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Mibefradil dihydrochloride

CAS No. : 116666-63-8

MCE 站：Mibefradil dihydrochloride

产品活性：Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) 是一种钙离子通道 (calcium channel) 抑制剂，选择性作用于 T 型 Ca²⁺通道，作用于 T 型和 L 型通道，IC₅₀ 分别为 2.7 μM 和 18.6 μM。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：Calcium Channel

In Vitro: Mibefradil dihydrochloride inhibits reversibly the T- and L-type currents with IC₅₀ values of 2.7 and 18.6 μM, respectively. The inhibition of the L-type current is voltage-dependent, whereas that of the T-type current is not. Ro 40-5967 blocks T-type current already at a holding potential of -100 mV At a higher concentration (20 ?M), Mibefradil 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). At a higher Mibefradil concentration (20 ?M) there is significant membrane potential depolarisation and a slowing of repolarisation. These actions of Mibefradil are consistent with K⁺ channel inhibition, which has been shown to occur in human myoblasts and other cells.

In Vivo: The hearing thresholds of the 24-26 week old C57BL/6J mice differ following the 4-week treatment period. The hearing threshold at 24 kHz is significantly decreased in the Mibefradil-treated and benidipine-treated groups compared with the saline-treated group (P<0.05). Compared with the saline-treated group, rats receiving Mibefradil or NSC 64013 show significant lower Ca_V3.2 expression in the spinal cord and DRG.

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