Pharmacophore models for metabotropic 5-HT receptor ligands

Curr Top Med Chem. 2006;6(18):2005-26. doi: 10.2174/156802606778522186.

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-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.

Publication types

  • Review

MeSH terms

  • Ligands
  • Molecular Structure
  • Receptors, Serotonin / metabolism*
  • Serotonin Antagonists / chemistry*
  • Serotonin Antagonists / pharmacology*
  • Serotonin Receptor Agonists / chemistry*
  • Serotonin Receptor Agonists / pharmacology*
  • Structure-Activity Relationship

Substances

  • Ligands
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Serotonin Receptor Agonists