Overview
Alomone Labs Mibefradil dihydrochloride hydrate inhibits T-type CaV channels heterologously expressed in Xenopus oocytes.A. Time course of CaV3.2 peak current amplitude, elicited by 100 ms voltage step from holding potential of -100 mV to -20 mV, delivered every 10 seconds. Application of 10 µM Mibefradil dihydrochloride hydrate (#M-150) inhibits CaV3.2current in a reversible manner (indicated by the horizontal bar).
B. Representative current traces before and during application of 10 µM Mibefradil dihydrochloride hydrate as indicated.
Mibefradil dihydrochloride hydrate, a potent T-type calcium antagonist, belongs to a new class of Ca2+ antagonists, the tetralol derivatives. It selectively blocks T-type Ca2+ channels in contrast to other Ca2+ antagonists which block only L-type channels1. Mibefradil also modulates the gating properties of KV10.1 channel6. It also blocks Orai1-3 channels with the following IC50: 52.6, 14.1, and 3.8 μM respectively, in whole-cell and excised-membrane patch clamp7.
Mibefradil dihydrochloride hydrate has moderate selectivity for T-type Ca2+ channels displaying IC50 values of 2.7 μM and 18.6 μM for T-type and L-type channels respectively2. Mibefradil relaxes coronary arteries without suppressing myocardial contractility and causes a dose-related decrease in heart rate. Mibefradil demonstrated end organ protection such as preventing neointima formation after vascular injury and myocardial hypertrophy3. In addition, it has been shown that it inhibits human cancer cell proliferation in vitro with several cell lines including glioblastoma (GB), by inhibiting passage beyond the G1/S interphase4,5.
