Background: The serotonin 2B receptor subtype (5-HT2BR), located in central nervous
system (CNS), cardiovascular system (CVS) and the gastrointestinal tract (GIT), is an important
target for the treatment of migraine, obesity and irritable bowel syndrome. 5-HT2BR is necessary for
the myocardial cell proliferation and differentiation at the embroyonic stage for healthy
development of heart. Recently, its involvement in drug induced valvulopathy and other myocardial
disorders, have paved a way for selective antagonist for the treatment of cardiac disorders.
Conclusion: The current review summarizes the limited progress made in the past decade for
design and development of 5-HT2BR antagonists for the treatment of disorders related to heart. We
focus primarily on the different scaffolds reported in both manuscripts and patents, that have led to
selectivity for 5-HT2B over subtype 5-HT2A/2C. Opportunities in cardiovascular drug development
for novel 5-HT2BR antagonists are also presented.