Yokochi E, Kohno S, Ohata K
Department of Pharmacology, Kyoto Pharmaceutical University, Japan.
Nihon Yakurigaku Zasshi. 1988 Nov;92(5):297-310. doi: 10.1254/fpj.92.297.
Effects of the clathrate compound of mobenzoxamine (MBX) with beta-cyclodextrin (MBX-CD), a new gastro-intestinal function modulator, on the digestive system were studied in comparison with those of metoclopramide, domperidone and trimebutine. MBX-CD showed inhibitory effects that were approximately 1/4 times as potent as metoclopramide on both apomorphine- and copper sulfate-induced emesis and about 1/40 times as potent as domperidone on apomorphine-induced emesis in dogs. In rats, MBX-CD enhanced gastric emptying as potently as metoclopramide, and only MBX-CD showed a clear amelioration of the delayed gastric emptying induced by BaCl2. Similarly, only MBX-CD showed an ameliorative effect on small intestinal transport accelerated by BaCl2 in mice. Though both MBX and trimebutine inhibited spontaneous contractions of the isolated guinea pig stomach and rabbit intestine, it seemed that the properties of these effects were different from those of papaverine. On isolated guinea pig ileum, MBX inhibited contractions induced by various agonists equally to or more potently than trimebutine or papaverine. The results suggest that MBX-CD or MBX acts extensively on the gastro-intestinal system for the reason that it has not only the respective properties of the gastro-intestinal function modulators used as the standards, but also its own characteristic effects.
将新型胃肠功能调节剂莫苯沙明(MBX)与β-环糊精的包合物(MBX-CD)对消化系统的作用,与胃复安、多潘立酮和曲美布汀进行了比较研究。在犬身上,MBX-CD对阿扑吗啡和硫酸铜诱导的呕吐均显示出抑制作用,其效力约为胃复安的1/4,对阿扑吗啡诱导的呕吐的效力约为多潘立酮的1/40。在大鼠中,MBX-CD增强胃排空的效力与胃复安相当,并且只有MBX-CD对BaCl2诱导的胃排空延迟有明显改善作用。同样,只有MBX-CD对BaCl2加速的小鼠小肠转运有改善作用。虽然MBX和曲美布汀都抑制离体豚鼠胃和兔肠的自发收缩,但这些作用的性质似乎与罂粟碱不同。在离体豚鼠回肠上,MBX抑制各种激动剂诱导的收缩的效力与曲美布汀或罂粟碱相当或更强。结果表明,MBX-CD或MBX广泛作用于胃肠系统,因为它不仅具有用作标准的胃肠功能调节剂各自的特性,还具有自身的特征性作用。