We studied the antioxidant activities of calcium antagonists against autoxi
dation in rat brain homogenates. The homogenates were incubated for 30 min
at 37 degrees C with or without a calcium antagonist and subsequently assay
ed for lipid peroxide content. Percent inhibition of the lipid peroxidation
was used as an index of the antioxidant effect. Dihydropyridine calcium an
tagonists exhibited concentration-dependent (3-300 mu mol/l) inhibitory eff
ects against lipid peroxidation. The relative order of antioxidant potency
and associated IC50 values (mu mol/l) of the calcium antagonists for inhibi
tion of the lipid peroxidation were as follows: nifedipine (51.5)>barnidipi
ne (58.6)>benidipine (71.2)>nicardipine (129.3)>amlodipine (135.5)>nilvadip
ine (167.3)>nitrendipine (252.1)>> diltiazem (>300) verapamil (>300). These
results suggest that some dihydropyridine calcium antagonists show antioxi
dant properties, The antioxidant effects of the calcium antagonists may con
tribute to their pharmacological actions.