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Ethcathinone
Ethcathinone, also known as ethylpropion or ETH-CAT, is a stimulant drug of the phenethylamine, amphetamine, and cathinone chemical classes. It is an active metabolite of the prodrug diethylcathinone and is fully responsible for its effects. Ethcathinone has been identified as an ingredient in both quasi-legal " party pills", and, along with mephedrone, has also been reported as having been sold as "ecstasy" in the Australian city of Cairns. Pharmacology The pharmacology for ethcathinone appeared alongside other psychostimulants in a paper by Rothman and Baumann in 2006. The predominant two modes of action for ethcathinone is as a moderately active releaser of noradrenaline (EC50 = 99.3nM); however it is only a relatively weak inhibitor of dopamine reuptake (Ki = 1,014nM). Since diethylcathinone appears to be an inactive prodrug and only becomes active after it has been further metabolized to ethcathinone, it thereby would appear rational to consider that ethcathinone wou ...
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Mephedrone
Mephedrone, also known as , , and , is a synthetic stimulant drug of the amphetamine and cathinone classes. Slang names include drone, , White Magic, meow meow, bubble, ''txomin'' and yurrpt. It is chemically similar to the cathinone compounds found in the khat plant of eastern Africa. It comes in the form of tablets or crystals, which users can swallow, snort or inject, producing effects similar to those of MDMA, amphetamines and cocaine. In addition to its stimulant effects, mephedrone produces side effects, of which bruxism is the most common. The metabolism of mephedrone has been studied in rats and humans and the metabolites can be detected in urine after usage. Mephedrone was first synthesised in 1929, but did not become widely known until it was rediscovered in 1999–2000 at which point it was legal to produce and possess in many countries. By 2000, mephedrone was reported to be available for sale on the internet, by 2008 law enforcement agencies had become aware of the ...
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Substituted Cathinone
Substituted cathinones, which include some stimulants and entactogens, are derivatives of cathinone. They feature a phenethylamine core with an alkyl group attached to the alpha carbon, and a ketone group attached to the beta carbon, along with additional substitutions. Cathinone occurs naturally in the plant khat whose leaves are chewed as a recreational drug. List of substituted cathinones The derivatives may be produced by substitutions at four locations of the cathinone molecule: * R1 = hydrogen, or any combination of one or more alkyl, alkoxy, alkylenedioxy, haloalkyl or halide substituents * R2 = hydrogen or any alkyl group * R3 = hydrogen, any alkyl group, or incorporation in a cyclic structure * R4 = hydrogen, any alkyl group, or incorporation in a cyclic structure The following table displays notable derivatives that have been reported: Legality On 2 April 2010, the Advisory Council on the Misuse of Drugs in the UK announced that a broad structure-based ...
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Cathinones
Substituted cathinones, which include some stimulants and entactogens, are derivatives of cathinone. They feature a phenethylamine core with an alkyl group attached to the alpha carbon, and a ketone group attached to the beta carbon, along with additional substitutions. Cathinone occurs naturally in the plant khat whose leaves are chewed as a recreational drug. List of substituted cathinones The derivatives may be produced by substitutions at four locations of the cathinone molecule: * R1 = hydrogen, or any combination of one or more alkyl, alkoxy, alkylenedioxy, haloalkyl or halide substituents * R2 = hydrogen or any alkyl group * R3 = hydrogen, any alkyl group, or incorporation in a cyclic structure * R4 = hydrogen, any alkyl group, or incorporation in a cyclic structure The following table displays notable derivatives that have been reported: Legality On 2 April 2010, the Advisory Council on the Misuse of Drugs in the UK announced that a broad structure-based b ...
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Substituted Cathinone
Substituted cathinones, which include some stimulants and entactogens, are derivatives of cathinone. They feature a phenethylamine core with an alkyl group attached to the alpha carbon, and a ketone group attached to the beta carbon, along with additional substitutions. Cathinone occurs naturally in the plant khat whose leaves are chewed as a recreational drug. List of substituted cathinones The derivatives may be produced by substitutions at four locations of the cathinone molecule: * R1 = hydrogen, or any combination of one or more alkyl, alkoxy, alkylenedioxy, haloalkyl or halide substituents * R2 = hydrogen or any alkyl group * R3 = hydrogen, any alkyl group, or incorporation in a cyclic structure * R4 = hydrogen, any alkyl group, or incorporation in a cyclic structure The following table displays notable derivatives that have been reported: Legality On 2 April 2010, the Advisory Council on the Misuse of Drugs in the UK announced that a broad structure-based ...
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Monoamine 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 ...
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Substituted Amphetamine
Substituted amphetamines are a class of compounds based upon the amphetamine structure; it includes all derivative compounds which are formed by replacing, or substituting, one or more hydrogen atoms in the amphetamine core structure with substituents. The compounds in this class span a variety of pharmacological subclasses, including stimulants, empathogens, and hallucinogens, among others. Examples of substituted amphetamines are amphetamine (itself), methamphetamine, ephedrine, cathinone, phentermine, mephentermine, bupropion, methoxyphenamine, selegiline, amfepramone (diethylpropion), pyrovalerone, MDMA (ecstasy), and DOM (STP). Some of amphetamine's substituted derivatives occur in nature, for example in the leaves of '' Ephedra'' and khat plants. Amphetamine was first produced at the end of the 19th century. By the 1930s, amphetamine and some of its derivative compounds found use as decongestants in the symptomatic treatment of colds and also occasionally ...
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Flephedrone
Flephedrone, also known as 4-fluoromethcathinone (4-FMC), is a stimulant drug of the cathinone chemical class that has been sold online as a designer drug starting in 2008. Toxicity Flephedrone has only a short history of human use and its toxicity is not well established. Legality Flephedrone has been illegal in Denmark since December 2008. Flephedrone has been illegal in the UK since April 2010. Flephedrone has been illegal in the Lithuania since April 2010. Flephedrone is illegal in Brazil since 2017 as an analogue or derivative of cathinone. Flephedrone is most likely illegal in Australia as an analogue or derivative of cathinone. Flephedrone has been illegal in Poland since April 2010. Flephedrone has been classed as a narcotic in Sweden since October 2010. In the United States, flephedrone is temporarily listed as a Schedule I controlled substance. It is permanently listed as a Schedule I controlled substance in Florida, Georgia, and Pennsylvania. As of October ...
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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 compounds of phenethylamine which can be formed by replacing, or substituting, one or more hydrogen atoms in the phenethylamine core structure with substituents. The structural formula of any substituted phenethylamine contains a phenyl ring that is joined to an amino (NH) group via a two-carbon sidechain. Hence, any substituted phenethylamine can be classified according to the substitution of hydrogen (H) atoms on phenethylamine's phenyl ring, sidechain, or amino group with a specific group of atoms. Many substituted phenethylamines are psychoactive drugs which belong to a variety of different drug classes, including central nervous system stimulants (e.g., amphetamine), hallucinogens (e.g., dl-2,5-dimethoxy-4-methylamphetamine DOM), entactogens (e.g., 3,4-methylenedioxyamphet ...
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Cathinone
Cathinone (also known as benzoylethanamine, or β-keto-amphetamine) 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'', also known as khat. 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 ...
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Diethylcathinone
Amfepramone, also known as diethylpropion, is a stimulant drug of the phenethylamine, amphetamine, and cathinone classes that is used as an appetite suppressant. It is used in the short-term management of obesity, along with dietary and lifestyle changes. Amfepramone is most closely chemically related to the antidepressant and smoking cessation aid bupropion (previously called amfebutamone), which has also been developed as a weight-loss medicine when in a combination product with naltrexone. Pharmacology Amfepramone itself lacks any affinity for the monoamine transporters and instead functions as a prodrug to ethcathinone. Ethcathinone (and therefore amfepramone as well) is a very weak dopaminergic and serotonergic, and is approximately 10x and 20x stronger on norepinephrine in comparison, respectively. As a result, ethcathinone and amfepramone can essentially be considered a member of the class of drugs known as norepinephrine releasing agents (NRAs). Chemistry Amfepramon ...
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Dopamine Reuptake Inhibitor
A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron. This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission. DRIs are used in the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy for their psychostimulant effects, and in the treatment of obesity and binge eating disorder for their appetite suppressant effects. They are sometimes used as antidepressants in the treatment of mood disorders, but their use as antidepressants is limited given that strong DRIs have a high abuse potential and legal restrictions on their use. Lack of dopamine reuptake and the increase in extracellular levels of dopamine have ...
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Designer Drugs
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects, and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human trials, the use of some of these drugs may result i ...
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