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Overview
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Background
Labetalol HCl is a selective antagonist for the α1-adrenergic receptor and a non-selective antagonist for the β-adrenergic receptor. Labetalol HCl has been used for the treatment of high blood pressure. Labetalol HCl competitively targets the α1-adrenergic receptors expressed in vascular smooth muscle, thus inhibiting adrenergic stimulation on endothelial cells and vasoconstriction in peripheral blood vessels. Labetalol HCl also blocks the β-adrenergic receptors in bronchial and vascular smooth muscle to counteract adrenergic stimulation. Ultimately, labetalol HCl causes decreases in resting and exercise heart rates, cardiac output, as well as in both systolic and diastolic blood pressure, exherting vasodilation, as well as negative chronotropic and inotropic cardiac effects.
1. National Center for Biotechnology Information (2021). PubChem Compound Summary for CID 3869, Labetalol. Retrieved August 21, 2021.
2. Dage RC, Hsieh CP. Direct vasodilatation by labetalol in anaesthetized dogs. British Journal of Pharmacology, 1980, 70(2): 287-293.
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Overview