Background
(±)-Methoxyverapamil is a phenylalkylamine L-type calcium channel blocker and methoxy derivative of verapamil . (±)-Methoxyverapamil blocks recombinant rat L-type calcium channels expressed in tsA201 cells with IC50 values of 782 and 8,000 nM at holding potentials of 10 and -60 mV, respectively. It blocks maitotoxin-induced calcium influx in NIH3T3 fibroblasts (IC50 = 16 μM) and inhibits histamine-induced acid secretion by primary enriched guinea pig parietal cells (IC50 = 10.9 μM). (±)-Methoxyverapamil binds to rat myocardial membranes (IC50 = 16 nM) and inhibits electrically-stimulated contractions in rat right myocardial ventricular strips (EC50 = 1.95 μM). In conscious, ovariectomized, post-partum rats, it decreases blood pressure by 30 mm Hg and induces 60% inhibition of uterine contractions when administered at doses of 204 and 324 μg/kg, respectively.
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