Bojarski Andrzej J
Department of Medicinal Chemistry Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31-343 Kraków, Poland.
Curr Top Med Chem. 2006;6(18):2005-26. doi: 10.2174/156802606778522186.
An overview of pharmacophore models, developed for different subtypes of serotonin receptors belonging to the GPCR family, is presented. Starting with early models for 5-HT1A and 5-HT2 receptor ligands, and ending with the latest ones for 5-HT6- and 5-HT7 receptors, as many as fifty others are briefly summarized. No models have been developed for 5-HT1F-, 5-HT2B- and 5-HT5B receptor ligands, and in the case of 5-HT1E- and 5-HT5A Rs only single pilot studies with non-selective tryptamine derivatives are reported. For all the other subtypes of 5-HTRs, various pharmacophore hypotheses--either qualitative and/or quantitative--are characterized by sets of ligands used for their generation, a templates for alignment, the computational methods applied and, eventually, interfeature distances and/or statistical results--if available.
本文概述了针对属于GPCR家族的不同亚型血清素受体开发的药效团模型。从5-HT1A和5-HT2受体配体的早期模型开始，到5-HT6和5-HT7受体的最新模型结束，简要总结了多达五十个其他模型。尚未开发出针对5-HT1F、5-HT2B和5-HT5B受体配体的模型，对于5-HT1E和5-HT5A受体，仅报道了使用非选择性色胺衍生物的单一试点研究。对于5-HTRs的所有其他亚型，各种药效团假设（定性和/或定量）的特征在于用于生成它们的配体集、比对模板、应用的计算方法，以及最终的特征间距离和/或统计结果（如果可用）。
