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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Pharmacophore Models for Metabotropic 5-HT Receptor Ligands

Author(s): Andrzej J. Bojarski

Volume 6, Issue 18, 2006

Page: [2005 - 2026] Pages: 22

DOI: 10.2174/156802606778522186

Price: $65


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.

Keywords: 5-HT1 receptors, 5-HT2 receptors, 5-HT4 receptors, 5-HT6 receptors, 5-HT7 receptors, pharmacophore models, 3-D QSAR

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