3-Fluorophenmetrazine
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3-Fluorophenmetrazine
3-Fluorophenmetrazine (also known as 3-FPM, 3-FPH and PAL-593) is a phenylmorpholine-based stimulant and fluorinated analogue of phenmetrazine that has been sold online as a designer drug. Chemistry 3-Fluorophenmetrazine is a fluorinated analogue of phenmetrazine, a stimulant of the morpholine class. 3-Fluorophenmetrazine is a regioisomer of both 2-fluorophenmetrazine and 4-fluorophenmetrazine. Pharmacology 3-FPM acts as a norepinephrine–dopamine releasing agent with EC50 values of 30 nM and 43 nM, respectively. It shows only negligible efficacy as a releaser of serotonin, with an EC50 value of 2558 nM. 3-FPM also inhibits uptake mediated by dopamine transporters and norepinephrine transporters in HEK293 cells with potencies comparable to cocaine (IC50 values 80 μM). At sufficient doses, 3-FPM is capable of reversing monoamine transporters, particularly transporters of the catecholamines dopamine and norepinephrine, and, to a much lesser degree, serotonin transporters, ...
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Substituted Phenylmorpholine
Substituted phenylmorpholines, or substituted phenmetrazines alternatively, are chemical derivatives of phenylmorpholine or of the psychostimulant drug phenmetrazine. Most such compounds act as releasers of monoamine neurotransmitters, and have stimulant effects. Some also act as agonists at serotonin receptors, and compounds with an N-propyl substitution act as dopamine receptor agonists. A number of derivatives from this class have been investigated for medical applications, such as for use as anorectics or medications for the treatment of ADHD. Some compounds have also become subject to illicit use as designer drugs. See also * Substituted amphetamine * Substituted benzofuran * Substituted cathinone * Substituted methylenedioxyphenethylamine * List of aminorex analogues * List of methylphenidate analogues * List of phenyltropanes * List of cocaine analogues This is a list of cocaine analogues. A cocaine analogue is an (usually) artificial construct of a novel chemi ...
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Phenmetrazine
Phenmetrazine (INN, USAN, BAN) (brand name Preludin, and many others) is a stimulant drug first synthesized in 1952 and originally used as an appetite suppressant, but withdrawn from the market in the 1980s due to widespread abuse. It was initially replaced by its analogue phendimetrazine (under the brand name Prelu-2) which functions as a prodrug to phenmetrazine, but now it is rarely prescribed, due to concerns of abuse and addiction. Chemically, phenmetrazine is a substituted amphetamine containing a morpholine ring. History 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. Medical use In clinical use, phenmetrazine produces less nervousness, hyperexcitability, euphoria and insomnia than drugs of the amphetamine family ...
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Phenylmorpholines
Substituted phenylmorpholines, or substituted phenmetrazines alternatively, are chemical derivatives of phenylmorpholine or of the psychostimulant drug phenmetrazine. Most such compounds act as releasers of monoamine neurotransmitters, and have stimulant effects. Some also act as agonists at serotonin receptors, and compounds with an N-propyl substitution act as dopamine receptor agonists. A number of derivatives from this class have been investigated for medical applications, such as for use as anorectics or medications for the treatment of ADHD. Some compounds have also become subject to illicit use as designer drugs. See also * Substituted amphetamine * Substituted benzofuran * Substituted cathinone * Substituted methylenedioxyphenethylamine * List of aminorex analogues * List of methylphenidate analogues * List of phenyltropanes * List of cocaine analogues This is a list of cocaine analogues. A cocaine analogue is an (usually) artificial construct of a novel ...
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Phendimetrazine
Phendimetrazine (Bontril, Adipost, Anorex-SR, Appecon, Melfiat, Obezine, Phendiet, Plegine, Prelu-2, Statobex) is a stimulant drug of the morpholine chemical class used as an appetite suppressant. Pharmacology 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. While the addition of an N-methyl group to amphetamine significantly increases its potency and bioavailability, methylation of phenmetrazine renders the compound virtually inactive. However, phendimetrazine is a prodrug for phenmetrazine which acts as the active metabolite. Phendimetrazine possesses preferable phar ...
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Phenmetrazine
Phenmetrazine (INN, USAN, BAN) (brand name Preludin, and many others) is a stimulant drug first synthesized in 1952 and originally used as an appetite suppressant, but withdrawn from the market in the 1980s due to widespread abuse. It was initially replaced by its analogue phendimetrazine (under the brand name Prelu-2) which functions as a prodrug to phenmetrazine, but now it is rarely prescribed, due to concerns of abuse and addiction. Chemically, phenmetrazine is a substituted amphetamine containing a morpholine ring. History 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. Medical use In clinical use, phenmetrazine produces less nervousness, hyperexcitability, euphoria and insomnia than drugs of the amphetamine family ...
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Manifaxine
Manifaxine (developmental code name GW-320,659) is a norepinephrine–dopamine reuptake inhibitor developed by GlaxoSmithKline through structural modification of radafaxine, an isomer of hydroxybupropion and one of the active metabolites of bupropion. Manifaxine was researched for treatment of attention deficit hyperactivity disorder (ADHD) and obesity and was found to be safe, reasonably effective, and well-tolerated for both applications. However, no results were reported following these initial trials and development was discontinued. Synthesis The Grignard reaction between 3,5-difluorobenzonitrile 4248-63-1(1) and ethylmangensium bromide gives 3,5-difluoropropiophenone 35306-45-5(2). Halogenation with molecular bromine occurs at the alpha-keto position providing 2-bromo-3',5'-difluoropropiophenone 35306-46-6(3). Intermolecular ring formation with DL-Alaninol (2-Aminopropanol) 168-72-5completed the synthesis of Manifaxine (4). See also * 3,5-Difluoromethcathinone * 3-Fl ...
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3F-PVP
3-Fluoro-alpha-PVP (3F-PVP) is a recreational designer drug from the substituted cathinone family with stimulant effects, which first appeared on the illicit market in around 2018. It is illegal in Finland. See also * 3-Fluoroamphetamine * 3-Fluoromethamphetamine * 3-Fluoroethamphetamine * 3-Fluoromethcathinone * 3-Fluorophenmetrazine * 3F-NEH * 3F-PiHP * 4F-PVP * 4Cl-PVP 4-Chloro-''alpha''-pyrrolidinovalerophenone (also known as 4-chloro-''alpha''-pyrrolidinopentiophenone, 4-chloro-α-PVP, 4Cl-PVP, or 4C-PVP) is an emerging recreational designer drug of the pyrrolidinophenone class, similar in structure to ''al ... * 4F-PHP References Pyrrolidinophenones Designer drugs Serotonin-norepinephrine-dopamine releasing agents {{nervous-system-drug-stub ...
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G-130
G-130 (GP-130, 2-Phenyl-5,5-dimethyltetrahydro-1,4-oxazine) is a drug with stimulant and anorectic effects, related to phenmetrazine. Structural analogs Compounds related to G-130 and radafaxine were synthesized that behave as combined inhibitors of monoamine uptake and nicotinic acetylcholine receptors. Synthesis Ex 1: 2 moles of 2-methyl-2-aminopropanol (aminomethyl propanol) (1) is reacted with 1 moles of styrene oxide (phenyloxirane) 6-09-3(2) in 0.2 mole water. Ex 2: Fepradinol 6981-91-6 3075-47-8(3) is treated with acid, to cyclize to the morpholine ring. See also * 2-Phenyl-3,6-dimethylmorpholine * 3-Fluorophenmetrazine * 4-Methylphenmetrazine * Phendimetrazine * Manifaxine Manifaxine (developmental code name GW-320,659) is a norepinephrine–dopamine reuptake inhibitor developed by GlaxoSmithKline through structural modification of radafaxine, an isomer of hydroxybupropion and one of the active metabolites of bup ... References Stimulants Phenylmor ...
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2-Phenyl-3,6-dimethylmorpholine
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. Anecdotal reports suggest, however, that the compound is inactive aside from anorectic effects. See also * 3-Fluorophenmetrazine * G-130 (2-Phenyl-5,5-dimethylmorpholine) * 3,4-Phendimetrazine (2-Phenyl-3,4-dimethylmorpholine) * PDM-35 (3,5-Phendimetrazine) (2-Phenyl-3,5-dimethylmorpholine) * Manifaxine Manifaxine (developmental code name GW-320,659) is a norepinephrine–dopamine reuptake inhibitor developed by GlaxoSmithKline through structural modification of radafaxine, an isomer of hydroxybupropion and one of the active metabolites of bup ... * Radafaxine References Stimulants Substituted amphetamines Phenylmorpholines Designer drugs Phenyl compounds {{nervous-system-drug-stub ...
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4-Methylphenmetrazine
4-Methylphenmetrazine (mephenmetrazine, 4-MPM, PAL-747) is a recreational designer drug with stimulant effects. It is a substituted phenylmorpholine derivative, closely related to better known drugs such as phenmetrazine and 3-fluorophenmetrazine. It was first identified in Slovenia in 2015, and has been shown to act as a monoamine releaser with some preference for serotonin release. See also * 4,4'-DMAR * 4-Methylamphetamine * 4-Methylmethylphenidate * G-130 * Mephedrone * RTI-32 * Phendimetrazine * PDM-35 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 an ... References Substituted amphetamines Phenylmorpholines Designer drugs {{pharm-stub ...
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Stimulants
Stimulants (also often referred to as psychostimulants or colloquially as uppers) is an overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and invigorating, or drugs that have Sympathomimetic drug, sympathomimetic effects. Stimulants are widely used throughout the world as prescription medicines as well as without a prescription (either legally or Prohibition (drugs), illicitly) as performance-enhancing substance, performance-enhancing or recreational drug use, recreational drugs. Among narcotics, stimulants produce a noticeable crash or ''Comedown (drugs), comedown'' at the end of their effects. The most frequently prescribed stimulants as of 2013 were lisdexamfetamine (Vyvanse), methylphenidate (Ritalin), and amphetamine (Adderall). It was estimated in 2015 that the percentage of the world population that had used cocaine during a year was 0.4%. For the category "amphetamines and p ...
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