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

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DRUG DISCOVERY TODAY
卷 27, 期 1, 页码 234-245

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ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2021.08.008

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

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Understanding the role of mast cells and histamine in cardiovascular diseases, particularly in cardiac hypertrophy, can lead to better disease management. Research on histamine receptors has shown improvement in cardiac function, suggesting potential for novel therapies in the future.
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 inflamma-tion 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.

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