Cardiovascular Concern of 5-HT2B Receptor and Recent Vistas in the Development of Its Antagonists

Author(s): Komal Padhariya, Richie Bhandare*, Daniel Canney, Vinay Velingkar

Journal Name: Cardiovascular & Hematological Disorders-Drug Targets
Formerly Current Drug Targets - Cardiovascular & Hematological Disorders

Volume 17 , Issue 2 , 2017

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Graphical Abstract:


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.

Keywords: Serotonin inhibitors, 5-HT2BR antagonist, valvulopathy, pulmonary arterial hypertension, tryptophan platelet, platelet aggregation.

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Article Details

Year: 2017
Page: [86 - 104]
Pages: 19
DOI: 10.2174/1871529X17666170703115111
Price: $65

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PDF: 74