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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] |
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] |
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] |
6-Fluoro-DMT
6-Fluoro-DMT, also known as 6-fluoro-''N'',''N''-dimethyltryptamine, is a synthetic serotonin receptor modulator of the tryptamine family. Effects 6-Fluoro-DMT has been said to not be active as a hallucinogen in humans. It has been claimed that this is due to it being " metabolically blocked", though this was not further elaborated on. In the 1960s, it had been theorized by Stephen Szára and colleagues that psychedelic tryptamines were prodrugs that required 6-hydroxylation to become hallucinogenic, but this theory was later found to be incorrect. 6-Fluoro-DMT has been thought to be inactive as a psychedelic in part because 6-fluoro-DET is inactive in terms of such effects. Pharmacology 6-Fluoro-DMT is known to possess varying affinities for serotonin receptors, adrenergic receptors, dopamine receptors, histamine receptors, the imidazoline I1 receptor, sigma receptors, and the serotonin transporter (SERT). It has been found to be a potent partial agonist of the seroto ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-Fluoro-DMT
4-Fluoro-DMT (or 4-F-DMT), also known as 4-fluoro-''N'',''N''-dimethyltryptamine, is a serotonin receptor agonist of the tryptamine family and a close analogue of psilocin (4-HO-DMT) and dimethyltryptamine (DMT). It is a modestly selective serotonin 5-HT2C receptor full agonist and doesn't appear to produce psychedelic-like effects in animals but instead produces antiobsessional-like effects. Pharmacology The drug's affinity (Ki) for the serotonin 5-HT1A receptor was 135nM. This can be compared to psilocin's affinity of 378nM and serotonin's affinity of 1.7nM. In another study, 4-F-DMT showed affinities (Ki) of 335nM for the serotonin 5-HT2A receptor, 8.39nM for the serotonin 5-HT2B receptor, and 82–84nM for the serotonin 5-HT2C receptor. Its activational potencies () and efficacies () were 949nM (49%) at the serotonin 5-HT2A receptor, 1,180nM (38%) at the serotonin 5-HT2B receptor, and 99nM (93%) at the serotonin 5-HT2C receptor. 4-F-DMT showed dramatically less pote ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-Fluoro-DET
5-Fluoro-DET (5F-DET, 5-fluoro-''N,N''-diethyltryptamine) is a tryptamine derivative related to drugs such as DET and 5-MeO-DET. It acts as an inhibitor of the enzyme myeloperoxidase, and is also thought to be an agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ... at the 5-HT2A receptor. See also * 5F-DMT * 5F-MET * 5F-EPT * 5F-T * 6F-DET References N,N-Dialkyltryptamines Diethylamino compounds Fluoroarenes 5-Halotryptamines Psychedelic tryptamines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluoroarenes
In organic chemistry, an aryl halide (also known as a haloarene) is an aromatic compound in which one or more hydrogen atoms directly bonded to an aromatic ring are replaced by a halide ion (such as fluorine F''−'', chlorine Cl−1,−3,−5, bromine Br−1, or iodine I−). Aryl halides are distinct from haloalkanes (alkyl halides) due to significant differences in their methods of preparation, chemical reactivity, and physical properties. The most common and important members of this class are aryl chlorides, but the group encompasses a wide range of derivatives with diverse applications in organic synthesis, pharmaceuticals, and materials science. Classification according to halide Aryl fluorides Aryl fluorides are used as synthetic intermediates, e.g. for the preparation of pharmaceuticals, pesticides, and liquid crystals. The conversion of diazonium salts is a well established route to aryl fluorides. Thus, anilines are precursors to aryl fluorides. In the classic Schiemann ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dimethylamino Compounds
Dimethylamine is an organic compound with the formula (CH3)2NH. This secondary amine is a colorless, flammable gas with an ammonia-like odor. Dimethylamine is commonly encountered commercially as a solution in water at concentrations up to around 40%. An estimated 270,000 tons were produced in 2005. Structure and synthesis The molecule consists of a nitrogen atom with two methyl substituents and one hydrogen. Dimethylamine is a base (chemistry), weak base and the pKa of the ammonium CH3--CH3 is 10.73, a value above methylamine (10.64) and trimethylamine (9.79). Dimethylamine reacts with acids to form salts, such as dimethylamine hydrochloride, an odorless white solid with a melting point of 171.5 °C. Dimethylamine is produced by catalytic reaction of methanol and ammonia Ammonia is an inorganic chemical compound of nitrogen and hydrogen with the chemical formula, formula . A Binary compounds of hydrogen, stable binary hydride and the simplest pnictogen hydride, ammoni ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GR-159897
GR-159897 is a potent and selective NK2 receptor antagonist drug. It has anxiolytic effects in animal models, and also inhibits bronchoconstriction of the airways, which may potentially make it useful in the treatment of asthma. See also * Ibodutant * Nepadutant * Saredutant Saredutant (SR-48,968) is a drug that acts as a NK2 receptor antagonist. It was under development by Sanofi-Aventis as a novel antidepressant and anxiolytic and made it to phase III clinical trials. However, in May 2009, Sanofi-Aventis publishe ... References Anxiolytics N,N-Dialkyltryptamines Ethers Fluoroarenes 5-Halotryptamines NK2 receptor antagonists Piperidines Sulfoxides {{Anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 effects to psychedelic drugs, it does not appear to produce psychedelic effects itself even at high doses. Relatedly, 6-F-DET does not substituted for LSD in drug discrimination tests and does not produce the head-twitch response in rodents. For the preceding reasons, it saw some use as an active placebo in early clinical trials of psychedelic drugs but was regarded as having little use otherwise, though more recent research into compounds such as AL-34662, TBG and zalsupindole has shown that these kind of non-psychedelic 5-HT2A agonists can have various useful applications. A hypothesis for the lack of head-twitch response in mice and hallucinogenic effects in humans is that 6-F-DET acts as a 5-HT2A receptor partial agonist of the Gq sign ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-Fluoro-5-methoxy-DMT
4-Fluoro-5-Methoxy-''N'',''N''-dimethyltryptamine (4-F-5-MeO-DMT) was first described by David E. Nichols team in 2000. It is a potent 5-HT1A agonist. Substitution with the 4-fluorine markedly increased 5-HT1A selectivity over 5-HT2A/2C receptors with potency greater than that of the 5-HT1A agonist 8-OH-DPAT. The analog compound with the ''N'',''N''-dialkyl substituents constrained into a pyrrolidine ring, is a slightly stronger agonist for the 5-HT1A receptor and retains the selectivity over the 5-HT2A/2C receptors. See also * 4-HO-5-MeO-DMT * 5-Fluoro-AMT * 6-Fluoro-DMT 6-Fluoro-DMT, also known as 6-fluoro-''N'',''N''-dimethyltryptamine, is a synthetic serotonin receptor modulator of the tryptamine family. Effects 6-Fluoro-DMT has been said to not be active as a hallucinogen in humans. It has been claimed th ... * 7F-5-MeO-MET * 4-F-5-MeO-pyr-T References N,N-Dialkyltryptamines 5-Methoxytryptamines Psychedelic tryptamines Serotonin receptor agonists< ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
6-Fluoro-AMT
6-Fluoro-α-methyltryptamine (6-fluoro-AMT, 6F-AMT) is a tryptamine derivative related to compounds such as α-methyltryptamine (AMT) and 5-MeO-AMT which has been sold as a designer drug. Animal tests showed the drug to be somewhat less potent in terms of pharmacological activity than AMT or 5-fluoro-AMT. It produces the head-twitch response, a behavioral proxy of psychedelic-like effects, in rodents. Its for monoamine oxidase A (MAO-A) inhibition is 580 to 1,800nM, compared to 180 to 450nM for 5-fluoro-AMT and 380nM for AMT. 6-Fluoro-AMT was allegedly manufactured and sold from the laboratory operated by Leonard Pickard and Gordon Todd Skinner, who described 6-fluoro-AMT as "a beast". In interviews, Skinner stated that he first began to experiment with 6-fluoro-AMT in the early 1980s by giving it to high school friends. Their experiences made him cautious about the appropriate doses, which he said ranged from 25 to 75mg (Skinner weighed about 250lbs at the time of his own ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
