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(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] |
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 compounds to discover new drugs. The virtual screening phase identifies potential high-affinity ligands and then selected promising compounds are synthesized and further evaluated in the laboratory, including in terms of properties like functional activity and selectivity. The purpose of Ultra-LSD is to discover novel chemical scaffolds for ligands of molecular targets. Ultra-LSD was developed by Brian Shoichet and John Irwin at the University of California, San Francisco, Bryan L. Roth at University of North Carolina at Chapel Hill, and other colleagues, and was first described in 2019. The researchers have conducted Ultra-LSD campaigns against a variety of targets, including the serotonin 5-HT2A receptor, the melatonin receptors, the dopami ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A Receptor
The 5-HT2A receptor is a subtype of the 5-HT2 receptor, 5-HT2 receptor that belongs to the serotonin receptor family and functions as a GPCR, G protein-coupled receptor (GPCR). It is a cell surface receptor that activates multiple intracellular signalling cascades. Like all 5-HT2 receptors, the 5-HT2A receptor is coupled to the Gq protein, Gq/G11 signaling pathway. It is the primary excitatory receptor subtype among the serotonin-responsive GPCRs. The 5-HT2A receptor was initially noted for its central role as the primary target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. It later regained research prominence when found to mediate, at least in part, the effects of many antipsychotic drugs, particularly atypical antipsychotic, atypical antipsychotics. Downregulation of post-synaptic 5-HT2A receptors is an adaptive response triggered by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Elevated 5-HT2A ... [...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] |
Zalsupindole
Zalsupindole,https://iris.who.int/bitstream/handle/10665/380497/9789240107038-eng.pdf "zalsupindolum zalsupindole (2R)-1-(5-methoxy-1H-indol-1-yl)-N,N-dimethylpropan-2-amine antidepressant" also known by its developmental code names DLX-001 and AAZ-A-154 and as (''R'')-5-methoxy-''N'',''N''-dimethyl-α-methylisotryptamine, is a novel isotryptamine derivative which acts as a serotonin 5-HT2A receptor agonist discovered and synthesized by the lab of Professor David E. Olson at the University of California, Davis. It is being developed for the treatment of major depressive disorder and other central nervous system disorders. Pharmacology Animal studies suggest that it produces antidepressant effects without the psychedelic action typical of drugs from this class. In tests, zalsupindole had antidepressant-like effects in mice without causing the head-twitch response linked to hallucinogenic effects. Due to the rapidly-induced and enduring neuroplasticity, zalsupindole is a member ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Z3517967757
Z3517967757, or simply Z7757, is a piperidine chemical derivative, derivative which acts as an agonist at the 5-HT2 receptor, 5-HT2 family of serotonin Receptor (biochemistry), receptors, first reported in 2024. It can also be viewed as a ring (chemistry), ring-restrained substituted phenethylamine, phenethylamine. It has strongest pharmacological activity, activity at the 5-HT2A receptor, 5-HT2A receptor and lower affinity (pharmacology), affinity at the 5-HT2B receptor, 5-HT2B and 5-HT2C receptor, 5-HT2C receptors. However, it has been reported to have excellent binding selectivity, selectivity for the 5-HT2A receptor, with no agonistic activity at the 5-HT2B and 5-HT2C receptors. The drug was developed using ''in silico'' modelling to docking (molecular), dock a large chemical library, library of compounds against a 5-HT2A receptor model generated by the artificial intelligence program AlphaFold, and then chemical synthesis, synthesised and tested in the laboratory to confirm a ... [...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] |
25N-N1-Nap
25N-N1-Nap is a phenethylamine derivative from the 25-NB class, which acts as a potent agonist at the 5-HT2A receptor with weaker activity at 5-HT2B and 5-HT2C. 25N-N1-Nap is a biased agonist, producing robust activation of 5-HT2A coupled signaling pathways mediated by beta arrestin 2, but with little or no activation of pathways mediated via Gq. In animal studies it produces antipsychotic-like effects but without producing the head-twitch response associated with psychedelic activity. See also * 25N-NBOMe (NBOMe-2C-N) * 25N-NBPh * 6-Fluoro-DET * Lisuride * (''R'')-69 * RS130-180 * Zalsupindole Zalsupindole,https://iris.who.int/bitstream/handle/10665/380497/9789240107038-eng.pdf "zalsupindolum zalsupindole (2R)-1-(5-methoxy-1H-indol-1-yl)-N,N-dimethylpropan-2-amine antidepressant" also known by its developmental code names DLX-001 and ... References 25-NB (psychedelics) Methoxy compounds Naphthalenes Nitrobenzene derivatives Non-hallucinogenic 5-HT2A rece ... [...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] |
RU-24969
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 d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2B Receptor
5-Hydroxytryptamine receptor 2B (5-HT2B) also known as serotonin receptor 2B is a protein that in humans is encoded by the ''HTR2B'' gene. 5-HT2B is a member of the 5-HT2 receptor, 5-HT2 receptor family that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). Like all 5-HT2 receptors, the 5-HT2B receptor is Gq protein, Gq/G11-protein coupled, leading to downstream activation of phospholipase C. Tissue distribution and function First discovered in the stomach of rats, 5-HT2B was challenging to characterize initially because of its structural similarity to the other 5-HT2 receptors, particularly 5-HT2C. The 5-HT2 receptors (of which the 5-HT2B receptor is a subtype) mediate many of the central and peripheral physiologic functions of serotonin. Cardiovascular effects include contraction of blood vessels and shape changes in platelets; central nervous system (CNS) effects include neuronal sensitization to tactile stimuli and mediation of some of the effects of halluci ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
