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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] |
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] |
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] |
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] |
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] |
Serotonin Receptor Modulator
5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in multiple tissues including the central and peripheral nervous systems. They mediate both excitatory and inhibitory neurotransmission. The serotonin (i.e., 5-hydroxytryptamine, hence "5-HT") receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many neurotransmitters, including glutamate, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. Serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, and thermoregulation. They are the target of a variety of pharmaceutical and recreational drugs, includin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1B Receptor
5-hydroxytryptamine receptor 1B also known as the 5-HT1B receptor is a protein that in humans is encoded by the ''HTR1B'' gene. The 5-HT1B receptor is a 5-HT receptor subtype. Tissue distribution and function 5-HT1B receptors are widely distributed throughout the central nervous system with the highest concentrations found in the frontal cortex, basal ganglia, striatum, and the hippocampus. The function of the 5-HT1B receptor differs depending upon its location. In the frontal cortex, it is believed to act as a terminal receptor inhibiting the release of dopamine. In the basal ganglia and the striatum, evidence suggests 5-HT signaling acts on an autoreceptor, inhibiting the release of serotonin and decreasing glutamatergic transmission by reducing miniature excitatory postsynaptic potential (mEPSP) frequency, respectively. In the hippocampus, a recent study has demonstrated that activation of postsynaptic 5-HT1B heteroreceptors produces a facilitation in excitatory synapt ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-Methoxytryptamines
5-Methoxytryptamine (5-MT, 5-MeO-T, or 5-OMe-T), also known as serotonin methyl ether or ''O''-methylserotonin and as mexamine, is a tryptamine derivative closely related to the neurotransmitters serotonin and melatonin. It has been shown to occur naturally in the body in low levels, especially in the pineal gland. It is formed via ''O''-methylation of serotonin or ''N''-deacetylation of melatonin. 5-MT is a highly potent and non-selective serotonin receptor agonist and shows serotonergic psychedelic-like effects in animals. However, it is inactive in humans, at least orally, likely due to rapid metabolism by monoamine oxidase (MAO). The levels and effects of 5-MT are dramatically potentiated by monoamine oxidase inhibitors (MAOIs) in animals. Biosynthesis 5-MT can be formed by ''O''-methylation of serotonin mediated by hydroxyindole ''O''-methyltransferase (HIOMT) or by ''N''-deacetylation of melatonin. It is also a precursor of 5-MeO-DMT in some species. Pharmacology Ph ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-Alkyltryptamines
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] |
Methysergide
Methysergide, sold under the brand names Deseril and Sansert, is a monoaminergic medication of the ergoline and lysergamide groups which is used in the prophylaxis and treatment of migraine and cluster headaches. It has been withdrawn from the market in the United States and Canada due to safety concerns. It is taken by mouth. The drug is a prodrug of methylergometrine (methylergonovine), which circulates at levels about 10times higher than those of methysergide during treatment with methysergide. Whereas methysergide is a mixed agonist of some serotonin receptors (e.g., the 5-HT1 receptors) and antagonist of other serotonin receptors (e.g., the 5-HT2 receptors), methylergonovine is a non-selective agonist of most of the serotonin receptors, including of both the serotonin 5-HT1 and 5-HT2 receptor subgroups. Methysergide and methylergometrine are ergolines and lysergamides and are related to the ergot alkaloids. Previously thought to be an exclusively synthetic compound, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MLD-41
MLD-41, also known as 1-methyl-LSD, is a derivative of LSD that has about one-third the psychoactive effects. It has been studied in cross-tolerance Cross-tolerance is a phenomenon that occurs when tolerance to the effects of a certain drug produces tolerance to another drug. It often happens between two drugs with similar functions or effects—for example, acting on the same cell receptor ... of LSD. Metabolism of other 1-methylated ergoloids to their secondary amine derivatives has been frequently noted in mammals. References Diethylamino compounds Methyl compounds Psychedelic lysergamides {{Hallucinogen-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Richard Glennon
Richard A. Glennon is an American medicinal chemist who studies psychedelics, stimulants, entactogens, and other psychoactive drugs. He has been an important pioneer of the use of animal drug discrimination tests in scientific research for studying psychoactive drugs like hallucinogens. Glennon has also done a large amount of work on the structure–activity relationships of psychedelics. In addition, he played an important role in the discovery that the hallucinogenic effects of psychedelics are mediated by activation of serotonin 5-HT2 receptors. He is one of the most widely cited scientists in his field. Glennon was the editor-in-chief of the journal '' Medicinal Chemistry Research'' from 1992 to 2002. He retired in 2022 but has continued to publish reviews and research since then. Selected publications * * * * * * * * * * * * * * * * * * * See also * David E. Nichols * Bryan Roth * Alexander Shulgin * Daniel Trachsel Daniel Trachsel is a Swiss people, S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
