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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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 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.[1]


  1. Functions of 5-HT2A receptor and its antagonists in the cardiovascular system. Nagatomo, T., Rashid, M., Abul Muntasir, H., Komiyama, T. Pharmacol. Ther. (2004) [Pubmed]
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