O-4310
O-4310, also known as 1-isopropyl-6-fluoropsilocin, is a serotonin receptor agonist of the tryptamine family. It is the 1-isopropylated and 6- flourinated derivative of the serotonergic psychedelic psilocin. Pharmacology The drug is said to be a serotonin 5-HT2A receptor agonist and to be highly selective for activation of this receptor over the closely related serotonin 5-HT2B and 5-HT2C receptors. Its at the serotonin 5-HT2A receptor was reported to be 5nM and it was said to have an of 89% relative to serotonin. Conversely, O-4310 was said to be inactive at the serotonin 5-HT2B receptor, with no or reported for this receptor, and was claimed to have an of 592nM at the serotonin 5-HT2C receptor with an of approximately 50%. Hence, O-4310 appears to show about 118-fold selectivity for activation of the serotonin 5-HT2A receptor over the serotonin 5-HT2C receptor. The pharmacodynamic activity of O-4310 was briefly described in a patent but not in the published scientifi ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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5-HT2A Receptor
The 5-HT2A receptor is a subtype of the 5-HT2 receptor, 5-HT2 receptor that belongs to the serotonin receptor family and functions as a GPCR, G protein-coupled receptor (GPCR). It is a cell surface receptor that activates multiple intracellular signalling cascades. Like all 5-HT2 receptors, the 5-HT2A receptor is coupled to the Gq protein, Gq/G11 signaling pathway. It is the primary excitatory receptor subtype among the serotonin-responsive GPCRs. The 5-HT2A receptor was initially noted for its central role as the primary target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. It later regained research prominence when found to mediate, at least in part, the effects of many antipsychotic drugs, particularly atypical antipsychotic, atypical antipsychotics. Downregulation of post-synaptic 5-HT2A receptors is an adaptive response triggered by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Elevated 5-HT2A ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Substituted Tryptamine
Substituted tryptamines, or simply tryptamines, also known as serotonin analogues (i.e., 5-hydroxytryptamine analogues), are organic compounds which may be thought of as being derived from tryptamine itself. The molecular structures of all tryptamines contain an indole ring, joined to an amino group, amino (NH2) group via an ethyl (−CH2–CH2−) side chain, sidechain. In substituted tryptamines, the indole ring, sidechain, and/or amino group are modified by substituting another group for one of the hydrogen (H) atoms. Well-known tryptamines include serotonin, an important neurotransmitter, and melatonin, a hormone involved in regulating the sleep-wake cycle. Tryptamine alkaloids are found in fungi, plants and animals; and sometimes used by humans for the neurological or psychotropic effects of the substance. Prominent examples of tryptamine alkaloids include psilocybin (from "psilocybin mushrooms") and dimethyltryptamine, DMT. In South America, dimethyltryptamine is obtained f ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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1-Methyltryptamine
1-Methyltryptamine (1-methyl-T, 1-MT or 1-Me-T; code name PAL-637) is a serotonin receptor agonist and monoamine releasing agent of the substituted tryptamine, tryptamine family. It is the 1-methyl group, methyl chemical derivative, derivative of tryptamine (T; PAL-235). The drug is known to act as a serotonin 5-HT2A receptor, 5-HT2A receptor agonist (Ki = 473nM; = 209–4,560nM; = 55–99%), as a serotonin releasing agent ( = 53.1nM), and to be inactive in inducing the release of norepinephrine and dopamine ( = >10,000nM). Its activities at other serotonin receptors were not reported. 1-Methyltryptamine shows dramatically reduced affinity (pharmacology), affinity and receptor activation, activational potency (pharmacology), potency as well as reduced intrinsic activity, efficacy at the serotonin 5-HT2A receptor compared to tryptamine (which showed Ki = 13.1nM; = 7.36–99nM; = 101–104%). It also shows slightly reduced potency as a serotonin releasing agent and abolished act ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Organix Inc
Organix Inc is a US fine chemicals company specialising in chemical synthesis of analytical standards and custom synthesis of finished compounds and intermediates.{{Citation needed, date=February 2020 Chemistry Organix carries out research and development of novel molecules used in a variety of pharmaceutical research applications. Some notable compounds include; * O-526 * O-774 * O-806 * O-823 * O-1057 * O-1072 (Tropoxane) * O-1125 * O-1238 * O-1269 * O-1270 * O-1399 * O-1602 O-1602 is a synthetic compound most closely related to abnormal cannabidiol, and more distantly related in structure to cannabinoid drugs such as THC. O-1602 does not bind to the classical cannabinoid receptors CB1 or CB2 with any significant ... * O-1656 * O-1660 * O-1812 * O-1871 * O-1918 * O-2050 * O-2113 * O-2172 * O-2371 * O-2372 * O-2387 * O-2390 * O-2394 * O-2545 * O-2694 * O-4210 * O-4310 Life sciences industry ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Psilocin
Psilocin, also known as 4-hydroxy-''N'',''N''-dimethyltryptamine (4-HO-DMT), is a substituted tryptamine alkaloid and a serotonergic psychedelic. It is present in most psychedelic mushrooms together with its phosphorylated counterpart psilocybin. Psilocybin, as well as synthetic esters such as 4-AcO-DMT (psilacetin; ''O''-acetylpsilocin) and 4-PrO-DMT (''O''-propionylpsilocin), are prodrugs of psilocin. Acting on the serotonin 5-HT2A receptors, psilocin's psychedelic effects are directly correlated with the drug's occupancy at these receptor sites. It also interacts with other serotonin receptors and targets. The subjective mind-altering effects of psilocin are highly variable in their qualitative nature but resemble those of lysergic acid diethylamide (LSD) and ''N'',''N''-dimethyltryptamine (DMT). Psilocin is a Schedule I drug under the Convention on Psychotropic Substances. Uses Psilocin is used recreationally, spirituality or shamanically, and medically. ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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SCHEMBL5334361
SCHEMBL5334361 is a drug which acts as an agonist at the 5-HT2 family of serotonin receptors, and was developed for the treatment of glaucoma. It is a benzazepine derivative structurally related to the anorectic drug lorcaserin. It is selective for 5-HT2A, with an EC50 of 0.4nM at 5-HT2A vs 3.9nM at 5-HT2C and a much lower affinity of 417nM at 5-HT2B. See also * 3C-BZ * 4-PhPr-3,5-DMA * AL-34662 * GSK-189254 * IHCH-7113 * O-4310 * WAY-470 * Zalsupindole Zalsupindole,https://iris.who.int/bitstream/handle/10665/380497/9789240107038-eng.pdf "zalsupindolum zalsupindole (2R)-1-(5-methoxy-1H-indol-1-yl)-N,N-dimethylpropan-2-amine antidepressant" also known by its developmental code names DLX-001 and ... References Serotonin receptor agonists Benzazepines 3-Methoxyphenyl compounds {{nervous-system-drug-stub ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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1-Methylpsilocin
1-Methylpsilocin (developmental code names CMY, CMY-16) is a tryptamine derivative developed by Sandoz which acts as a selective agonist of the serotonin 5-HT2C receptor ( of 12 nM, vs. 633 nM at 5-HT2A), and an inverse agonist at 5-HT2B (Ki of 38 nM). While 1-methylpsilocin does have higher affinity for 5-HT2C than 5-HT2A, it does produce a head-twitch response in mice that is dependent on 5-HT2A, so it is not entirely free of effects on 5-HT2A ''in vivo''. In contrast to psilocin, 1-methylpsilocin did not activate 5-HT1A receptors in mice. 1-Methylpsilocin has been investigated for applications such as treatment of glaucoma, obsessive–compulsive disorder (OCD), and cluster headaches, as these conditions are amenable to treatment with psychedelic drugs but are not generally treated with such agents due to the hallucinogenic side effects they produce, which are considered undesirable. 1-Methylpsilocin therefore represents a potential alternative treatment to ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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1-Propyl-5-MeO-AMT
1-Propyl-5-MeO-AMT, also known as 1-propyl-5-methoxy-α-methyltryptamine, is a serotonin receptor modulator of the tryptamine, α-alkyltryptamine, and 5-methoxytryptamine families. It is the 1-propyl derivative of 5-methoxy-α-methyltryptamine (5-MeO-AMT). Whereas most tryptamines are highly non-selective in terms of binding to serotonin receptors, 1-propyl-5-MeO-AMT shows selectivity for the serotonin 5-HT2A receptor. Its affinities (Ki) for serotonin receptors were 12nM for the serotonin 5-HT2A receptor, 120nM for the serotonin 5-HT2C receptor, 5,000nM for the serotonin 5-HT1B receptor, 7,100nM for the serotonin 5-HT1A receptor, and >10,000nM for the serotonin 5-HT1D receptor, whereas other serotonin receptors were not reported. Its capacity and potency in activating the serotonin receptors was also not reported. The drug was developed by Richard Glennon and colleagues and was first described in 1990. At the time, it was described as the most 5-HT2A receptor-selective t ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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5-Fluoro-DMT
5-Fluoro-''N'',''N''-dimethyltryptamine (5-fluoro-DMT, 5F-DMT) is a tryptamine derivative related to compounds such as 5-bromo-DMT and 5-MeO-DMT. It is known to have affinity for and to act as an agonist of the serotonin 5-HT1A and 5-HT2A receptors. Fluorination of psychedelic tryptamines either reduces or has little effect on 5-HT2A/C receptor affinity or intrinsic activity, although 6-fluoro-DET is inactive as a psychedelic despite acting as a 5-HT2A agonist (cf. lisuride), while 4-fluoro-5-methoxy-DMT is a much stronger agonist at 5-HT1A than 5-HT2A. 5F-DMT produces a robust head-twitch response in mice, and hence is a putative serotonergic psychedelic. In another study however, it failed to substitute for LSD in rodent drug discrimination tests, at least at the assessed doses. See also * 5-Fluoro-AMT * 5-Fluoro-DET * 5-Fluoro-MET * 5-Fluoro-T * 4-Fluoro-DMT * 6-Fluoro-AMT * 6-Fluoro-DMT 6-Fluoro-DMT, also known as 6-fluoro-''N'',''N''-dimethyltryptamine, is ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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DMBMPP
DMBMPP, also known as juncosamine or as 2-(2,5-dimethoxy-4-bromobenzyl)-6-(2-methoxyphenyl)piperidine, is a highly selective serotonin 5-HT2A receptor agonist and 2-benzylpiperidine analogue of the serotonergic psychedelic 25B-NBOMe which is used in scientific research. Use Research Despite its uniquely high selectivity for the serotonin 5-HT2A receptor, it has been said that DMBMPP is not widely used as a pharmacological tool in scientific research, presumably due to its chemical synthesis being relatively inaccessible. Consequently, 25CN-NBOH, another highly selective serotonin 5-HT2A receptor agonist, has been proposed as an alternative to DMBMPP for use in scientific research. DMBMPP and 25CN-NBOH are the two most selective serotonin 5-HT2A receptor agonists known as of 2020. Pharmacology The (''S'',''S'')-isomer ((2''S'',6''S'')-DMBMPP) is the most selective agonist for the human serotonin 5-HT2A receptor yet discovered, with a affinity ( Ki) of 2.5nM at the human se ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Lespedamine
Lespedamine, also known as 1-methoxy-''N'',''N''-dimethyltryptamine (1-methoxy-DMT or 1-MeO-DMT), is an indole alkaloid and substituted tryptamine present in the plant ''Lespedeza bicolor''. The alkaloid bears a close structural resemblance to the psychedelic alkaloid dimethyltryptamine (DMT) and it was speculated by Alexander Shulgin in TiHKAL that it might be psychoactive. No reports on lespedamine's biological activity are known to have been published. See also * 1-Methyltryptamine 1-Methyltryptamine (1-methyl-T, 1-MT or 1-Me-T; code name PAL-637) is a serotonin receptor agonist and monoamine releasing agent of the substituted tryptamine, tryptamine family. It is the 1-methyl group, methyl chemical derivative, derivative of ... * 1-Methylpsilocin (1-methyl-4-HO-DMT) * 1-Propyl-5-MeO-AMT References N,N-Dialkyltryptamines Dimethylamino compounds Methoxy compounds Tryptamine alkaloids {{Alkaloid-stub ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Animal Study
Animal testing, also known as animal experimentation, animal research, and ''in vivo'' testing, is the use of animals, as model organisms, in experiments that seek answers to scientific and medical questions. This approach can be contrasted with field studies in which animals are observed in their natural environments or habitats. Experimental research with animals is usually conducted in universities, medical schools, pharmaceutical companies, defense establishments, and commercial facilities that provide animal-testing services to the industry. The focus of animal testing varies on a continuum from Basic research, pure research, focusing on developing fundamental knowledge of an organism, to applied research, which may focus on answering some questions of great practical importance, such as finding a cure for a disease. Examples of applied research include testing disease treatments, breeding, defense research, and Toxicology testing, toxicology, including Testing cosmetics ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |