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C-DMT
C-DMT, also known as ''N'',''N''-dimethyl-2-(3''H''-inden-1-yl)ethylamine, is a serotonin receptor agonist and a 3- indenyl ethylamine derivative. It is an analogue and bioisostere of the tryptamine psychedelic ''N'',''N''-dimethyltryptamine (DMT) in which the indole ring has been replaced with an indene ring. Put another way, the nitrogen atom in the indole ring of DMT has been replaced with a carbon atom to make an indene ring. The drug shows similar affinity for and potency in activating the serotonin receptors in the rat fundus strip compared to DMT. These findings suggest that the indole-ring nitrogen atom of tryptamines is not essential for serotonergic activity. On the other hand however, C-DMT showed dramatically lower affinities for the serotonin 5-HT1E and 5-HT1F receptors compared to DMT (8- and 65-fold, respectively). The effects of C-DMT in animals and humans, and whether it produces hallucinogenic effects, do not appear to be known. See also * isoDMT * ... [...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] |
3-APBT
3-APBT (former developmental code name SKF-6678), also known as 3-(2-aminopropyl)benzo �hiophene, is a monoamine releasing agent and serotonin receptor agonist of the benzothiophene group. It is an analogue of α-methyltryptamine (AMT) in which the indole ring has been replaced with a benzothiophene ring. The drug acts as a potent and well-balanced serotonin–norepinephrine–dopamine releasing agent (SNDRA). It is also a full agonist of the serotonin 5-HT2 receptors, including of the serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptors. 3-APBT produces the head-twitch response, a behavioral proxy of psychedelic effects, in rodents. It does not stimulate locomotor activity in rodents, suggesting that it does not possess stimulant-type effects. The drug has been reported be a weak monoamine oxidase inhibitor (MAOI), specifically of monoamine oxidase A (MAO-A) ( = 16,200nM). 3-APBT was developed by Smith, Kline & French (SKF) as a potential pharmaceutical drug in the late 1950s. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dimemebfe
Dimemebfe (5-MeO-BFE) is a recreational drug and research chemical. It acts as an agonist for the 5-HT1A and 5-HT2 family of serotonin receptors. It is related in structure to the psychedelic tryptamine derivative 5-MeO-DMT, but with the indole nitrogen replaced by oxygen, making dimemebfe a benzofuran derivative. It is several times less potent as a serotonin agonist than 5-MeO-DMT and with relatively more activity at 5-HT1A, but still shows strongest effects at the 5-HT2 family of receptors. Legal status Dimemebfe is a Schedule I controlled substance in the US state of Alabama. See also * 5-MeO-DiBF 5-MeO-DiBF is a psychedelic that has been sold online as a designer drug and was first definitively identified in December 2015 by a forensic laboratory in Slovenia. It is thought to act as an agonist for the 5-HT1A and 5-HT2 family of seroto ... * C-DMT * 5-APB References Benzofuranethanamines Designer drugs Serotonin receptor agonists Benzofuran ethers ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2ZEDMA
TACT908, also known as -(indolizin-1-yl)ethylimethylamine (2ZEDMA), is a serotonin receptor agonist which is under development for the treatment of cluster headaches. It is an positional isomer of the famous tryptamine serotonergic psychedelic ''N'',''N''-dimethyltryptamine (DMT) in which the indole ring has been replaced with an indolizine ring. The drug acts as a serotonin 5-HT1B and 5-HT2A receptor agonist. Its at the serotonin 5-HT2A receptor is 52nM ( ≈ 30% of that of serotonin) and its at the serotonin 5-HT1B receptor is 143nM. TACT908 is said to be a non-hallucinogenic serotonin 5-HT2A receptor agonist. It showed little or no activity at 45other screened targets, including the serotonin 5-HT1A, 5-HT2B, and 5-HT3 receptors as well as the monoamine transporters (MATs). Other serotonin receptors besides the preceding, such as the serotonin 5-HT2C receptor, were not assessed. The drug was a weak monoamine oxidase inhibitor (MAOI), specifically of monoamine oxidase A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IsoDMT
isoDMT, also known as ''N'',''N''-dimethylisotryptamine, is a putatively non-hallucinogenic serotonin 5-HT2A receptor agonist and psychoplastogen of the isotryptamine group. It is the isotryptamine homologue of dimethyltryptamine (DMT), a more well-known serotonergic psychedelic of the tryptamine family, and represents a small structural modification of DMT. Pharmacology The drug does not produce hallucinogen-like stimulus generalization in animal drug discrimination tests and similarly does not produce the head-twitch response, an animal behavioral proxy of psychedelic-like effects. As such, it is not expected to be hallucinogenic in humans. However, isoDMT retains significant activity at the serotonin 5-HT2 receptors and shows psychoplastogenic effects comparable to those of serotonergic psychedelics in preclinical research. Its affinities (Ki) for the serotonin 5-HT2 receptors have been reported to be 600–650nM for 5-HT2A and 720nM at 5-HT2C. Analogs Several deriv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Agonist
A serotonin receptor agonist is an agonist of one or more serotonin receptors. They activate serotonin receptors in a manner similar to that of serotonin (5-hydroxytryptamine; 5-HT), a neurotransmitter and hormone and the endogenous ligand of the serotonin receptors. Non-selective agonists Serotonergic psychedelics such as tryptamines (e.g., psilocybin, psilocin, , 5-MeO-DMT, bufotenin), lysergamides (e.g., , ergine ()), phenethylamines (e.g., mescaline, 2C-B, 25I-NBOMe), and amphetamines (e.g., , ) are non-selective agonists of serotonin receptors. Their hallucinogenic effects are specifically mediated by activation of the 5-HT2A receptor. Drugs that increase extracellular serotonin levels such as serotonin reuptake inhibitors (e.g., fluoxetine, venlafaxine), serotonin releasing agents (e.g., fenfluramine, ), and monoamine oxidase inhibitors (e.g., phenelzine, moclobemide) are indirect non-selective serotonin receptor agonists. They are used variously as antidepressant ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Affinity (pharmacology)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition o ... [...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] |
Hallucinogen
Hallucinogens, also known as psychedelics, entheogens, or historically as psychotomimetics, are a large and diverse class of psychoactive drugs that can produce altered states of consciousness characterized by major alterations in thought, mood, and perception as well as other changes. Hallucinogens are often categorized as either being psychedelics, dissociatives, or deliriants, but not all hallucinogens fall into these three classes. Examples of hallucinogens include psychedelics or serotonin 5-HT2A receptor agonists like LSD, psilocybin, mescaline, and DMT; dissociatives or NMDA receptor antagonists like ketamine, PCP, DXM, and nitrous oxide; deliriants or antimuscarinics like scopolamine and diphenhydramine; cannabinoids or cannabinoid CB1 receptor agonists like THC, nabilone, and JWH-018; κ-opioid receptor agonists like salvinorin A and pentazocine; GABAA receptor agonists like muscimol and gaboxadol; and oneirogens like ibogaine and harmaline, a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1F Receptor
5-hydroxytryptamine (serotonin) receptor 1F, also known as HTR1F is a 5-HT1 receptor protein and also denotes the human gene encoding it. Agonists * 5-''n''-Butyryloxy-DMT: >60-fold selectivity versus 5-HT1E receptor * BRL-54443 - mixed 5-HT1E/1F agonist * Eletriptan - mixed 5-HT1B/1D/1E/1F/2B/7 agonist * LY-334,370 - as well as related benzamides * LY-344,864 (N- 3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl4-fluorobenzamide) * Naratriptan - mixed 5-HT1B/1D/1F agonist * Lasmiditan - selective 5-HT1F agonist, a first-in-class ditan molecule Antagonists MLS000756415 See also * 5-HT1 receptor * 5-HT receptor 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 nervous system, central and peripheral nervous systems ... References Further reading * * * * * * * * External links * * Sero ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1E Receptor
5-hydroxytryptamine (serotonin) 1E receptor (5-HT1E) is a highly expressed human G-protein coupled receptor that belongs to the 5-HT1 receptor family (Gi-coupled serotonin receptor). The human gene is denoted as HTR1E. Function The function of the 5-HT1E receptor is unknown due to the lack of selective pharmacological tools, specific antibodies, and permissive animal models. The 5-HT1E receptor gene lacks polymorphisms amongst humans (few mutations), indicating a high degree of evolutionary conservation of genetic sequence, which suggests that the 5-HT1E receptor has an important physiological role in humans. It is hypothesized that the 5-HT1E receptor is involved in the regulation of memory in humans due to the high abundance of receptors in the frontal cortex, hippocampus, and olfactory bulb, all of which are regions of the brain integral to memory regulation. This receptor is unique among the serotonin receptors in that it is not known to be expressed by rats or mouse spec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin
Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, memory, and physiological processes such as vomiting and vasoconstriction. In the CNS, serotonin regulates mood, appetite, and sleep. Most of the body's serotonin—about 90%—is synthesized in the gastrointestinal tract by enterochromaffin cells, where it regulates intestinal movements. It is also produced in smaller amounts in the brainstem's raphe nuclei, the skin's Merkel cells, pulmonary neuroendocrine cells, and taste receptor cells of the tongue. Once secreted, serotonin is taken up by platelets in the blood, which release it during clotting to promote vasoconstriction and platelet aggregation. Around 8% of the body's serotonin is stored in platelets, and 1–2% is found in the CNS. Serotonin acts as both a vasoconstrictor and vas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
