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O-4310
O-4310 (1-isopropyl-6-fluoro-psilocin) is a tryptamine derivative developed by Organix Inc which acts as a serotonin receptor agonist. It is claimed to have an EC50 of 5nM at 5-HT2A with 89% efficacy vs 5-HT, and 100x selectivity over 5-HT2C, while being apparently inactive at the 5-HT2B antitarget. See also * 1-Methylpsilocin * 5-Fluoro-DMT * Psilocin * SCHEMBL5334361 * 7F-5-MeO-MET 5-MeO-7-F-MET (5-MeO-7F-MET, 5-Methoxy-7-fluoro-''N''-methyl-''N''-ethyltryptamine) is a tryptamine derivative which acts as a serotonin receptor agonist selective for the 5-HT2 subtypes, with a pEC50 of 8.71 at 5-HT2A, vs 8.25 at 5-HT2B and 7 ... References Tryptamines Fluoroarenes Isopropyl compounds Dimethylamino compounds Phenols {{Pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tryptamines
Substituted tryptamines, or serotonin 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 (NH2) group via an ethyl (−CH2–CH2−) 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 DMT. In South America, dimethyltryptamine is obtained from numerous plant sources, like chacruna, and it is often used in ayahuasca brews. Many synthetic tryptamines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
1-Methylpsilocin
1-Methylpsilocin is a tryptamine derivative which acts as a selective agonist for the 5-HT2C receptor (IC50 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 are 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, 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 psilocin that may be less likely to produce hallucinogenic effects. See also * 2-Bromo-LSD * CP-1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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. 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. See also * 5-Fluoro-AMT * 5-Fluoro-DET * 5-Fluoro-MET * 6-fluoro-AMT * 6-Fluoro-DMT * 4-fluoro-5-methoxy-DMT * 6-Fluoro-DET 6-Fluoro-DET (6F-DET, 6-fluoro-''N,N''-diethyltryptamine) is a substituted tryptamine derivative related to drugs such as DET and 5-fluoro-DET. It acts as a partial agonist at the 5-HT2A receptor, but while it produces similar physiological eff ...br>6-Fluoro-DET * O-4310 *It's worth noting that GR-159897 is based on the same structure. References Psychedelic tryptamines Tryptamines Fluo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A Receptor
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). The 5-HT2A receptor is a cell surface receptor, but has several intracellular locations. 5-HT is short for 5-hydroxy-tryptamine or serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones. Downregulation of post-synaptic 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Suicidal and otherwis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 * AAZ-A-154 * AL-34662 * GSK-189254 * IHCH-7113 * O-4310 O-4310 (1-isopropyl-6-fluoro-psilocin) is a tryptamine derivative developed by Organix Inc which acts as a serotonin receptor agonist. It is claimed to have an EC50 of 5nM at 5-HT2A with 89% efficacy vs 5-HT, and 100x selectivity over 5-HT2C, ... References Serotonin receptor agonists Benzazepines O-methylated phenols {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Psilocin
Psilocin (also known as 4-HO-DMT, 4-hydroxy DMT, psilocine, psilocyn, or psilotsin) is a substituted tryptamine alkaloid and a serotonergic psychedelic substance. It is present in most psychedelic mushrooms together with its phosphorylated counterpart psilocybin. Psilocin is a Schedule I drug under the Convention on Psychotropic Substances. Acting on the 5-HT2A receptors, psilocin modulates the production and reuptake of serotonin. The mind-altering effects of psilocin are highly variable and subjective and resemble those of LSD and DMT. Chemistry Psilocin and its phosphorylated cousin, psilocybin, were first isolated and named in 1958 by Swiss chemist Albert Hofmann. Hofmann obtained the chemicals from laboratory-grown specimens of the entheogenic mushroom ''Psilocybe mexicana''. Hofmann also succeeded in finding synthetic routes to these chemicals. Psilocin can be obtained by dephosphorylation of natural psilocybin under strongly acidic or under alkaline conditions (hyd ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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-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 O-4310 (1-isopropyl-6-fluoro-psilocin) is a tryptamine derivative developed by Organix Inc which acts as a serotonin receptor agonist. It is claimed to have an EC50 of 5nM at 5-HT2A with 89% efficacy vs 5-HT, and 100x selectivity over 5-HT2C, ... Life sciences industry ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isopropyl Compounds
In organic chemistry, propyl is a three-carbon alkyl substituent with chemical formula for the linear form. This substituent form is obtained by removing one hydrogen atom attached to the terminal carbon of propane. A propyl substituent is often represented in organic chemistry with the symbol Pr (not to be confused with the element praseodymium). An isomeric form of propyl is obtained by moving the point of attachment from a terminal carbon atom to the central carbon atom, named 1-methylethyl or isopropyl. To maintain four substituents on each carbon atom, one hydrogen atom has to be moved from the middle carbon atom to the carbon atom which served as attachment point in the ''n''-propyl variant, written as . Linear propyl is sometimes termed normal and hence written with a prefix ''n''- (i.e., ''n-''propyl), as the absence of the prefix ''n''- does not indicate which attachment point is chosen, i.e. absence of prefix does not automatically exclude the possibility of it be ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
7F-5-MeO-MET
5-MeO-7-F-MET (5-MeO-7F-MET, 5-Methoxy-7-fluoro-''N''-methyl-''N''-ethyltryptamine) is a tryptamine derivative which acts as a serotonin receptor agonist selective for the 5-HT2 subtypes, with a pEC50 of 8.71 at 5-HT2A, vs 8.25 at 5-HT2B and 7.69 at 5-HT2C. In animal tests it produced the most potent head-twitch response of a range of related fluorinated tryptamine derivatives tested, though still with slightly lower potency than psilocybin. See also * 5-MeO-MET * 4-Fluoro-5-methoxy-DMT * 5-Methoxy-7,N,N-trimethyltryptamine * 7-Chloro-AMT 7-Chloro-α-methyltryptamine (7-Cl-AMT) is a tryptamine derivative with stimulant effects, invented in the 1960s. It is a weak monoamine oxidase inhibitor but its pharmacology has not otherwise been studied by modern techniques, though several c ... References {{Hallucinogens Designer drugs Psychedelic tryptamines Serotonin receptor agonists Tryptamines Fluoroarenes Methoxy compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tryptamine
Tryptamine is an indolamine metabolite of the essential amino acid, tryptophan. The chemical structure is defined by an indole ─ a fused benzene and pyrrole ring, and a 2-aminoethyl group at the second carbon (third aromatic atom, with the first one being the heterocyclic nitrogen). The structure of tryptamine is a shared feature of certain aminergic neuromodulators including melatonin, serotonin, bufotenin and psychedelic derivatives such as dimethyltryptamine (DMT), psilocybin, psilocin and others. Tryptamine has been shown to activate trace amine-associated receptors expressed in the mammalian brain, and regulates the activity of dopaminergic, serotonergic and glutamatergic systems. In the human gut, symbiotic bacteria convert dietary tryptophan to tryptamine, which activates 5-HT4 receptors and regulates gastrointestinal motility. Multiple tryptamine-derived drugs have been developed to treat migraines, while trace amine-associated receptors are being explored as a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antitarget
In pharmacology, an antitarget (or off-target) is a receptor, enzyme, or other biological target that, when affected by a drug, causes undesirable side-effects. During drug design and development, it is important for pharmaceutical companies to ensure that new drugs do not show significant activity at any of a range of antitargets, most of which are discovered largely by chance. Among the best-known and most significant antitargets are the hERG channel and the 5-HT2B receptor, both of which cause long-term problems with heart function that can prove fatal (long QT syndrome and cardiac fibrosis, respectively), in a small but unpredictable proportion of users. Both of these targets were discovered as a result of high levels of distinctive side-effects during the marketing of certain medicines, and, while some older drugs with significant hERG activity are still used with caution, most drugs that have been found to be strong 5-HT2B agonists were withdrawn from the market, and any new ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
