Indapyrophenidone
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Indapyrophenidone
Indapyrophenidone is a synthetic drug of the cathinone class that has been sold online as a designer drug. The substance is the indanyl-α-phenyl analogue of the stimulant drug α-PVP, however it is also structurally related to diarylethylamines such as fluorolintane and UWA-001. Its mechanism of action is unknown. See also * βk-Ephenidine * Diphenidine * Ephenidine * Lefetamine * Methoxphenidine * Pyrovalerone * TH-PVP TH-PVP is a substituted cathinone derivative which has been sold as a designer drug. It was first identified by a forensic laboratory in Hungary in 2015, but has subsequently been found in numerous other countries around the world including Spai ... References Designer drugs Diarylethylamines Drugs with unknown mechanisms of action Pyrrolidinophenones Stimulants {{nervous-system-drug-stub ...
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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 ba ...
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TH-PVP
TH-PVP is a substituted cathinone derivative which has been sold as a designer drug. It was first identified by a forensic laboratory in Hungary in 2015, but has subsequently been found in numerous other countries around the world including Spain, Belgium, Poland, Turkey and Brazil. Pharmacological studies ''in vitro'' showed it to inhibit reuptake and promote the release of monoamine neurotransmitters with some selectivity for serotonin, but it failed to produce stimulant effects in animals, and has a pharmacological profile more comparable to that of sedating empathogens such as MDAI and 5-Methyl-MDA. See also * 4-Et-PVP * 6-APT * EDMA * Indapyrophenidone * Naphyrone * O-2390 O-2390 (3,4-Dichloro-alpha-PVP, DCPVP) is a recreational designer drug from the substituted cathinone family, which acts as a potent inhibitor of dopamine and noradrenaline reuptake ''in vitro'', with weaker but still significant inhibition of se ... References {{Entactogens, state=expanded D ...
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βk-Ephenidine
2-(Ethylamino)-1,2-diphenylethanone (also known as α-ethylamino-deoxybenzoin, ±-(Ethylamino)benzyl(phenyl)-ketone and βk-Ephenidine) is a chemical compound which was first invented in 1955, researched by ICI in 1969 as an antidepressant, and subsequently claimed by AstraZeneca as an inhibitor of the enzyme 11β-Hydroxysteroid dehydrogenase type 1. No other pharmacological data has been disclosed, though its chemical structure closely resembles that of certain designer drug compounds such as ephenidine and N-ethylhexedrone. See also * α-PCYP * Fluorolintane * Indapyrophenidone * Lefetamine * UWA-001 UWA-001 (also known as α-phenyl-MDMA and methylenedioxymephenidine) is a phenethylamine derivative invented at the University of Western Australia as non-toxic alternative to 3,4-methylenedioxy-''N''-methylamphetamine (MDMA) and researched as ... References Enzyme inhibitors AstraZeneca brands {{nervous-system-drug-stub ...
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Lefetamine
Lefetamine (Santenol) is a drug which is a stimulant and also an analgesic with effects comparable to codeine. Discovery Lefetamine-related 1,2-diphenylethylamines were invented in the 1940s and showed weak analgesic activity. It was investigated in Japan in 1950s. The l-isomer showed weak analgesic action comparable to codeine and antitussive action far weaker than codeine. The d-isomer showed no such activity but caused seizures in rats. Society and culture It was abused in Japan during the 1950s. In a small study in 1989 it showed some effect against opioid withdrawal symptoms without causing withdrawal symptoms itself. It was concluded that it may be an opioid partial agonist. It has been abused in Europe; in 1989 a small study of 15 abusers and some volunteers found that it had some partial similarity to opioids, that it produced withdrawal symptoms, and had dependence and abuse potential to a certain degree. In a small study in 1994, it was compared to clonid ...
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Drugs With Unknown Mechanisms Of Action
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via inhalation, injection, smoking, ingestion, absorption via a patch on the skin, suppository, or dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to treat, cure, prevent, or diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a regular basis for chronic disorders. Pharmaceutical drugs are often classified into drug classes—groups of related drugs ...
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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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Pyrovalerone
(Centroton, 4-Methyl-β-keto-prolintane, Thymergix, O-2371) is a psychoactive drug with stimulant effects via acting as a norepinephrine-dopamine reuptake inhibitor (NDRI), and is used for the clinical treatment of chronic fatigue or lethargy and as an anorectic or appetite suppressant for weight loss purposes. It was developed in the late 1960s and has since been used in France and several other European countries, and although pyrovalerone is still occasionally prescribed, it is used infrequently due to problems with abuse and dependence. It is closely related on a structural level to a number of other stimulants, such as α-PVP, MDPV and prolintane (Promotil, Katovit). Side effects of pyrovalerone include anorexia or loss of appetite, anxiety, fragmented sleep or insomnia, and trembling, shaking, or muscle tremors. Withdrawal following abuse upon discontinuation often results in depression. The ''R''-enantiomer of pyrovalerone is devoid of activity. See also * ...
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Methoxphenidine
Methoxphenidine (methoxydiphenidine, 2-MeO-Diphenidine, MXP) is a dissociative of the diarylethylamine class that has been sold online as a designer drug. Methoxphenidine was first reported in a 1989 patent where it was tested as a treatment for neurotoxic injury. Shortly after the 2013 UK ban on arylcyclohexylamines methoxphenidine and the related compound diphenidine became available on the gray market, where it has been encountered as a powder and in tablet form. Though diphenidine possesses higher affinity for the NMDA receptor, anecdotal reports suggest methoxphenidine has greater oral potency. Of the three isomeric anisyl-substituents methoxphenidine has affinity for the NMDA receptor that is higher than 4-MeO-Diphenidine but lower than 3-MeO-Diphenidine, a structure–activity relationship shared by the arylcyclohexylamines. Side effects Acute methoxphenidine intoxication has been reported to produce confusion, hypertension, and tachycardia that was responsive to treat ...
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Ephenidine
Ephenidine (also known as NEDPA and EPE) is a dissociative anesthetic that has been sold online as a designer drug. It is illegal in some countries as a structural isomer of the banned opioid drug lefetamine, but has been sold in countries where it is not yet banned. Pharmacology Pharmacodynamics Ephenidine and related diarylethylamines have been studied in vitro as treatments for neurotoxic injuries, and are antagonists of the NMDA receptor (Ki = 66.4 nM for ephenidine). Ephenidine also possesses weaker affinity for dopamine and norepinephrine transporters (379 nM and 841 nM, respectively) as well as σ1R (629 nM) and σ2R (722 nM) binding sites. Pharmacokinetics Metabolism Ephenidine's metabolic pathway consists of N-oxidation, N-dealkylation, mono- and bis-hydroxylation of the benzene ring, and hydroxylation of the phenyl ring only after N-dealkylation. The dihydroxy metabolites were conjugated by methylation of one hydroxy group, and hydroxy metab ...
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Designer Drug
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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Diphenidine
Diphenidine (1,2-DEP, DPD, DND) is a dissociative anesthetic that has been sold as a designer drug. The synthesis of diphenidine was first reported in 1924, and employed a Bruylants reaction analogous to the one that would later be used to discover phencyclidine in 1956. Shortly after the 2013 UK ban on arylcyclohexylamines, diphenidine and the related compound methoxphenidine became available on the grey market. Anecdotal reports describe high doses of diphenidine producing "bizarre somatosensory phenomena and transient anterograde amnesia." Diphenidine and related diarylethylamines have been studied in vitro as treatments for neurotoxic injury and are antagonists of the NMDA receptor. In dogs diphenidine exhibits greater antitussive potency than codeine phosphate. Electrophysiological analysis demonstrates that the amplitude of NMDA-mediated fEPSPs are reduced by diphenidine and ketamine to a similar extent, with diphenidine displaying a slower onset of antagonism. The two en ...
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