Bepridil is a dihydropyridine that has anti-anginal and anti-arrhythmic actions by blocking calcium channels in heart and smooth muscle. It is recognized as a non-selective channel blocker, altering myocardial Ca2+, Na+, and K+ currents. For example, it blocks voltage-gated Ca2+ (Cav3.2) and K+ (hERG and KCNQ4) channels, sarcoplasmic ATP-sensitive K+ (KATP) channels, and Na+-activated (KNa) channels (IC50s = 7.1, 22, 9.4, 10, and 2.2 μM, respectively). It also activates mitochondrial ATP-sensitive KATP channels (ED50 = 27.5 μM).
