Bisoprolol-d7 (hemifumarate) is intended for use as an internal standard for the quantification of bisoprolol (Item No. 23827) by GC- or LC-MS. Bisoprolol is a potent B-adrenergic receptor (B-AR) antagonist that is selective for B1-ARs over B2-ARs (Kis = 25 and 480 nM, respectively in S49 cells overexpressing the human receptors).{39505} It also selectively binds to B1-ARs over B2-ARs in human myocardium (Kis = 75.8 and 991 nM, respectively).{39506} Bisoprolol binds to rat ventricular myocytes and heart membrane (Kis = 20 and 38.1 nM, respectively) and to rat B1-AR in salivary glands and B2-AR in reticulocytes (Kis = 24 and 1,945 nM, respectively).{39507,39508} In vivo, it inhibits increases in heart rate induced by isoproterenol (Item No. 15592) in guinea pigs.{39509} Bisoprolol (0.3 mg/kg) inhibits isoproterenol-induced increases in heart rate and myocardial contractility in conscious dogs. It also decreases blood pressure and heart rate in spontaneously hypertensive rats (SHRs) when chronically administered at a dose of 7.5 mg/kg twice per day over 19 weeks. Formulations containing bisoprolol have been used in the treatment of heart failure, angina pectoris, mild to moderate hypertension, and for secondary prevention of myocardial infarction.
1 mg
Cayman Chemical
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