1998Endocrine ResearchRequires access

Mibefradil, AT-type calcium channel antagonist in Y1 cells

M Esneu, Nicole Gallo‐Payet, M Payet

Open publisher page 7 citations

Abstract

The effect of mibefradil, a new nondihydropyridine Ca2+ channel antagonist, was investigated on Y1 cells which exhibited T-and L-type Ca2+ currents. In the great majority of these cells, mibefradil rapidly and selectively blocked T-type Ca2+ current in a dose-dependent manner with a half maximum action at 10-7 M. Furthermore, the specific L-type Ca2+ channel inhibitor, nifedipine, blocked the Ca2+ inward current remaining after the action of mibefradil. Mibefradil does not modify the voltage-dependent characteristics of the current/voltage relationship. However, mibefradil is more effective at depolarized membrane potential.

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What this paper is about

The effect of mibefradil, a new nondihydropyridine Ca2+ channel antagonist, was investigated on Y1 cells which exhibited T-and L-type Ca2+ currents. In the great majority of these cells, mibefradil rapidly and selectively blocked T-type Ca2+ current in a dose-dependent manner with a half maximum action at 10-7 M. Furthermore, the specific L-type Ca2+ channel inhibitor, nifedipine, blocked the Ca2+ inward current remaining after the action of mibefradil. Mibefradil does not modify the voltage-dependent characteristics of the current/voltage relationship. However, mibefradil is more effective at depolarized membrane potential.

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Available abstract

The effect of mibefradil, a new nondihydropyridine Ca2+ channel antagonist, was investigated on Y1 cells which exhibited T-and L-type Ca2+ currents. In the great majority of these cells, mibefradil rapidly and selectively blocked T-type Ca2+ current in a dose-dependent manner with a half maximum action at 10-7 M. Furthermore, the specific L-type Ca2+ channel inhibitor, nifedipine, blocked the Ca2+ inward current remaining after the action of mibefradil. Mibefradil does not modify the voltage-dependent characteristics of the current/voltage relationship. However, mibefradil is more effective at depolarized membrane potential.

Key concepts: Mibefradil, Nifedipine, Antagonist, T-type calcium channel, Voltage-dependent calcium channel, Chemistry, Calcium channel, Calcium

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