Antiulcer effect of (-)-cis-2,3-dihydro-3-(4-methylpiperazinylmethyl)-2-phenyl-1,5-benzothiazepin-4-(5H)-one hydrochloride (BTM-1086) in experimental animals.

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Effects of (-)cis-2, 3-dihydro-3-(4-methylpiperazinylmethyl)-2-phenyl-1, 5-benzothiazepin-4-(5H)-one hydrochloride (BTM-1086) on various experimental gastric and duodenal ulcers were studied in rats. In the pylorus-ligated ulcer, restraint and water immersion stress ulcer, and drug-induced ulcer (indomethacin, aspirin, reserpine, serotonin, cysteamine), BTM-1086 prevented the development of ulcer at a dose of 0.1 to 1 mg/kg, p.o., but only weakly inhibited the histamine-induced gastric ulcer. The inhibitory activities of BTM-1086 were significantly higher than those of atropine sulfate. In the healing experiment with the acetic acid-induced stomach ulcer, BTM-1086 (1 mg/kg/day, p.o., ×14) showed a significant healing effect, which was higher than that of propantheline bromide. BTM-1086 at a dose of 0.2 mg/kg, i.d., remarkably inhibited the gastric secretion 6 hr after pylorus ligation. The aspirin-induced reductions of the total acid and K<SUP>+</SUP> as well as the increments of the volume and Na<SUP>+</SUP> in the gastric secretion were prevented dose-dependently by pretreatment with BTM-1086.
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