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

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

Research output: Contribution to journalReview articlepeer-review

9 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)234-245
Number of pages12
JournalDrug Discovery Today
Issue number1
StatePublished - Jan 2022


  • Antihistamines
  • Cardiovascular disease
  • Histamine
  • Histamine 2 receptor
  • Histamine antagonists
  • Histamine receptor
  • Inflammation
  • Mast cell
  • Histamine Antagonists/pharmacology
  • Histamine/metabolism
  • Humans
  • Inflammation/metabolism
  • Receptors, Histamine H2/metabolism
  • Cardiovascular Diseases/drug therapy
  • Mast Cells/drug effects

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology


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