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RS134-49
RS134-49 is a tetrahydropyridine derivative related to psychedelic tryptamines which acts as a 5-HT2A receptor agonist, with a 5-HT2A Ki of 11.5nM and an EC50 of 22nM. It is a biased agonist selective for activation of the Gq coupled signalling pathway with weaker activation of the β-arrestin 2 coupled pathway, but shows a more balanced profile than related compounds such as (R)-69. See also * Cyclized tryptamine * RU-28253 * 4-Methyl-α-methyltryptamine * 4-Methyl-α-ethyltryptamine * CP-94253 * RU-24,969 * SN-22 SN-22 is a chemical compound which acts as a moderately selective agonist at the 5-HT2 family of serotonin receptors, with a Ki of 19 nM at 5-HT2 subtypes versus 514 nM at 5-HT1A receptors. Many related derivatives are known, most of ... * VU6067416 References Designer drugs N-Monoalkyltryptamines Tetrahydropyridinylindoles {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclized 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] |
RU-28253
RU-28253 is a non-selective serotonin receptor agonist of the tryptamine and 5-methoxytryptamine families. It is a tetrahydropyridylindole and a conformationally constrained analogue of 5-MeO-DMT. The drug shows high affinity for the serotonin 5-HT1A receptor (Ki = 5.7nM) and lower affinity for the serotonin 5-HT2A receptor (Ki = 230nM). Its affinities for these receptors were higher than those of dimethyltryptamine (DMT). RU-28253 is described as a potent agonist of the serotonin 5-HT1 and 5-HT2 receptors, including of the serotonin 5-HT1B receptor, and is also an agonist of the serotonin 5-HT4 receptor. RU-28253 was first described in the scientific literature by 1983. See also * Cyclized tryptamine * VU6067416 * RS134-49 * (''R'')-69 * RU-24,969 * EMD-386088 * SN-22 * MPMI * Pyr-T Pyr-T, also known as ''N'',''N''-tetramethylenetryptamine or as 3-(2-pyrrolidinoethyl)indole, is a lesser-known serotonin receptor modulator of the tryptamine family. It is the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-Methyl-α-methyltryptamine
4-Methyl-α-methyltryptamine (4-Me-αMT or 4-Me-AMT), also known as 4,α-dimethyltryptamine (4,α-DMT) and by its developmental code name MP-809, is an experimental antidepressant of the tryptamine and α-alkyltryptamine families. It is closely structurally related to serotonergic psychedelics and entactogens like α-methyltryptamine (αMT) and α-ethyltryptamine (αET). 4-Me-αMT was investigated as an antidepressant by Sandoz in Canada in the early 1960s, although it was never marketed. Dosage and effects It is active at a dosage of 20 to 60mg orally in humans, though described as being an antidepressant rather than a hallucinogen. It was found to be effective as an antidepressant in preliminary clinical studies. Alexander Shulgin has said that 4-Me-αMT produced some feelings of unreality at a dose of 20mg, as well as skin flushing, muscle tightness, and mydriasis. However, he has said that it could not be called a hallucinogen at assessed doses and has listed the hallu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
VU6067416
VU6067416 is an indazole derivative which acts as an agonist for the 5-HT2 family of serotonin receptors. It is a potent full agonist at 5-HT2B, and has slightly lower affinity and partial agonist effects at 5-HT2A and 5-HT2C, though some related compounds have improved selectivity for 5-HT2A. See also * RU-28253 * (''R'')-69 * 6-APB * BW-723C86 * RS134-49 * VER-3323 VER-3323 is a drug which acts as a selective agonist for both the 5-HT2B receptor, 5-HT2B and 5-HT2C receptor, 5-HT2C serotonin Receptor (biochemistry), receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT ... References 5-HT2B agonists Serotonin receptor agonists Indazoles Bromoarenes Tetrahydropyridines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RU-24,969
RU-24,969 is a serotonin receptor modulator related to 5-MeO-DMT which is used in scientific research. It is a selective agonist of the serotonin 5-HT1A and 5-HT1B receptors, with 5-fold preference for the latter receptor over the former. In studies, its affinities (Ki) were 2nM for the serotonin 5-HT1 receptor, 5nM for the serotonin 5-HT1A receptor, 4nM for the serotonin 5-HT1B receptor, 780 to 1,000nM for the serotonin 5-HT2 receptor, and 400nM for the serotonin 5-HT2C receptor. It also has affinity for the serotonin 5-HT5A, 5-HT5B, and 5-HT7 receptors. The drug produces MDMA-like locomotor hyperactivity in animals and this is thought to be mediated by activation of both serotonin 5-HT1A and 5-HT1B receptors. As with other serotonin 5-HT1B receptor agonists such as CP-94,253, RU-24,969 has also been found to increase the reinforcing properties of cocaine in animals, suggesting a role for serotonin 5-HT1B receptors in cocaine addiction as well. RU-24,969 was first de ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-Methyl-α-ethyltryptamine
4-Methyl-α-ethyltryptamine (4-Me-αET) is a drug of the tryptamine class. It is a designer drug and is sold online as a "research chemical". Legality 4-Methyl-α-ethyltryptamine is illegal in Singapore. See also * 4-Methyl-αMT * 5-Fluoro-αET * 7-Chloro-αMT * 7-Methyl-αET * RS134-49 RS134-49 is a tetrahydropyridine derivative related to psychedelic tryptamines which acts as a 5-HT2A receptor agonist, with a 5-HT2A Ki of 11.5nM and an EC50 of 22nM. It is a biased agonist selective for activation of the Gq coupled signalling ... References Alpha-Alkyltryptamines Methyl compounds {{Psychoactive-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Designer Drugs
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union, Australia, and New Zealand, as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these designer drugs were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human tr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SN-22
SN-22 is a chemical compound which acts as a moderately selective agonist at the 5-HT2 family of serotonin receptors, with a Ki of 19 nM at 5-HT2 subtypes versus 514 nM at 5-HT1A receptors. Many related derivatives are known, most of which are ligands for 5-HT1A, 5-HT6 or dopamine D2 receptors or show SSRI activity. See also * BRL-54443 * LY-334370 * LY-367,265 * MPMI * MPTP * Naratriptan * N,N-Dimethyltryptamine * RU-24969 * Sertindole Sertindole, sold under the brand name Serdolect among others, is an antipsychotic medication. Sertindole was developed by the Danish pharmaceutical company Lundbeck and marketed under license by Abbott Labs. Like other atypical antipsychotics, ... References Piperidinylindoles Serotonin receptor agonists {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CP-94253
CP-94253 is a drug which acts as a potent and selective serotonin 5-HT1B receptor 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 ..., with approximately 25× and 40× selectivity over the closely related 5-HT1D and 5-HT1A receptors. It has a range of behavioral effects, based on animal testing. The effects include the following: promoting wakefulness by increasing dopamine release in the brain; reducing food intake and promoting satiety; enhancing the reinforcing effects of cocaine; and possible antidepressant effects. A recent study found that "Regardless of sex, CP94253 decreased cocaine intake after abstinence and during resumption of SA elf-administrationand decreased cue reactivity" suggesting that agonism of the inhibitory 5-HT2B receptors may diminish the cognitive ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tetrahydropyridine
Tetrahydropyridines (or piperideines) are heterocycles with the formula . Three isomers exist, which differ by the location of the double bond. None of the parent species occur widely, so they are mainly of theoretical interest. Although the parent tetrahydropyridines are rare, many substituted tetrahydropyridines are known. Preparation and occurrence 2,3,4,5-Tetrahydropyridine, a colorless liquid, is commercially available. It is an imine. Illustrating another isomer of tetrahydropyridine, 6-acetyl-2,3,4,5-tetrahydropyridine occurs naturally. Partial reduction of pyridinium salts gives N-alkyltetrahydropyridines. Treatment of N-methylpyridinium with borohydride Borohydride refers to the anion , which is also called tetrahydroborate or more commonly tetrahydrobiopterin, and its salts. Borohydride or hydroborate is also the term used for compounds containing , where ''n'' is an integer from 0 to 3, for ex ... reagents gives 1-methyl-1,2,3,6-tetrahydropyridine. A modified ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Psychedelic
Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary mental states (known as psychedelic experiences or "trips") and a perceived "expansion of consciousness". Also referred to as classic hallucinogens or serotonergic hallucinogens, the term ''psychedelic'' is sometimes used more broadly to include various other types of hallucinogens as well, such as those which are atypical or adjacent to psychedelia like salvia and MDMA, respectively. Classic psychedelics generally cause specific psychological, visual, and auditory changes, and oftentimes a substantially altered state of consciousness. They have had the largest influence on science and culture, and include mescaline, LSD, psilocybin, and DMT. There are a large number of both naturally occurring and synthetic serotonergic psychedelics. Most psychedelic drugs fall into one of the three families of chemical compounds: tryptamines, phenethylamines, or lysergamides. They produce ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
(R)-69
(''R'')-69 (3IQ) is a tetrahydropyridine derivative which acts as a 5-HT2A receptor agonist, with 4.6-fold selectivity over 5-HT2B and 49-fold selectivity over 5-HT2C. It has a 5-HT2A Ki of 680 nM and an EC50 of 41 nM. (''R'')-69 is a biased agonist selective for activation of the Gq coupled signalling pathway, with much weaker activation of the β-arrestin 2 coupled pathway. In animal studies it produces antidepressant-like activity but without producing the head-twitch response associated with psychedelic effects. See also * 25N-N1-Nap * RU-24969 * RU-28253 * SN-22 * VU6067416 * Z3517967757 * Zalsupindole * Ultra-large-scale docking Ultra-large-scale docking, sometimes abbreviated as Ultra-LSD, is an ultra-large-scale approach to protein–ligand docking and virtual screening. It employs molecular docking campaigns against libraries of millions or billions of chemical compound ... References Designer drugs Non-hallucinogenic 5-HT2A receptor agonists Pyrrolo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
