Description
Metoprolol-d6 is intended for use as an internal standard for the quantification of metoprolol (Item No. 15429) by GC- or LC-MS. 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.WARNING This product is not for human or veterinary use.
References
[1] C HOFFMANN. Comparative pharmacology of human beta-adrenergic receptor subtypes–characterization of stably transfected receptors in CHO cells.[J]. Naunyn-Schmiedeberg’s archives of pharmacology, 2004, 369 2: 151-159. DOI:
10.1007/s00210-003-0860-y[2] CARLA ANDREA DI VERNIERO. In vitro and in vivo pharmacodynamic properties of metoprolol in fructose-fed hypertensive rats.[J]. Journal of Cardiovascular Pharmacology, 2008, 51 6: 532-541. DOI:
10.1097/fjc.0b013e3181730306
