Title: Pharmacophore Models for Metabotropic 5-HT Receptor Ligands
Volume: 6
Issue: 18
Author(s): Andrzej J. Bojarski
Affiliation:
Keywords:
5-HT1 receptors, 5-HT2 receptors, 5-HT4 receptors, 5-HT6 receptors, 5-HT7 receptors, pharmacophore models, 3-D QSAR
Abstract: 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-HT5ARs 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.
