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

•Mast cells are important mediators in cardiovascular diseases.•The mast cell mediator, histamine is involved in cardiovascular pathophysiology.•Histamine receptors are better target for treating cardiovascular therapies.•Antihistamines have been used widely in preclinical and clinical studies for C...

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Published in:Drug discovery today 2022-01, Vol.27 (1), p.234-245
Main Authors: Saheera, Sherin, Potnuri, Ajay Godwin, Guha, Ashrith, Palaniyandi, Suresh S., Thandavarayan, Rajarajan A.
Format: Article
Language:English
Subjects:
Antihistamines
Cardiovascular disease
Cardiovascular Diseases - drug therapy
Cardiovascular Diseases - metabolism
Cardiovascular Diseases - physiopathology
Histamine
Histamine - metabolism
Histamine 2 receptor
Histamine antagonists
Histamine Antagonists - pharmacology
Histamine receptor
Humans
Inflammation
Inflammation - metabolism
Inflammation - pathology
Mast cell
Mast Cells - drug effects
Mast Cells - physiology
Receptors, Histamine H2 - metabolism
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Summary:•Mast cells are important mediators in cardiovascular diseases.•The mast cell mediator, histamine is involved in cardiovascular pathophysiology.•Histamine receptors are better target for treating cardiovascular therapies.•Antihistamines have been used widely in preclinical and clinical studies for CVDs.•Repurposing of H2 receptor antagonists will aid in better adjuvant therapies for CVDs. 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.
ISSN:1359-6446
1878-5832
DOI:10.1016/j.drudis.2021.08.008