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Metoprolol is a β1-adrenergic receptor (β1-AR) antagonist (Ki = 47 nM in CHO cells expressing the human receptor).1 It is selective for β1- over β2- and β3-ARs (Kis = 2,730 and >10,000 nM, respectively, in CHO cells expressing the human receptors). Metoprolol (4.7 µM) reduces GTP-induced adenylyl cyclase (AC) activity in CHO cells expressing β1- and β2-ARs. It reduces pulse rate in isolated rat atria in a concentration-dependent manner.2 Metoprolol (10 mg/kg) reduces increased heart rate and mean arterial pressure (MAP) in a rat model of systolic hypertension induced by a fructose-rich diet. Formulations containing metoprolol have been used in the treatment of exercised-induced hypertension, angina, and tachycardia. This product is also available as an analytical reference standard (Item No. 21165).
WARNING This product is not for human or veterinary use.
1. Comparative pharmacology of human β-
2. In vitro and in vivo pharmacodynamic properties of metoprolol in fructose-