1049728-52-0

1049728-52-0 structure

Name: Mibefradil dihydrochloride hydrate
Chemical Name: Mibefradil dihydrochloride hydrate
CAS Number: 1049728-52-0
Molecular Formula: C₂₉H₄₂Cl₂FN₃O₄
Molecular Weight: 586.57
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Calcium Channel
Create Date: 2022-08-16 20:30:37
Modify Date: 2024-01-14 16:36:57
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].

Name	Mibefradil dihydrochloride hydrate

Description	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].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Cardiovascular Disease
Target	Calcium channel[1]
In Vitro	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].
References	[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.

Molecular Formula	C₂₉H₄₂Cl₂FN₃O₄
Molecular Weight	586.57