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Title

Mibefradil (Ro 40-5967) inhibits several Ca2+ and K+ currents in human fusion-competent myoblasts

Authors
Liu, J. H.
Bijlenga, P.
Occhiodoro, T.
Published in British Journal of Pharmacology. 1999, vol. 126, no. 1, p. 245-250
Abstract 1. The effect of mibefradil (Ro 40-5967), an inhibitor of T-type Ca2+ current (I(Ca)(T)), on myoblast fusion and on several voltage-gated currents expressed by fusion-competent myoblasts was examined. 2. At a concentration of 5 microM, mibefradil decreases myoblast fusion by 57%. At this concentration, the peak amplitudes of I(Ca)(T) and L-type Ca2+ current (I(Ca)(L)) measured in fusion-competent myoblasts are reduced by 95 and 80%, respectively. The IC50 of mibefradil for I(Ca)(T) and I(Ca)(L) are 0.7 and 2 microM, respectively. 3. At low concentrations, mibefradil increased the amplitude of I(Ca)(L) with respect to control. 4. Mibefradil blocked three voltage-gated K+ currents expressed by human fusion-competent myoblasts: a delayed rectifier K+ current, an ether-a-go-go K+ current, and an inward rectifier K+ current, with a respective IC50 of 0.3, 0.7 and 5.6 microM. 5. It is concluded that mibefradil can interfere with myoblast fusion, a mechanism fundamental to muscle growth and repair, and that the interpretation of the effect of mibefradil in a given system should take into account the action of this drug on ionic currents other than Ca2+ currents.
Keywords AdolescentBenzimidazoles/ pharmacologyCalcium Channel Blockers/ pharmacologyCalcium Channels/ drug effects/metabolismCell Fusion/drug effectsElectric StimulationHumansInfantMembrane Potentials/drug effects/physiologyMibefradilMuscle, Skeletal/cytology/ drug effects/metabolismPatch-Clamp TechniquesPotassium Channels/ drug effects/metabolismTetrahydronaphthalenes/ pharmacology
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PMID: 10051142
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