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Cathinones
Substituted cathinones, or simply cathinones, which include some stimulants and Empathogen-entactogen, entactogens, are chemical derivative, derivatives of cathinone. They feature a substituted phenethylamine, phenethylamine core with an alkyl functional group, group attached to the alpha and beta carbon, alpha carbon, and a ketone group attached to the alpha and beta carbon, beta carbon, along with additional Substitution reaction, substitutions. Cathinone occurs naturally in the plant khat whose leaves are chewed as a recreational drug. Substituted cathinones act as monoamine releasing agents and/or monoamine reuptake inhibitors, including of norepinephrine, dopamine, and/or serotonin. In contrast to substituted amphetamines, most substituted cathinones do not act as agonists of the human trace amine-associated receptor 1 (TAAR1). This may potentiate their stimulating and drug addiction, addictive effects. In addition, β-keto-substituted phenethylamines, such as βk-2C-B, app ...
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Monoamine Releasing Agent
A monoamine releasing agent (MRA), or simply monoamine releaser, is a drug that induces the release of one or more monoamine neurotransmitters from the presynaptic neuron into the synapse, leading to an increase in the extracellular concentrations of the neurotransmitters and hence enhanced signaling by those neurotransmitters. The monoamine neurotransmitters include serotonin, norepinephrine, and dopamine; MRAs can induce the release of one or more of these neurotransmitters. MRAs work by reversing the direction of the monoamine transporters (MATs), including the serotonin transporter (SERT), norepinephrine transporter (NET), and/or dopamine transporter (DAT), causing them to promote efflux of non-vesicular cytoplasmic monoamine neurotransmitter rather than reuptake of synaptic monoamine neurotransmitter. Many, but not all MRAs, also reverse the direction of the vesicular monoamine transporter 2 (VMAT2), thereby additionally resulting in efflux of vesicular monoamine neuro ...
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Cathinone
Cathinone (; also known as β-ketoamphetamine) is a monoamine alkaloid found in the shrub ''Catha edulis'' (khat) and is chemically similar to ephedrine, cathine, methcathinone and other amphetamines. It is probably the main contributor to the stimulant effect of ''Catha edulis''. Cathinone differs from many other amphetamines in that it has a ketone functional group. Other phenethylamines that share this structure include the stimulants methcathinone, MDPV, mephedrone and the antidepressant bupropion. History Discovery Khat has been cultivated in the Horn of Africa and Arabian Peninsula region of the world for thousands of years. It is most commonly chewed for the euphoric effect it produces. The active ingredient was first proposed in 1930, when cathine was identified as a predominant alkaloid in the plant. Cathine was thought to be the main active ingredient in khat until the 1960s, when it was found that the amount of cathine in the khat leaves is insufficient to prod ...
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Trace Amine-associated Receptor 1
Trace amine-associated receptor 1 (TAAR1) is a trace amine-associated receptor (TAAR) protein that in humans is encoded by the ''TAAR1'' gene. TAAR1 is a primarily intracellular amine-activated and G protein-coupled receptor (GPCR) that is primarily expressed in several peripheral organs and cells (e.g., the stomach, small intestine, duodenum, and white blood cells), astrocytes, and in the intracellular milieu within the presynaptic plasma membrane (i.e., axon terminal) of monoamine neurons in the central nervous system (CNS). TAAR1 is one of six functional human TAARs, which are so named for their ability to bind endogenous amines that occur in tissues at trace concentrations. TAAR1 plays a significant role in regulating neurotransmission in dopamine, norepinephrine, and serotonin neurons in the CNS; it also affects immune system and neuroimmune system function through different mechanisms. Endogenous ligands of the TAAR1 include trace amines, monoamine neurotransmitter ...
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2-Methylmethcathinone
2-Methylmethcathinone (2-MMC, ortomephedrone) is a recreational designer drug with stimulant and euphoric effects. It is a substituted cathinone derivative, closely related to better known drugs such as 3-methylmethcathinone and 4-methylmethcathinone (mephedrone). It was first identified in Sweden in 2014, and has subsequently been reported in other European countries such as Poland and Spain. Chemistry 2-Methylmethcathinone's chemical name is 2-(methylamino)-1-phenylpropan-1-one. It is one of many substituted cathinones, synthetic chemicals derived from the natural chemical cathinone, found in khat. 2-MMC is a positional isomer of 3-MMC and 4-MMC. Pharmacology 2-MMC is a serotonin-norepinephrine-dopamine releasing agent, with higher preference for the norepinephrine and dopamine transporters. 2-MMC is expected to have similar characteristics to other cathinones, although studies show 2-substituted cathinones are weaker compared to 3 and 4-substituted ones. This is potentiall ...
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Substituted Phenethylamine
Substituted phenethylamines (or simply phenethylamines) are a chemical class of organic compounds that are based upon the phenethylamine structure; the class is composed of all the derivative (chemistry), derivative compounds of phenethylamine which can be formed by replacing, or substitution reaction, substituting, one or more hydrogen atoms in the phenethylamine core structure with substituents. Phenylethylamines are also generally found to be central nervous system stimulants with many also being entactogens/empathogens, and hallucinogens. Structural classification The structural formula of any substituted phenethylamine contains a phenyl group, phenyl ring that is joined to an amino group, amino (NH) group via a two-carbon substituent, sidechain. Hence, any substituted phenethylamine can be classified according to the substitution of hydrogen atom, hydrogen (H) atoms on phenethylamine's phenyl ring, sidechain, or amino group with a moiety (chemistry), specific group of at ...
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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, Mood disorder, mood, and physical activity, physical performance. Some stimulants occur naturally, while others are exclusively synthetic. Common stimulants include caffeine, nicotine, amphetamines, cocaine, methylphenidate, and modafinil. Stimulants may be subject to varying forms of regulation, or outright prohibition, depending on jurisdiction. Stimulants increase activity in the sympathetic nervous system, either directly or indirectly. Prototypical stimulants increase synaptic concentrations of neurotransmitter, excitatory neurotransmitters, particularly norepinephrine and dopamine (e.g., methylphenidate). Other stimulants work by binding to the Receptor (biochemistry), receptors of excitatory neurotransmitters (e.g., nicotine) or by ...
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βk-2C-B
βk-2C-B, or β-keto-2C-B, also known as 4-bromo-2,5-dimethoxy-β-ketophenylethylamine, is a novel psychedelic substance. It is the beta (β) ketone structural analogue of 2C-B, a psychedelic drug of the 2C family. It is used as a recreational drug, usually taken orally. βk-2C-B is a controlled substance in Canada, Germany, Switzerland, and the United Kingdom. History βk-2C-B is a designer drug, more specifically it is the beta keto analogue of the controlled substance 2C-B (2,5-dimethoxy-4-bromophenethylamine) which was first synthesized by Alexander Shulgin. It is unknown who first synthesized βk-2C-B, but it first appeared on the market mid-2013 as a recreational drug. Although a synthesis of the compound had previously been described, in the years after its emergence on the market, papers reporting analytical characterizations of the substance appeared. It is offered online and is termed a psychedelic drug. Since 12 October 2016, βk-2C-B has become a controlled substa ...
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Drug Addiction
Addiction is a neuropsychological disorder characterized by a persistent and intense urge to use a drug or engage in a behavior that produces natural reward, despite substantial harm and other negative consequences. Repetitive drug use can alter brain function in synapses similar to natural rewards like food or falling in love in ways that perpetuate craving and weakens self-control for people with pre-existing vulnerabilities. This phenomenon – drugs reshaping brain function – has led to an understanding of addiction as a brain disorder with a complex variety of psychosocial as well as neurobiological factors that are implicated in the development of addiction. While mice given cocaine showed the compulsive and involuntary nature of addiction, for humans this is more complex, related to behavior or personality traits. Classic signs of addiction include compulsive engagement in rewarding stimuli, ''preoccupation'' with substances or behavior, and continued use de ...
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2-Fluoromethcathinone
2-Fluoromethcathinone (2-FMC), also known as 2-flephedrone, is a psychostimulant and designer drug of the cathinone family. It acts as a dopamine and norepinephrine releasing agent (NDRA). Pharmacology The drug has an for dopamine release of 48.7nM and induces 85% release of norepinephrine at a concentration of 10μM. For comparison, the values of methcathinone are 49.9nM for dopamine release and 22.4nM for norepinephrine release and it induces 100% release of norepinephrine at a concentration of 10μM. Hence, compared to methcathinone, 2-FMC appears to be relatively more selective or efficacious for induction of dopamine release over norepinephrine release. It is notable in this regard that selective dopamine releasing agents are largely unknown. See also * 3-Methoxymethcathinone * 3-Fluoromethcathinone * 4-Fluoromethcathinone (flephedrone) * 2-Fluoromethamphetamine 2-Fluoromethamphetamine (2-FMA) is a stimulant drug of the amphetamine family which has been used as ...
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