Trimebutine maleate has inhibitory effects on the voltage-dependent Ca2+ inward current and other membrane currents in intestinal smooth muscle cells.
We examined effects of trimebutine maleate on the membrane currents of the intestinal smooth muscle cells by using the tight-seal whole cell clamp technique. Trimebutine suppressed the Ba2+ inward current through voltage-dependent Ca2+ channels in a dose-dependent manner. The inhibitory effect of trimebutine on the Ba2+ inward current was not use-dependent. It shifted the steady-state inactivation curve to the left along the voltage axis. Trimebutine also had inhibitory effects on the other membrane currents of the cells, such as the voltage-dependent K+ current, the Ca2(+)-activated oscillating K+ current and the acetylcholine-induced inward current. These relatively non-specific inhibitory effects of trimebutine on the membrane currents may explain, at least in part, the dual actions of the drug on the intestinal smooth muscle contractility, i.e. inhibitory as well as excitatory.
Shimada
T
T
Second Department of Internal Medicine, Faculty of Medicine, University of Tokyo, Japan.
Kurachi
Y
Y
Terano
A
A
Hamada
E
E
Sugimoto
T
T
D000818:Animals; D001565:Benzoates / Q000494:pharmacology*; D015220:Calcium Channels / Q000187:drug effects*; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008564:Membrane Potentials / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects*; D011817:Rabbits; D014287:Trimebutine / Q000494:pharmacology*
D001565:Benzoates; D015220:Calcium Channels; D014287:Trimebutine