Key result
Targeting α1A-adrenergic receptors shows emerging cardioprotective effects across recent physiological and therapeutic studies.
Why the study?
While the physiological functions of myocardial β1-adrenergic receptors and vascular smooth muscle α1-adrenergic receptors have been extensively explicated, recent developments have revealed emerging cardioprotective effects of the cardiac α1A-adrenergic receptor subtype.
This review highlights recent developments in cardiac α1-adrenergic receptor biology, specifically focusing on the emerging cardioprotective effects of the α1A-AR subtype as a potential therapeutic target.
The cardiovascular system is required to adapt continuously to fluctuations in physiological demands from exercise, stress, and hemodynamic load. The sympathetic nervous system (SNS) plays a central role in these adaptations through the release of norepinephrine (NE) and epinephrine (EPI). These endogenous catecholamines bind to adrenergic receptors (ARs) in the heart and blood vessels to regulate cardiac output and blood pressure. Adrenergic receptors are ligand-activated G-protein-coupled receptors (GPCRs) that most broadly are divided into α- and β-AR families. Cardiomyocytes predominantly express β1-ARs, with smaller populations of β2-ARs, α1-ARs. The physiological functions of the myocardial β1-AR and vascular smooth muscle α1-ARs have been explicated extensively. This review will focus on recent developments in our understanding of α1-AR biology in the heart, with a particular focus on recent data explicating the emerging cardioprotective effects of the α1A-AR subtype.
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Nagalingam et al. (2026) reported a review. α1A-adrenergic receptor targeting was evaluated. Cardiac α1A-adrenergic receptor biology demonstrates emerging cardioprotective effects in recent physiological and therapeutic studies.
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