Suppression of charge movement by calcium antagonists is not related to calcium channel block.
The calcium channel-inhibiting drugs nitrendipine and diltiazem represent two important classes of organic calcium antagonists. In the present study, the effect of these drugs on calcium currents and charge displacement currents in bullfrog semitendinosus muscle fibers was examined using a vaseline gap voltage clamp. Nitrendipine (10 microM) reduced the quantity of charge that moved both during the ON phase (QON) and the OFF phase (QOFF) of charge movement. This action appeared to be most selective for QON. However, at this same concentration, nitrendipine had no blocking action on inward calcium currents. In contrast to these findings, diltiazem blocked calcium currents in a concentration-dependent manner, while slightly increasing the quantity of charge moved during QON and QOFF. The enhancement of charge movement by diltiazem resulted from two actions. First, diltiazem shifted the voltage-dependence of charge movement to more negative potentials. Second, diltiazem increased the maximum amount of charge moved.
D000818:Animals; D002118:Calcium / Q000378:metabolism*; D004110:Diltiazem / Q000494:pharmacology*; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects* / Q000502:physiology; D008564:Membrane Potentials / Q000187:drug effects; D009132:Muscles / Q000187:drug effects*; D009568:Nitrendipine / Q000494:pharmacology*; D011892:Rana catesbeiana
D007473:Ion Channels; D009568:Nitrendipine; D004110:Diltiazem; D002118:Calcium