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Pharmacophore Models for Metabotropic 5-HT Receptor Ligands

[ Vol. 6 , Issue. 18 ]

Author(s):

Andrzej J. Bojarski   Pages 2005 - 2026 ( 22 )

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.

Keywords:

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

Affiliation:

Department of Medicinal Chemistry Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, 31-343 Kraków, Poland.



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