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右美沙芬和左美沙芬对大鼠胃排空和肠道转运的影响。

Effect of dextromethorphan and levomethorphan on gastric emptying and intestinal transit in the rat.

作者信息

Gaginella T S, Bertko R J, Kachur J F

出版信息

J Pharmacol Exp Ther. 1987 Feb;240(2):388-91.

PMID:3806403
Abstract

Dextromethorphan and levomethorphan were evaluated using 51Cr as a marker for their effects on gastric emptying and intestinal transit in the rat. Levomethorphan at 10 mg/kg i.p. and 10 and 50 mg/kg p.o. significantly (P less than or equal to .05) inhibited gastric emptying; dextromethorphan did not inhibit gastric emptying at p.o. doses up to 100 mg/kg or i.p. doses up to 10 mg/kg. Naloxone (1 mg/kg i.p.) significantly antagonized the effect of p.o. levomethorphan (50 mg/kg). Levomethorphan (10 and 50 mg/kg p.o. and 1 and 10 mg/kg i.p.) significantly inhibited intestinal transit. Dextromethorphan significantly inhibited intestinal transit after p.o. (10, 50, 100, 200 mg/kg) and i.p. (50 mg/kg) administration. As in the case of gastric emptying, naloxone inhibited the effect of levomethorphan but did not alter the effect of dextromethorphan. Naloxone itself (1 mg/kg i.p.) did not affect gastric emptying or intestinal transit. The results suggest that levomethorphan exerts inhibitory effects on intestinal transit and gastric emptying that are probably mediated partly through an opiate mechanism whereas the effects of dextromethorphan may be mediated through a nonopiate mechanism of action.

摘要

以51Cr作为标记物,评估右美沙芬和左美沙芬对大鼠胃排空和肠道转运的影响。腹腔注射10mg/kg以及口服10和50mg/kg的左美沙芬显著(P≤0.05)抑制胃排空;口服剂量高达100mg/kg或腹腔注射剂量高达10mg/kg的右美沙芬均未抑制胃排空。纳洛酮(1mg/kg腹腔注射)显著拮抗口服左美沙芬(50mg/kg)的作用。左美沙芬(口服10和50mg/kg以及腹腔注射1和10mg/kg)显著抑制肠道转运。口服(10、50、100、200mg/kg)和腹腔注射(50mg/kg)右美沙芬后均显著抑制肠道转运。与胃排空情况相同,纳洛酮抑制左美沙芬的作用,但不改变右美沙芬的作用。纳洛酮本身(1mg/kg腹腔注射)不影响胃排空或肠道转运。结果表明,左美沙芬对肠道转运和胃排空产生抑制作用,可能部分通过阿片类机制介导,而右美沙芬的作用可能通过非阿片类作用机制介导。

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