Abstract
We have investigated the effects of MCC-134 (1-[4-(1 H-imidazol-1-yl)benzoyl]- N-methyl-cyclobutanecarbothioamide) on membrane currents and ATP-sensitive K + channel (K ATP channel) opener-induced currents in pig urethra by use of patch-clamp techniques (conventional whole-cell configuration and nystatin perforated patch recordings). Tension measurement was also performed to study the effects of MCC-134 on the resting tone of pig urethral strips. MCC-134 reduced the resting tone of pig urethra in a concentration-dependent manner (EC 50=6 μM). The MCC-134 (30 μM)-induced relaxation was suppressed by glibenclamide. In voltage-clamp experiments, MCC-134 produced a concentration-dependent inward K + current which was suppressed by application of glibenclamide at a holding potential of −50 mV (symmetrical 140 mM K + conditions). Application of MCC-134 enhanced diazoxide-induced inward currents and inhibited pinacidil-induced inward currents in a concentration-dependent manner at −50 mV. These results suggest that MCC-134 induces glibenclamide-sensitive K ATP currents in pig urethra.
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