Sato M, Kitagawa H, Fujiwara M
Nihon Yakurigaku Zasshi. 1982 Apr;79(4):307-15.
The effects of tofisopam on gastric functions were examined in rats. Intracerebroventricular (i.c.v.) injection of tofisopam (50 ot 100 microgram) increased both basal gastric acid output and mucosal blood flow (MBF) in rats anesthetized with urethane, while intravenous injection of tofisopam (10 mg/kg) did not change the basal gastric acid output. Ten micrograms of tofisopam, i.c.v., a dose which did not show any effect on the basal gastric acid output, significantly inhibited the decrease in gastric acid output induced by noradrenaline (5 microgram, i.c.v.). Tofisopam (10 mg/kg, i.v. or 100 microgram, i.c.v.) showed no effect on the increase in gastric acid output induced by electrical stimulation of the lateral hypothalamic area (LHA). These results, together with the previous findings, suggest the tofisopam (i.c.v.) acts on the nucleus dorsalis n. vagi and/or LHA and competes with noradrenaline. The gastric acid output was increased remarkably under water-immersion stress, and this increase lasted during the stress-loading, but the MBF did not show a corresponding increase. Pretreatment of rats with tofisopam (100 mg/kg, intraduodenal) significantly increased the MBF and inhibited the ulcer formation caused by the stress. From these results, tofisopam may restore the unbalance between sympathetic and parasympathetic nervous tones induced by stress-loading.
研究了托非索泮对大鼠胃功能的影响。向用乌拉坦麻醉的大鼠脑室内注射托非索泮（50或100微克）可增加基础胃酸分泌量和黏膜血流量（MBF），而静脉注射托非索泮（10毫克/千克）对基础胃酸分泌量无影响。脑室内注射10微克托非索泮，该剂量对基础胃酸分泌量无任何影响，但能显著抑制去甲肾上腺素（脑室内注射5微克）引起的胃酸分泌量减少。托非索泮（静脉注射10毫克/千克或脑室内注射100微克）对电刺激下丘脑外侧区（LHA）引起的胃酸分泌量增加无影响。这些结果与先前的研究结果表明，脑室内注射托非索泮作用于迷走神经背核和/或LHA，并与去甲肾上腺素竞争。在水浸应激下胃酸分泌量显著增加，且在应激加载期间持续增加，但MBF未相应增加。用托非索泮（十二指肠内注射100毫克/千克）预处理大鼠可显著增加MBF并抑制应激引起的溃疡形成。从这些结果来看，托非索泮可能恢复应激加载引起的交感和副交感神经张力失衡。
