5-HT2B Receptor Ligands

Serotonin 5-HT_2B receptors, previously known as 5-HT_2F receptors, are located primarily in the stomach fundus, uterus, vascular endothelial and vascular and GI smooth muscle, with limited distribution in the brain. The functions of 5-HT_2B receptors include regulation of differentiation and proliferation of the embryonic and adult heart, gastrointestinal contraction and endothelium-dependent relaxation. Furthermore, 5-HT_2B receptor knockout mice exhibit gross heart defects and 5-HT_2B overexpression leads to ventricular hypertrophy. The human 5-HT_2B receptor gene has been localized to chromosome 2 (2q36.3-q37.1).