Kojima K, Iwano K, Nishimura H, Yoshimura A, Okuda H, Suzuki Y
Nihon Yakurigaku Zasshi. 1982 Jan;79(1):23-32.
Effects of TPH-3 on various experimental gastric ulcers in rats and guinea-pigs were studied and the following results were obtained. In the preventive experiments, such as the Shay's ulcer, pylorus-ligated aspirin ulcer and restraint and water immersion stress ulcer, TPH-3 (200 mg/kg i.d. or p.o.) showed a statistically significant inhibition. TPH-3 markedly inhibited the histamine-induced gastric ulcer in guinea-pigs and a dose-response relationship was obtained for doses of 12.5, 25 and 50 mg/kg p.o. TPH-3 showed the weak inhibition regarding therapy for serosa-seared gastric ulcer and the recovery process of restraint and water immersion stress ulcer in rats. TPH-3, dosing 100 mg/kg intraduodenally, significantly inhibited the gastric secretion in the pylorus-ligated rats. TPH-3 significantly inhibited the histamine, pentagastrin and carbachol-induced acid secretion in the stomach-perfused rats. In particular, TPH-3 showed strong sensitivity to the action of histamine. TPH-3 had no anti-ACh or anti-H1-receptor effects.
研究了TPH - 3对大鼠和豚鼠各种实验性胃溃疡的影响，获得了以下结果。在预防性实验中，如 Shay 溃疡、幽门结扎阿司匹林溃疡以及束缚和水浸应激溃疡，TPH - 3（腹腔注射或口服200mg/kg）显示出具有统计学意义的抑制作用。TPH - 3显著抑制豚鼠组胺诱导的胃溃疡，对于口服剂量为12.5、25和50mg/kg的情况获得了剂量 - 反应关系。TPH - 3对大鼠浆膜烧灼性胃溃疡的治疗以及束缚和水浸应激溃疡的恢复过程显示出较弱的抑制作用。十二指肠内给药100mg/kg的TPH - 3显著抑制幽门结扎大鼠的胃酸分泌。TPH - 3显著抑制胃灌流大鼠中组胺、五肽胃泌素和卡巴胆碱诱导的胃酸分泌。特别是，TPH - 3对组胺的作用表现出强烈的敏感性。TPH - 3没有抗乙酰胆碱或抗H1受体作用。
