Methylaminorex has effects comparable to methamphetamine but with a longer duration. Chemistry 4-Methylaminorex exists as four stereoisomers : (±)-''cis'' and (±)-''trans''. The (±)-''cis'' isomers are the form used recreationally. Synthesis The (±)-''cis'' isomers acemate (1:1-mixture) of the (4''R'',5''S'')-isomer and the enantiomeric (4''S'',5''R'')-isomergenerally synthesized from dl-phenylpropanolamine in one step by cyclization with cyanogen bromide (sometimes prepared ''in situ'' by reacting sodium cyanide with bromine). Alternate synthesis routes generally involve more steps, such as replacing cyanogen bromide with sodium or potassium cyanate to form an intermediate and then reacting it with concentrated hydroch ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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] |
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] |
