Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 6, Issue 18, Pages 2005-2026Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/156802606778522186
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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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-HTIE- and 5-HT(5A)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.
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