Review of 5-HT4R ligands: state of art and clinical applications

Curr Top Med Chem. 2010;10(5):527-53. doi: 10.2174/156802610791111551.

Abstract

This article reviews the medicinal implications of 5-HT(4)R in the peripheral and central nervous systems, based on data from two hundred bibliographic references. An exhaustive compilation of molecules reported to be antagonists or agonists for 5-HT(4)R is presented, including chemical structures, binding properties and pharmacological profiles. In the last part of the review, some key concepts concerning structure-activity relationships are highlighted.

Publication types

  • Review

MeSH terms

  • Humans
  • Ligands
  • Receptors, Serotonin, 5-HT4 / metabolism
  • Serotonin 5-HT4 Receptor Agonists*
  • Serotonin 5-HT4 Receptor Antagonists*
  • Serotonin Antagonists / chemistry
  • Serotonin Antagonists / pharmacology*
  • Serotonin Antagonists / therapeutic use*
  • Serotonin Receptor Agonists / chemistry
  • Serotonin Receptor Agonists / pharmacology*
  • Serotonin Receptor Agonists / therapeutic use*
  • Structure-Activity Relationship

Substances

  • Ligands
  • Serotonin 5-HT4 Receptor Agonists
  • Serotonin 5-HT4 Receptor Antagonists
  • Serotonin Antagonists
  • Serotonin Receptor Agonists
  • Receptors, Serotonin, 5-HT4