Functions of 5-HT2A receptor and its antagonists in the cardiovascular system

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 arter...

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Bibliographic Details
Published in:Pharmacology & therapeutics (Oxford) 2004-10, Vol.104 (1), p.59-81
Main Authors: Nagatomo, Takafumi, Rashid, Mamunur, Abul Muntasir, Habib, Komiyama, Tadazumi
Format: Article
Language:English
Subjects:
Animals
Cardiovascular Diseases - drug therapy
Cardiovascular Diseases - metabolism
Cardiovascular System - drug effects
Cardiovascular System - metabolism
Humans
Protein Binding - drug effects
Protein Binding - physiology
Receptor, Serotonin, 5-HT2A - physiology
Serotonin 5-HT2 Receptor Antagonists
Serotonin Antagonists - chemistry
Serotonin Antagonists - pharmacology
Serotonin Antagonists - therapeutic use
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Summary: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.
ISSN:0163-7258
DOI:10.1016/j.pharmthera.2004.08.005