Cardiovascular concern of 5-HT2B receptor and recent vistas in the development of its antagonists

Komal Padhariya; Richie Bhandare; Daniel Canney; Vinay Velingkar

doi:10.2174/1871529X17666170703115111

Cardiovascular concern of 5-HT_2B receptor and recent vistas in the development of its antagonists

Komal Padhariya
, Richie Bhandare
, Daniel Canney
, Vinay Velingkar

College of Pharmacy and Health Sciences

Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management
Temple University

Research output: Contribution to journal › Review article › peer-review

9 Scopus citations

Abstract

Background: The serotonin 2B receptor subtype (5-HT_2BR), 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-HT_2BR 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-HT_2BR 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-HT_2B over subtype 5-HT_2A/2C. Opportunities in cardiovascular drug development for novel 5-HT_2BR antagonists are also presented.

Original language	English
Pages (from-to)	86-104
Number of pages	19
Journal	Cardiovascular and Hematological Disorders - Drug Targets
Volume	17
Issue number	2
DOIs	https://doi.org/10.2174/1871529X17666170703115111
State	Published - 1 Aug 2017

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

5-HTR antagonist
Platelet aggregation
Pulmonary arterial hypertension
Serotonin inhibitors
Tryptophan platelet
Valvulopathy

Access to Document

10.2174/1871529X17666170703115111

Cite this

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title = "Cardiovascular concern of 5-HT2B receptor and recent vistas in the development of its antagonists",

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 = "5-HTR antagonist, Platelet aggregation, Pulmonary arterial hypertension, Serotonin inhibitors, Tryptophan platelet, Valvulopathy",

author = "Komal Padhariya and Richie Bhandare and Daniel Canney and Vinay Velingkar",

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year = "2017",

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language = "English",

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T1 - Cardiovascular concern of 5-HT2B receptor and recent vistas in the development of its antagonists

AU - Padhariya, Komal

AU - Bhandare, Richie

AU - Canney, Daniel

AU - Velingkar, Vinay

PY - 2017/8/1

Y1 - 2017/8/1

N2 - 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.

AB - 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.

KW - 5-HTR antagonist

KW - Platelet aggregation

KW - Pulmonary arterial hypertension

KW - Serotonin inhibitors

KW - Tryptophan platelet

KW - Valvulopathy

UR - https://www.scopus.com/pages/publications/85040245871

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DO - 10.2174/1871529X17666170703115111

M3 - Review article

C2 - 28676029

AN - SCOPUS:85040245871

SN - 1871-529X

VL - 17

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EP - 104

JO - Cardiovascular and Hematological Disorders - Drug Targets

JF - Cardiovascular and Hematological Disorders - Drug Targets

IS - 2

ER -