Functions of 5HT 2A receptor and its antagonists in the cardiovascular system (original) (raw)

2004, Pharmacology & Therapeutics

The serotonin (5-hydroxytryptamine, 5-HT) receptors have conventionally been divided into seven subfamilies, most of which have several subtypes. Among them, 5-HT 2A receptor is associated with the contraction of vascular smooth muscle, platelet aggregation and thrombus formation and coronary artery spasms. Accordingly, selective 5-HT 2A antagonists may have potential in the treatment of cardiovascular diseases. Sarpogrelate, a selective 5-HT 2A antagonist, has been introduced clinically as a therapeutic agent for the treatment of ischemic diseases associated with thrombosis. Molecular modeling studies also suggest that sarpogrelate is a 5-HT 2A selective antagonist and is likely to have pharmacological effects beneficial in the treatment of cardiovascular diseases. This review describes the above findings as well as the signaling linkages of the 5-HT 2A receptors and the mode of agonist binding to 5-HT 2A receptor using data derived from molecular modeling and site-directed mutagenesis.