AI Article Synopsis
- - The serotonin receptors, particularly the 5-HT(2A) subtype, play a role in various cardiovascular functions, including factors like blood vessel contraction and blood clot formation.
- - Selective antagonists like sarpogrelate target the 5-HT(2A) receptors and may offer new treatment options for cardiovascular diseases, particularly those related to thrombosis.
- - This review discusses the molecular mechanisms of 5-HT(2A) receptors, including how agonists bind to them, supported by molecular modeling studies and experimental techniques like site-directed mutagenesis.
Article Abstract
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.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.pharmthera.2004.08.005 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!