Ishizawa M
Nihon Heikatsukin Gakkai Zasshi. 1984 Oct;20(5):419-25. doi: 10.1540/jsmr1965.20.419.
The effects of trimebutine (2-dimethylamino-2-phenylbutyl-3, 4, 5-trimethoxy benzoate hydrogen maleate) and metoclopramide (N-diethylaminoethyl-2-methoxy-4-amino-5-chlorobenzamide) on propulsive activity of the isolated segmental colon, and on longitudinal and circular muscle layers of colon in guinea-pig were investigated. Trimebutine in doses up to 10(-7) g/ml slightly stimulated propulsive activity, but in doses as high as 10(-7) g/ml inhibited it. However, metoclopramide (10(-7)-10(-5) g/ml) stimulated propulsive activity in a dose dependent manner. Neostigmine-stimulated propulsive activity was inhibited by trimebutine (10(-6) g/ml) but potentiated by metoclopramide (10(-5) g/ml). Trimebutine (10(-8)-10(-5) g/ml) contracted circular muscle layer in a dose dependent manner, and contracted longitudinal muscle layer in doses up to 10(-7) g/ml, but in doses as high as 10(-7) g/ml relaxed it. While, metoclopramide (10(-8)-10(-5) g/ml) contracted both muscle layers. These results indicate that, at high doses, trimebutine-induced inhibition of propulsive activity may depend on a relaxation of longitudinal muscle, and at low doses, trimebutine-induced stimulation of propulsive activity may depend on a contraction of longitudinal muscle which was partly inhibited by atropine (10(-6) g/ml), though metoclopramide at low doses had little effect on propulsive activity.
研究了曲美布汀(马来酸氢 2 - 二甲氨基 - 2 - 苯基丁基 - 3,4,5 - 三甲氧基苯甲酸酯)和甲氧氯普胺(N - 二乙氨基乙基 - 2 - 甲氧基 - 4 - 氨基 - 5 - 氯苯甲酰胺)对豚鼠离体节段性结肠推进活性以及结肠纵行和环行肌层的影响。曲美布汀剂量高达 10⁻⁷g/ml 时对推进活性有轻微刺激作用,但剂量高达 10⁻⁶g/ml 时则抑制推进活性。然而,甲氧氯普胺(10⁻⁷ - 10⁻⁵g/ml)以剂量依赖性方式刺激推进活性。新斯的明刺激的推进活性被曲美布汀(10⁻⁶g/ml)抑制,但被甲氧氯普胺(10⁻⁵g/ml)增强。曲美布汀(10⁻⁸ - 10⁻⁵g/ml)以剂量依赖性方式使环行肌层收缩,剂量高达 10⁻⁷g/ml 时使纵行肌层收缩,但剂量高达 10⁻⁶g/ml 时则使其松弛。而甲氧氯普胺(10⁻⁸ - 10⁻⁵g/ml)使两层肌肉均收缩。这些结果表明,高剂量时曲美布汀诱导的推进活性抑制可能依赖于纵行肌的松弛,低剂量时曲美布汀诱导的推进活性刺激可能依赖于纵行肌的收缩,而阿托品(10⁻⁶g/ml)可部分抑制这种收缩,尽管低剂量的甲氧氯普胺对推进活性影响不大。