Receptor:5-HT2B
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5-HT2B is a G protein-coupled serotonin receptor of the 5-HT2 family, coupling through Gq/11 proteins and phospholipase C.[1] It is expressed in the cardiovascular system, the gut, and parts of the central nervous system. Sustained agonism of 5-HT2B receptors on cardiac valve fibroblasts drives proliferative valvular heart disease, the mechanism behind the valvulopathy associated with fenfluramine, pergolide, and other 5-HT2B agonists; screening out 5-HT2B activity is now a standard step in drug development.[2]
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References
- ↑ Hoyer D, Hannon JP, Martin GR. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacology, Biochemistry, and Behavior. 2002 Apr;71(4):533-554. PMID: 11888546.
- ↑ Roth BL. Drugs and valvular heart disease. New England Journal of Medicine. 2007 Jan 4;356(1):6-9. PMID: 17202450.