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Bespoke library docking for 5-HT2A receptor agonists with antidepressant activity Nature doi:10.1038/s41586-022-05258-z DNA编码库和虚拟筛选是目前进行大规模药物筛选的重要手段,然而,由于可拓展的化学空间过于庞大,因此一些人们较少关注的化学结构必定会在数据集中缺失或不足。例如本篇文章focus的骨架四氢吡啶THP。
1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2Areceptor agonists. McLean et al. J.Med.Chem., 2006;49:5794 The serotonin 5-HT2Areceptor agonist TCB-2: a behavioral and neurophysiological analysis. ...
[1].Meghan J. Orr, et al. Highly Potent Serotonin 5-HT2 Receptor Agonists Inspired by Heteroyohimbine Natural Products. 5-HT2A receptor agonist-2物理化学性质 分子式C20H21ClN2O3 分子量372.85 [5-HT2A receptor agonist-2]化源网提供5-HT2A receptor agonist-2CAS号528525-37-3,5-HT2A recept...
激动剂(AGONISTS)是指与受体(例如5-HT2A受体)相互作用且激活所述受体的半族,且触发所述受体的生理学或药理学反应特征。例如,当半族结合至受体时会激活胞内反应,或增强GTP与膜的结合。本文所使用的氨基酸缩写如表1所示表1术语拮抗剂(ANTAGONISTS)是指在与激动剂相同的部位(例如,内源性配体)竞争性结合受体的半...
Activation of 5-HT 2A receptors using agonists at surprisingly low concentrations was shown to potently inhibit TNF-α-induced inflammation in multiple cell types. Significantly, proinflammatory markers were also inhibited by the agonist, (R)-DOI, even many hours after treatment with TNF-α. With ...
Storage: Desiccate at RT CAS No: 1539266-32-4 The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. Tocris products are intended for laboratory research use only, unless stated otherwise. ...
5-HT2Aagonists such as serotonin and DOI, or dopamine—a partial agonist were shown to activate the receptor and cause an intracellular Ca2+rise in both Rat2ASB1 and Hu2AAB1 cells11,12,13,15. We report here that activation of 5-HT2Aby these ligands also results in increased adhesion of...
Further, pretreatment of rats in vivo with melatonin and related agonists reduced the cortical PI hydrolysis response to the 5-HT2A agonist alpha methyl-5-HT but did not alter cortical 5-HT2A receptor density. The present data support an interaction between melatonin and 5-HT2A receptors in ...
Here, we aimed to assess tolerance and cross-tolerance to HTR elicited by psychedelic and nonpsychedelic serotonin 2A receptor (5-HT2AR) agonists in mice. We show that repeated (4 days) administration of the psychedelic 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) induced a ...