Review of 5-HT4R ligands: state of art and clinical applications.
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.
Bureau
Ronan
R
Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN) UPRES EA 4258, FR CNRS 3038, Université de Caen, Boulevard Becquerel, 14032 Caen, France. ronan.bureau@unicaen.fr
Boulouard
Michel
M
Dauphin
François
F
Lezoualc'h
Frank
F
Rault
Sylvain
S
D006801:Humans; D008024:Ligands; D044422:Receptors, Serotonin, 5-HT4 / Q000378:metabolism; D058828:Serotonin 5-HT4 Receptor Agonists; D058832:Serotonin 5-HT4 Receptor Antagonists; D012702:Serotonin Antagonists / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D017366:Serotonin Receptor Agonists / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D013329:Structure-Activity Relationship
D008024:Ligands; D058828:Serotonin 5-HT4 Receptor Agonists; D058832:Serotonin 5-HT4 Receptor Antagonists; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; D044422:Receptors, Serotonin, 5-HT4