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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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 meta ... [...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 * βk-Ephenidine * Diphenidine * Ephenidine * Lefetamine * Methoxphenidine * 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 letharg ... * TH-PVP References Designer drugs Diarylethylamines Drugs with unknown mechanisms of action Pyrrolidinophenones Stimulants {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Imperial Chemical Industries
Imperial Chemical Industries (ICI) was a British chemical company. It was, for much of its history, the largest manufacturer in Britain. It was formed by the merger of four leading British chemical companies in 1926. Its headquarters were at Millbank in London. ICI was a constituent of the FT 30 and later the FTSE 100 indices. ICI made general chemicals, plastics, paints, pharmaceuticals and speciality products, including food ingredients, speciality polymers, electronic materials, fragrances and flavourings. In 2008, it was acquired by AkzoNobel, which immediately sold parts of ICI to Henkel and integrated ICI's remaining operations within its existing organisation. History Development of the business (1926–1944) The company was founded in December 1926 from the merger of four companies: Brunner Mond, Nobel Explosives, the United Alkali Company, and British Dyestuffs Corporation. It established its head office at Millbank in London in 1928. Competing with Du ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidepressant
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, headaches, sexual dysfunction, and emotional blunting. There is a slight increased risk of suicidal thinking and behavior when taken by children, adolescents, and young adults. Discontinuation syndrome may occur after stopping any antidepressant which resembles recurrent depression. Some research regarding the effectiveness of antidepressants for depression in adults has found benefits, whilst other research has not. Evidence of benefit in children and adolescents is unclear. The twenty-one most commonly prescribed antidepressant medications are more effective than placebo for the short-term (acute) treatments of adults with major depressive disorder. There is debate in the medical community about how much of the observed effects of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AstraZeneca
AstraZeneca plc () is a British-Swedish multinational pharmaceutical and biotechnology company with its headquarters at the Cambridge Biomedical Campus in Cambridge, England. It has a portfolio of products for major diseases in areas including oncology, cardiovascular, gastrointestinal, infection, neuroscience, respiratory, and inflammation. It has been involved in developing the Oxford–AstraZeneca COVID-19 vaccine. 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). 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 concentrated in three strategic centres: Cambridge, Engl ... [...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 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 ... [...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 values of 0.0978 and 0.0467 μM, respectively. ''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 substances and bypass drug laws. It is one ... [...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 Sympathomimetic drugs (also known as adrenergic drugs and adrenergic amines) are stimulant compounds which mimic the effects of endogenous agonists of the sympathetic nervous system. Examples of sympathomimetic effects include increases in hea .... See also * AD-1211 * Diphenidine * Ephenidine * Lanicemine * Methoxphenidine (MXP) * MT-45 * Prolintane * Remacemide References Designer drugs Dissociative drugs NMDA receptor antagonists Diarylethylamines Fluoroarenes Pyrrolidines {{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 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 clonidine an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 a potential treatment for Parkinson's disease. It has a 5-HT2A receptor affinity of 1.2 μM (∼10-fold increase compared to MDMA), 1.3 μM for the serotonin transporter (∼4-fold decrease compared to MDMA), 13.4 μM for the norepinephrine transporter (∼26-fold increase compared to MDMA) and virtually no affinity for the dopamine transporter (>50 μM). Unlike MDMA and ''para''-methoxyamphetamine (but similarly to ketamine), UWA-001 increases prepulse inhibition and was therefore considered to be non-psychoactive, though it was not assayed at other binding sites. It is toxic to the SH-SY5Y cell line at high concentrations, however significantly less toxic than MDMA at all concentrations tested. UWA-001 is structurally related to th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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