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5-Fluoro-αET
5-Fluoro-AET, also known as 5-fluoro-α-ethyltryptamine or by the code name PAL-545, is a substituted tryptamine derivative which acts as a serotonin–dopamine releasing agent (SDRA) and as an agonist of the serotonin 5-HT2A receptor. Its values for monoamine release are 36.6nM for serotonin, 5,334nM for norepinephrine, and 150nM for dopamine in rat brain synaptosomes. Its at the serotonin 5-HT2A receptor is 246nM and its at the receptor is 87%. Several close analogues of 5-fluoro-αET, including 5-fluoro-αMT and 5-chloro-αMT, are known to be potent monoamine oxidase inhibitors (MAOIs), specifically of monoamine oxidase A (MAO-A). However, α-ethyltryptamine (αET) is a very weak MAOI. 5-Fluoro-αET has also more recently been assessed, and in contrast to αET, but similarly to drugs like 5-fluoro-αET, was found to be a potent MAOI, with an of 2,480nM. Potent monoamine oxidase inhibition by monoamine releasing agents (MRAs) has been associated with dangerous and somet ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Releasing Agent
A monoamine releasing agent (MRA), or simply monoamine releaser, is a drug that induces the release of one or more monoamine neurotransmitters from the presynaptic neuron into the synapse, leading to an increase in the extracellular concentrations of the neurotransmitters and hence enhanced signaling by those neurotransmitters. The monoamine neurotransmitters include serotonin, norepinephrine, and dopamine; MRAs can induce the release of one or more of these neurotransmitters. MRAs work by reversing the direction of the monoamine transporters (MATs), including the serotonin transporter (SERT), norepinephrine transporter (NET), and/or dopamine transporter (DAT), causing them to promote efflux of non-vesicular cytoplasmic monoamine neurotransmitter rather than reuptake of synaptic monoamine neurotransmitter. Many, but not all MRAs, also reverse the direction of the vesicular monoamine transporter 2 (VMAT2), thereby additionally resulting in efflux of vesicular monoamine neuro ... [...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] |
Serotonin–dopamine Releasing Agent
A serotonin–dopamine releasing agent (SDRA) is a type of drug which induces the synapse, release of serotonin and dopamine in the body and/or brain. SDRAs are rare, as it has proven extremely difficult to dissociate dopamine and norepinephrine release. However, in 2014, the first selective SDRAs, a series of substituted tryptamines, albeit also acting as serotonin receptor agonists, were described. A closely related type of drug is a serotonin–dopamine reuptake inhibitor (SDRI), for instance UWA-101 (α-cyclopropyl-MDMA). Examples of SDRAs A number of tryptamine chemical derivative, derivatives, specifically substituted α-alkyltryptamine, α-alkyltryptamines, have been found to act as SDRAs. One such agent is 5-chloro-αMT (PAL-542), which has been reported as having about 64-fold selectivity for dopamine release over norepinephrine release and about 3-fold selectivity for serotonin release over dopamine release, making it a highly selective and well-balanced SDRA. Anothe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin–norepinephrine–dopamine Releasing Agent
A serotonin–norepinephrine–dopamine releasing agent (SNDRA), also known as a triple releasing agent (TRA), is a type of drug which induces the release of serotonin, norepinephrine/epinephrine, and dopamine in the brain and body. SNDRAs produce euphoriant, entactogen, and psychostimulant effects, and are almost exclusively encountered as recreational drugs. A closely related type of drug is a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI). Examples of SNDRAs Examples of SNDRAs include specific amphetamines such as MDMA, MDA, 4-methylamphetamine, methamphetamine (in high doses), certain substituted benzofurans such as 5-APB and 6-APB, naphthylisopropylamine; cathinones such as mephedrone and methylone; tryptamines such as αMT and αET; along with agents of other chemical classes such as 4,4'-DMAR, and 5-IAI.Bruce E. Blough, Richard Rothman, Antonio Landavazo, Kevin M. Page, Ann Marie Decker. Phenylmorpholines and analogues thereof. US Patent 2013/0 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Oxidase Inhibition
Monoamine oxidase inhibitors (MAOIs) are a class of drugs that inhibit the activity of one or both monoamine oxidase enzymes: monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). They are best known as effective antidepressants, especially for treatment-resistant depression and atypical depression. They are also used to treat panic disorder, social anxiety disorder, Parkinson's disease, and several other disorders. Reversible inhibitors of monoamine oxidase A (RIMAs) are a subclass of MAOIs that selectively and reversibly inhibit the MAO-A enzyme. RIMAs are used clinically in the treatment of depression and dysthymia. Due to their reversibility, they are safer in single-drug overdose than the older, irreversible MAOIs, and weaker in increasing the monoamines important in depressive disorder. RIMAs have not gained widespread market share in the United States. Medical uses MAOIs have been found to be effective in the treatment of panic disorder with agoraphobia, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Toxicity
Toxicity is the degree to which a chemical substance or a particular mixture of substances can damage an organism. Toxicity can refer to the effect on a whole organism, such as an animal, bacteria, bacterium, or plant, as well as the effect on a substructure of the organism, such as a cell (biology), cell (cytotoxicity) or an organ such as the liver (hepatotoxicity). Sometimes the word is more or less synonymous with poison#Poisoning, poisoning in everyday usage. A central concept of toxicology is that the effects of a toxicant are Dose (biochemistry), dose-dependent; even water can lead to water intoxication when taken in too high a dose, whereas for even a very toxic substance such as snake venom there is a dose below which there is no detectable toxic effect. Toxicity is species-specific, making cross-species analysis problematic. Newer paradigms and metrics are evolving to bypass animal testing, while maintaining the concept of toxicity endpoints. Etymology In Ancient G ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-Fluoro-MET
Bretisilocin, also known by its developmental code name GM-2505 and as 5-fluoro-''N''-methyl-''N''-ethyltryptamine (5F-MET or 5-fluoro-MET), is a serotonergic psychedelic of the tryptamine family which is under development for the treatment of major depressive disorder. It is an analogue of dimethyltryptamine (DMT) and is the 5-fluorinated derivative of methylethyltryptamine (MET). Bretisilocin's route of administration is intravenous infusion. The drug acts as a potent and well-balanced serotonin 5-HT2A and 5-HT2C receptor agonist, serotonin 5-HT2B receptor antagonist, and serotonin releasing agent. It produces psychedelic-like effects in animals and similarly produces robust hallucinogenic effects in humans. The duration of bretisilocin is 60 to 90minutes and is intermediate between the durations of DMT and psilocybin. It has been regarded by its developer as an improvement of DMT. Bretisilocin is under development by Gilgamesh Pharmaceuticals. As of March 2024, it ... [...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. 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] |
Matthew J
Matthew may refer to: * Matthew (given name) * Matthew (surname) * ''Matthew'' (album), a 2000 album by rapper Kool Keith * Matthew (elm cultivar), a cultivar of the Chinese Elm ''Ulmus parvifolia'' Christianity * Matthew the Apostle, one of the apostles of Jesus * Gospel of Matthew, a book of the Bible Ships * ''Matthew'' (1497 ship), the ship sailed by John Cabot in 1497, with two 1990s replicas * MV ''Matthew I'', a suspected drug-runner scuttled in 2013 * Interdiction of MV ''Matthew'', a 2023 operation of the Irish military against a 2001 Panamanian cargo ship See also * Matt (given name), the diminutive form of Matthew * Mathew, alternative spelling of Matthew * Matthews (other) * Matthew effect The Matthew effect, sometimes called the Matthew principle or cumulative advantage, is the tendency of individuals to accrue social or economic success in proportion to their initial level of popularity, friends, and wealth. It is sometimes summar ... * Tropic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
