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Drug Discov Today. 2021 Aug 23; doi: 10.1016/j.drudis.2021.08.008. Epub 2021 Aug 23.

Histamine 2 receptors in cardiovascular biology: A friend for the heart.

Drug discovery today

Sherin Saheera, Ajay Godwin Potnuri, Ashrith Guha, Suresh S Palaniyandi, Rajarajan A Thandavarayan

Affiliations

  1. Division of Cellular and Molecular Cardiology, Sree Chitra Tirunal Institute for Medical Sciences and Technology, Trivandrum, India.
  2. Department of Cardiology, Houston Methodist Hospital, Houston, TX 77030, USA.
  3. Division of Hypertension and Vascular Research, Henry Ford Health System, Detroit, MI 48202, USA.
  4. Department of Cardiology, Houston Methodist Hospital, Houston, TX 77030, USA. Electronic address: [email protected].

PMID: 34438076 DOI: 10.1016/j.drudis.2021.08.008

Abstract

Undermining new mediators involved in the development and progression of cardiovascular diseases (CVDs) is vital for better disease management. Existing studies implicate a crucial role for inflammation and inflammatory cells, particularly mast cells, in cardiac diseases. Interestingly, the mast cell mediator, histamine, and its receptors profoundly impact the pathophysiology of the heart, resulting in hypertension-induced cardiac hypertrophy and other cardiac anomalies. In this review, we provide a detailed description of mast cell activation, mediators, and histamine receptors, with a particular focus on histamine 2 receptors (H2Rs). Preclinical and clinical studies using histamine receptor antagonists report improvement in cardiac function. Insights into the precise function of histamine receptors will aid in developing novel therapies and pave the way for repurposing antihistamines for cardiovascular diseases.

Copyright © 2021 Elsevier Ltd. All rights reserved.

Keywords: Antihistamines; Cardiovascular disease; Histamine; Histamine 2 receptor; Histamine antagonists; Histamine receptor; Inflammation; Mast cell

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