Emerging Opportunities and Concerns for Drug Discovery at Serotonin 5-5-HT2B Receptors

5-HT2B receptors have been reported to play an important role at cardiac, intestinal and central levels, as well as in bone marrow formation and growth. In the last decade, 5-HT2B receptors have also gained much attention as new targets in therapeutics, but also as off-targets because their activation along with the inhibition of serotonin transporters plays a significant role in the pathogenesis of 5-HT induced valvulopathy. Taking this into account, the present review focuses on the new therapeutic applications of 5-HT2B receptor ligands as well as on the potential concerns.