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

Drug Discov Today. 2022 Jan;27(1):234-245. doi: 10.1016/j.drudis.2021.08.008. Epub 2021 Aug 23.

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.

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

Publication types

  • Review

MeSH terms

  • Cardiovascular Diseases* / drug therapy
  • Cardiovascular Diseases* / metabolism
  • Cardiovascular Diseases* / physiopathology
  • Histamine / metabolism
  • Histamine Antagonists / pharmacology*
  • Humans
  • Inflammation* / metabolism
  • Inflammation* / pathology
  • Mast Cells* / drug effects
  • Mast Cells* / physiology
  • Receptors, Histamine H2 / metabolism*

Substances

  • Histamine Antagonists
  • Receptors, Histamine H2
  • Histamine