Furukawa K, Kimoto Y
Jpn J Pharmacol. 1984 Jul;35(3):307-17. doi: 10.1254/jjp.35.307.
The effects of trimebutine maleate (TM-906) on electrical and mechanical activities of smooth muscles of the guinea-pig stomach were investigated using a microelectrode and isometric tension recording methods. TM-906 (2 X 10(-5) M) depolarized the membrane of smooth muscles in the antrum to about 10 mV. From the current-voltage relationship and changes in membrane potentials in various [K]0, the TM-906-induced depolarization is considered to be mainly due to a decrease in the K-conductance. TM-906 increased the amplitude of the first spike potential and regularized the rhythm of slow waves. These excitatory effects are presumably due to the K-channel-blocking action during the repolarizing phase of the spikes and to the depolarization. TM-906 reduced the amplitudes of mechanical activities and slow waves. These inhibitory effects are presumably due to the inhibition of Ca-release from storage sites and to the block of Ca-influx. The biphasic effects are possibly due to the local anesthetic properties. TM-906 modified neither the membrane potential nor the membrane conductance of circular muscles in the fundus. This may mean that the circular muscles in the fundus lack the K-channel sensitive to TM-906.
采用微电极和等长张力记录方法，研究了马来酸曲美布汀（TM - 906）对豚鼠胃平滑肌电活动和机械活动的影响。TM - 906（2×10⁻⁵ M）使胃窦平滑肌膜去极化约10 mV。根据电流 - 电压关系以及不同细胞外钾离子浓度（[K]₀）下膜电位的变化，认为TM - 906诱导的去极化主要是由于钾离子电导降低所致。TM - 906增加了第一个锋电位的幅度，并使慢波节律规则化。这些兴奋作用可能是由于在锋电位复极化阶段钾通道阻断作用以及去极化作用。TM - 906降低了机械活动和慢波的幅度。这些抑制作用可能是由于抑制了钙从储存部位的释放以及阻断了钙内流。其双相作用可能归因于局部麻醉特性。TM - 906对胃底环行肌的膜电位和膜电导均无影响。这可能意味着胃底环行肌缺乏对TM - 906敏感的钾通道。
