Padhariya Komal, Bhandare Richie, Canney Daniel, Velingkar Vinay
Department of Pharmaceutical Chemistry, SPP School of Pharmacy and Technology Management, SVKM's NMIMS University, V.L Mehta Road, Vile Parle (West), Mumbai 400056. India.
Department of Pharmaceutical Chemistry & Pharmacognosy, College of Pharmacy & Health Sciences, Ajman University, Ajman. United Arab Emirates.
Cardiovasc Hematol Disord Drug Targets. 2017;17(2):86-104. doi: 10.2174/1871529X17666170703115111.
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.
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.
血清素2B受体亚型（5-HT2BR）位于中枢神经系统（CNS）、心血管系统（CVS）和胃肠道（GIT），是治疗偏头痛、肥胖症和肠易激综合征的重要靶点。5-HT2BR对于胚胎期心肌细胞的增殖和分化以及心脏的健康发育是必需的。最近，其与药物性瓣膜病和其他心肌疾病的关联，为治疗心脏疾病的选择性拮抗剂开辟了道路。
本综述总结了过去十年在设计和开发用于治疗心脏相关疾病的5-HT2BR拮抗剂方面取得的有限进展。我们主要关注手稿和专利中报道的不同支架，这些支架导致了对5-HT2B相对于5-HT2A/2C亚型的选择性。还介绍了新型5-HT2BR拮抗剂在心血管药物开发中的机会。
