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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] |
List Of Miscellaneous 5-HT2A Receptor Agonists
This is a list of miscellaneous agonists of the serotonin receptor subtype 5-HT2A (and other 5-HT2 subtypes to a varying extent) that fall outside the common structural classes. Most agonists at this receptor are either substituted phenethylamine derivatives from the 2C, DOx and 25-NB groups, or substituted tryptamines and related compounds along with more complex derivatives of these such as lysergamides and iboga-type alkaloids. There are however numerous 5-HT2A receptor agonists which do not fall within any of these groups, some representative examples of which are listed below. Ki and EC50 values vary depending on the assay conditions used and so may not be directly comparable between sources. Many of these compounds have been designed to be non-psychoactive derivatives for medical applications, and it should not be assumed that a compound which acts as a 5-HT2A agonist will necessarily be psychedelic in nature. See also * Partial lysergamide * DPCPX * LY-341,495 * Ro ... [...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] |
LPH-5 (drug)
LPH-5 is a psychedelic discovered by Emil Marcher-Rørsted, Jesper L. Kristensen and Anders A. Jensen at Danish biopharmaceutical company Lophora. It is a conformationally-restricted derivative of the phenethylamine 2C-TFM, also a hallucinogen, and acts as a potent agonist of the 5-HT2A receptor (EC50 = 3.2 nM, Emax = 78%). It shows 10- to 100-fold selectivity for the 5-HT2A receptor over the 5-HT2B and 5-HT2C receptors and, along with related compounds like 25CN-NBOH, is said to be one of the few truly selective 5-HT2A receptor agonists. LPH-5 is expected to avoid the cardiac risks of 5-HT2B receptor activation. LPH-48, an analogue of LPH-5 that likewise acts as a selective serotonin 5-HT2A receptor agonist and psychedelic hallucinogen and shows similar characteristics but has a shorter duration of action, is also under development by Lophora. See also * 2C-B-PP * 2C-TFM * CYB-210010 * DEMPDHPCA * DEMPDHPCA-2C-D * DMBMPP * LPH-48 * OSU-6162 * TCB-2 TCB-2 is a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DMBMPP
DMBMPP, also known as juncosamine or as 2-(2,5-dimethoxy-4-bromobenzyl)-6-(2-methoxyphenyl)piperidine, is a highly selective serotonin 5-HT2A receptor agonist and 2-benzylpiperidine analogue of the serotonergic psychedelic 25B-NBOMe which is used in scientific research. Use Research Despite its uniquely high selectivity for the serotonin 5-HT2A receptor, it has been said that DMBMPP is not widely used as a pharmacological tool in scientific research, presumably due to its chemical synthesis being relatively inaccessible. Consequently, 25CN-NBOH, another highly selective serotonin 5-HT2A receptor agonist, has been proposed as an alternative to DMBMPP for use in scientific research. DMBMPP and 25CN-NBOH are the two most selective serotonin 5-HT2A receptor agonists known as of 2020. Pharmacology The (''S'',''S'')-isomer ((2''S'',6''S'')-DMBMPP) is the most selective agonist for the human serotonin 5-HT2A receptor yet discovered, with a affinity ( Ki) of 2.5nM at the human se ... [...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] |
IHCH-7113
IHCH-7113 is a putative psychedelic drug which acts as an agonist at the 5-HT2A serotonin receptor. It was derived by structural simplification of the 5-HT2A receptor antagonist atypical antipsychotic drug lumateperone along with several related compounds such as IHCH-7079 and IHCH-7086, which were found to be non-hallucinogenic biased 5-HT2A agonists that were active in antidepressant assays but did not produce psychedelic-like responding in mice. IHCH-7113 however produced a head-twitch response comparable to that of DOI or LSD, which was blocked by the 5-HT2A antagonist MDL100907. See also * Efavirenz * IHCH-7079 * IHCH-7086 * Lisuride * Mefloquine * NDTDI * RH-34 * SCHEMBL5334361 * WAY-163909 * Z3517967757 * 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 an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IHCH-7086
IHCH-7086 is a drug which acts as an agonist at the 5-HT2A serotonin receptor. It was derived by structural simplification of the 5-HT2A antagonist atypical antipsychotic drug lumateperone along with several related compounds such as IHCH-7079, which was found to be a non-hallucinogenic biased 5-HT2A agonist that was active in antidepressant assays but did not produce psychedelic-like responding in mice. The related structure IHCH-7113 was found to produce a positive head-twitch response in mice, suggesting likely hallucinogenic activity in humans. See also * Efavirenz * IHCH-7079 * IHCH-7113 * Lisuride * Mefloquine Mefloquine, sold under the brand name Lariam among others, is a medication used to prevent or treat malaria. When used for prevention it is typically started before potential exposure and continued for several weeks after potential exposure. It ... * NDTDI * RH-34 * SCHEMBL5334361 * WAY-163909 * Z3517967757 * Zalsupindole References 2-Methoxy ... [...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] |
Artificial Intelligence
Artificial intelligence (AI) is the capability of computer, computational systems to perform tasks typically associated with human intelligence, such as learning, reasoning, problem-solving, perception, and decision-making. It is a field of research in computer science that develops and studies methods and software that enable machines to machine perception, perceive their environment and use machine learning, learning and intelligence to take actions that maximize their chances of achieving defined goals. High-profile applications of AI include advanced web search engines (e.g., Google Search); recommendation systems (used by YouTube, Amazon (company), Amazon, and Netflix); virtual assistants (e.g., Google Assistant, Siri, and Amazon Alexa, Alexa); autonomous vehicles (e.g., Waymo); Generative artificial intelligence, generative and Computational creativity, creative tools (e.g., ChatGPT and AI art); and Superintelligence, superhuman play and analysis in strategy games (e.g., ... [...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] |
IHCH-7079
IHCH-7079 is a drug which acts as an agonist at the 5-HT2A serotonin receptor. It was derived by structural simplification of the 5-HT2A antagonist atypical antipsychotic drug lumateperone along with several related compounds such as IHCH-7086, which was found to be a non-hallucinogenic biased 5-HT2A agonist that was active in antidepressant assays but did not produce psychedelic-like responding in mice. The related structure IHCH-7113 was found to produce a positive head-twitch response in mice, suggesting likely hallucinogenic activity in humans. See also * AAZ-A-154 * Efavirenz * IHCH-7086 * IHCH-7113 * ITI-333 * Lisuride * Mefloquine Mefloquine, sold under the brand name Lariam among others, is a medication used to prevent or treat malaria. When used for prevention it is typically started before potential exposure and continued for several weeks after potential exposure. It ... * NDTDI * RH-34 * SCHEMBL5334361 * WAY-163909 References 2-Methoxyphenyl co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Racemic Mixture
In chemistry, a racemic mixture or racemate () is a mixture that has equal amounts (50:50) of left- and right-handed enantiomers of a chiral molecule or salt. Racemic mixtures are rare in nature, but many compounds are produced industrially as racemates. History The first known racemic mixture was racemic acid, which Louis Pasteur found to be a mixture of the two enantiomeric isomers of tartaric acid. He manually separated the crystals of a mixture, starting from an aqueous solution of the sodium ammonium salt of racemate tartaric acid. Pasteur benefited from the fact that ammonium tartrate salt gives enantiomeric crystals with distinct crystal forms (at 77 °F). Reasoning from the macroscopic scale down to the molecular, he reckoned that the molecules had to have non-superimposable mirror images. A sample with only a single enantiomer is an ''enantiomerically pure'' or ''enantiopure'' compound. Etymology The word ''racemic'' derives from Latin , meaning pertaining to a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
