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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 α-PCyP (α-PyrrolidinoCyclohexanoPhenone) is a stimulant drug of the Substituted cathinone, cathinone class that has been sold online as a designer drug. In a series of alpha-substituted pyrrolidinyl cathinone derivatives developed in 2015, th ... * Alpha-D2PV * Fluorolintane * Indapyrophenidone * Lefetamine * UWA-001 References Enzyme inhibitors Drugs developed by AstraZeneca {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ephenidine
Ephenidine (also known as NEDPA and EPE) is a Dissociative drug, dissociative anesthesia, 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 Receptor antagonist, antagonists of the NMDA receptor (Ki = 66.4 nM for ephenidine). Ephenidine also possesses weaker affinity for Dopamine transporter, dopamine and norepinephrine transporters (379 nM and 841 nM, respectively) as well as Sigma-1 receptor, σ1R (629 nM) and Sigma-2 receptor, σ2R (722 nM) binding sites. Pharmacokinetics Metabolism Ephenidine's metabolic pathway consists of N-oxidation, N-dealkylation, mono- and bis-hydroxylation of the benzyl ring, and hydroxylation of the phenyl ring only after N-dea ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
α-PCYP
α-PCyP (α-PyrrolidinoCyclohexanoPhenone) is a stimulant drug of the Substituted cathinone, cathinone class that has been sold online as a designer drug. In a series of alpha-substituted pyrrolidinyl cathinone derivatives developed in 2015, the alpha-cyclopentyl derivative was found to have around the same potency ''in vitro'' as an dopamine reuptake inhibitor, inhibitor of the dopamine transporter as the alpha-propyl derivative alpha-Pyrrolidinopentiophenone, α-PVP, while the alpha-cyclohexyl derivative α-PCyP was around twice as strong. See also * Rolicyclidine, PCPy * Picilorex * Alpha-Pyrrolidinohexiophenone, α-PHP * α-PHiP * Alpha-D2PV * βk-Ephenidine * Diphenidine * Indapyrophenidone * UWA-101 * Zylofuramine References Pyrrolidinophenones Designer drugs Serotonin-norepinephrine-dopamine releasing agents {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 * 3,4-Pr-PipVP * 5-BPDi * Alpha-D2PV * βk-Ephenidine * Diphenidine * Ephenidine * Lefetamine * Methoxphenidine * Pyrovalerone (Centroton, 4-Methyl-β-keto-prolintane, Thymergix, O-2371) is a central nervous system (CNS) stimulant that acts as a norepinephrine–dopamine reuptake inhibitor (NDRI). It was developed in the 1980s and had briefly been approved in Spain an ... * TH-PVP References Designer drugs Drugs with unknown mechanisms of action Stimulants 1,2-Diarylethylamines Pyrrolidinophenones {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Imperial Chemical Industries
Imperial Chemical Industries (ICI) was a British Chemical industry, chemical company. It was, for much of its history, the largest manufacturer in Britain. Its headquarters were at Millbank in London. ICI was listed on the London Stock Exchange and was a constituent of the FT 30 and later the FTSE 100 Index, FTSE 100 indices. ICI was formed in 1926 as a result of the merger of four of Britain's leading chemical companies. From the onset, it was involved in the production of various chemicals, explosives, fertilisers, insecticides, dyestuffs, non-ferrous metals, and paints; the firm soon become involved in plastics and a variety of speciality products, including food ingredients, polymers, electronic materials, fragrances and flavourings. During the Second World War, ICI's subsidiary Nobel Enterprises, ICI Nobel produced munitions for Britain's war effort; the wider company was also involved with Britain's nuclear weapons programme codenamed Tube Alloys. Throughout the 1940s and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidepressant
Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathisia, sexual dysfunction, and emotional blunting. There is an increased risk of Suicidal ideation, suicidal thinking and Suicide, behavior when taken by children, adolescents, and young adults. Antidepressant discontinuation syndrome, Discontinuation syndrome, which resembles recurrent Depression (mood), depression in the case of the Selective serotonin reuptake inhibitor, SSRI class, may occur after stopping the intake of any antidepressant. Research regarding the effectiveness of antidepressants for depression in adults is controversial and has found both benefits and drawbacks. Meanwhile, evidence of benefit in children and adolescents is unclear, even though antidepressant use has considerably increased in children and adolescents in th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AstraZeneca
AstraZeneca plc () (AZ) is a British-Swedish multinational pharmaceutical and biotechnology company with its headquarters at the Cambridge Biomedical Campus in Cambridge, UK. It has a portfolio of products for major diseases in areas including oncology, cardiovascular, gastrointestinal, infection, neuroscience, respiratory, and inflammation. The company was founded in 1999 through the merger of the Swedish Astra AB and the British Zeneca Group (itself formed by the demerger of the pharmaceutical operations of Imperial Chemical Industries in 1993). Its portfolio includes primary and speciality care, coverage for rare diseases, and a robust global presence across various regions. Since the merger it has been among the world's largest pharmaceutical companies and has made numerous corporate acquisitions, including Cambridge Antibody Technology (in 2006), MedImmune (in 2007), Spirogen (in 2013) and Definiens (by MedImmune in 2014). It has its research and development conc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
11β-Hydroxysteroid Dehydrogenase Type 1
11β-Hydroxysteroid dehydrogenase type 1, also known as cortisone reductase, is an NADPH-dependent enzyme highly expressed in key metabolic tissues including liver, adipose tissue, and the central nervous system. In these tissues, HSD11B1 reduces cortisone to the active hormone cortisol that activates glucocorticoid receptors. It belongs to the family of short-chain dehydrogenases. It is encoded by the gene. Function The protein encoded by this gene is a microsomal enzyme that catalyzes the conversion of the stress hormone cortisol to the inactive metabolite cortisone. In addition, the encoded protein can catalyze the reverse reaction, the conversion of cortisone to cortisol. Too much cortisol can lead to central obesity, and a particular variation in this gene has been associated with obesity and insulin resistance in children. Two transcript variants encoding the same protein have been found for this gene. Clinical significance 11β-HSD1 is inhibited by carbenoxolone, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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, Australia, and New Zealand, as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these designer drugs 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 tr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
N-ethylhexedrone
''N''-Ethylhexedrone (also known as α-ethylaminocaprophenone, ''N''-ethylnorhexedrone, hexen, and NEH) is a stimulant of the cathinone class that acts as a norepinephrine–dopamine reuptake inhibitor (NDRI) with IC50 inhibition values of 0.0978 and 0.0467 μM, respectively (97 nM and 46 nM). ''N''-Ethylhexedrone was first mentioned in a series of patents by Boehringer Ingelheim in the 1960s which led to the development of the better-known drug methylenedioxypyrovalerone (MDPV). Since the mid-2010s, ''N''-ethylhexedrone has been sold online as a designer drug. In 2018, ''N''-ethylhexedrone was the second most common drug of the cathinone class to be identified in Drug Enforcement Administration seizures. ''N''-Ethylhexedrone was first synthesized by Boehringer Ingelheim in 1964. It appears to have emerged on the online research chemical market in late 2015. It is an example of a novel psychoactive substance specifically chosen to mimic the features of prohibited substance ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluorolintane
Fluorolintane (also known as 2-FPPP and 2-F-DPPy) is a dissociative anesthetic drug that has been sold online as a designer drug. Fluorolintane and related diarylethylamines are antagonists of the NMDA receptor and have been studied ''in vitro'' as potential treatments for neurotoxic injury, depression and as sympathomimetic. See also * AD-1211 * Alpha-D2PV * Diphenidine * Ephenidine * Lanicemine Lanicemine (AZD6765) is a low-trapping NMDA receptor antagonist that was under drug development, development by AstraZeneca for the management of severe and treatment-resistant depression. Lanicemine differs from ketamine in that it is a ''low- ... * Methoxphenidine (MXP) * MT-45 * Prolintane * Remacemide References Designer drugs Dissociative drugs NMDA receptor antagonists 1,2-Diarylethylamines 2-Fluorophenyl compounds Phenyl compounds 1-Pyrrolidinyl compounds {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lefetamine
Lefetamine (Santenol) is a drug which is a stimulant and also an analgesic with effects comparable to codeine. Discovery The parent structure of lefetamine, 1,2-diphenylethylamine was first synthesized in the 1940s and showed weak analgesic activity. Lefetamine itself was first investigated in Japan in the 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 sm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
