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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 preferabl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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and many others) is a stimulant drug first synthesized in 1952 and originally used as an appetite suppressant, but withdrawn from the market in the 1980s due to widespread abuse.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 fami ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fenbutrazate
Fenbutrazate (INN), also known as phenbutrazate (BAN), is a psychostimulant used as an appetite suppressant under the trade names Cafilon, Filon, and Sabacid in Europe, Japan, and Hong Kong. It is a derivative of phenmetrazine and may function as a prodrug due to its similarity to phendimetrazine. See also * Morazone * Phendimetrazine * 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 initia ... References {{Phenethylamines Anorectics Antiobesity drugs Carboxylate esters Substituted amphetamines Phenylmorpholines Norepinephrine-dopamine releasing agents Stimulants ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Convention On Psychotropic Substances
The Convention on Psychotropic Substances of 1971 is a United Nations treaty designed to control psychoactive drugs such as amphetamine-type stimulants, barbiturates, benzodiazepines, and psychedelics signed in Vienna, Austria on 21 February 1971. The Single Convention on Narcotic Drugs of 1961 did not ban the many newly discovered psychotropics, since its scope was limited to drugs with cannabis, coca and opium-like effects. During the 1960s such drugs became widely available, and government authorities opposed this for numerous reasons, arguing that along with negative health effects, drug use led to lowered moral standards. The Convention, which contains import and export restrictions and other rules aimed at limiting drug use to scientific and medical purposes, came into force on 16 August 1976. As of 2013, 183 member states are Parties to the treaty. Many laws have been passed to implement the Convention, including the Canadian Controlled Drugs and Substances Act, th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Releasing Agent
A monoamine releasing agent (MRA), or simply monoamine releaser, is a drug that induces the release of a monoamine neurotransmitter from the presynaptic neuron into the synapse, leading to an increase in the extracellular concentrations of the neurotransmitter. Many drugs induce their effects in the body and/or brain via the release of monoamine neurotransmitters, e.g., trace amines, many substituted amphetamines, and related compounds. Types of MRAs MRAS can be classified by the monoamines they mainly release, although these drugs lie on a spectrum. * Selective for one neurotransmitter ** Serotonin releasing agent (SRA) ** Norepinephrine releasing agent (NRA) ** Dopamine releasing agent (DRA) * Non-selective, releasing two or more neurotransmitters ** Norepinephrine–dopamine releasing agent (NDRA) ** Serotonin–norepinephrine releasing agent (SNRA) ** Serotonin–dopamine releasing agent (SDRA) ** Serotonin–norepinephrine–dopamine releasing agent (SNDRA) Mechani ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stimulant
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 effects. Stimulants are widely used throughout the world as prescription medicines as well as without a prescription (either legally or illicitly) as performance-enhancing or recreational drugs. Among narcotics, stimulants produce a noticeable crash or '' 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 prescription stimulants" (with "amphetamines" including amphetamine and methamphetamine) the value was 0.7% ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methylation
In the chemical sciences, methylation denotes the addition of a methyl group on a substrate, or the substitution of an atom (or group) by a methyl group. Methylation is a form of alkylation, with a methyl group replacing a hydrogen atom. These terms are commonly used in chemistry, biochemistry, soil science, and the biological sciences. In biological systems, methylation is catalyzed by enzymes; such methylation can be involved in modification of heavy metals, regulation of gene expression, regulation of protein function, and RNA processing. In vitro methylation of tissue samples is also one method for reducing certain histological staining artifacts. The reverse of methylation is demethylation. In biology In biological systems, methylation is accomplished by enzymes. Methylation can modify heavy metals, regulate gene expression, RNA processing and protein function. It has been recognized as a key process underlying epigenetics. Methanogenesis Methanogenesis, the proce ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 __NOTOC__ Year 353 ( CCCLIII) was a common year starting on Friday (link will display the full calendar) of the Julian calendar. At the time, it was known as th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Morazone
Morazone (Novartrina, Orsimon, Rosimon-Neu, Tarcuzate) is a nonsteroidal anti-inflammatory drug (NSAID), originally developed by the German pharmaceutical company Ravensberg in the 1950s, which is used as an analgesic. It produces phenmetrazine as a major metabolite and has been reported to have been abused as a recreational drug in the past. See also * Famprofazone * Morforex Morforex (INN; Bo 637), also referable to as ''N''-morpholinoethylamphetamine, is an anorectic which was never marketed. It produces amphetamine as an active metabolite. Synthesis Amphetamine is reacted with N-Chloroethylmorpholine 240-94-6in ... References {{Phenethylamines Substituted amphetamines Phenylmorpholines Nonsteroidal anti-inflammatory drugs Pyrazolones Stimulants Norepinephrine-dopamine releasing agents ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 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 p ... * Manifaxine References Stimulants Phenyl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 b ... * Radafaxine References Stimulants Substituted amphetamines Phenylmorpholines Designer drugs Phenyl compounds {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
