Mibefradil dihydrochloride hydrate

Mibefradil dihydrochloride hydrate (Ro 40-5967 dihydrochloride hydrate) is a effectively long-acting calcium channel antagonist, used as an antihypertensive agent. Mibefradil dihydrochloride hydrate acts via a higher affinity block for low-voltage-activated (T) than for high-voltage-activated (L) calcium channels[1].

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Research Areas >> Cardiovascular Disease

Calcium channel[1]

Mibefradil inhibits reversibly the T- and L-type currents with IC50 values of 2.7 and 18.6 μM, respectively[2]. Mibefradil (20 µM) reduces the amplitude of excitatory junction potentials (by 37±10 %), slows the rate of repolarisation (by 44±16 %) and causes a significant membrane potential depolarisation (from -83±1 mV to -71±5 mV)[3].

[1]. Martin RL, Lee JH, Cribbs LL, Perez-Reyes E, Hanck DA. Mibefradil block of cloned T-type calcium channels. J Pharmacol Exp Ther. 2000 Oct;295(1):302-8.

[2]. Mehrke G, et al. The Ca(++)-channel blocker Ro 40-5967 blocks differently T-type and L-type Ca++ channels. J Pharmacol Exp Ther. 1994 Dec;271(3):1483-8.

[3]. Brain KL, et al. The sources and sequestration of Ca(2+) contributing to neuroeffector Ca(2+) transients in the mouse vas deferens. J Physiol. 2003 Dec 1;553(Pt 2):627-35.