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μ受体在犬阿片类药物胃分泌作用中的中枢和外周参与情况。

Central and peripheral involvement of mu receptors in gastric secretory effects of opioids in the dog.

作者信息

Soldani G, Del Tacca M, Mengozzi G, Bernardini C, Bartolini D

出版信息

Eur J Pharmacol. 1985 Nov 19;117(3):295-301. doi: 10.1016/0014-2999(85)90002-0.

DOI:10.1016/0014-2999(85)90002-0
PMID:3000805
Abstract

The effects of dermorphin and morphine on gastric acid secretion were studied in conscious dogs with both gastric fistulas (GF) and Heidenhain pouches (HP). Under basal conditions dermorphin and morphine, infused systemically at graded doses, produced a significant increase in acid secretion from both GF and HP. This increase was significantly inhibited by naloxone, naltrexone methylbromide and N-methyl-levallorphan methanesulphonate. Dermorphin did not modify the acid output stimulated by 2-deoxy-D-glucose from GF, while morphine significantly inhibited it; on the contrary acid secretion from HP was increased in this test by both dermorphin and morphine. Acid secretion from GF stimulated by pentagastrin was unaffected by morphine and significantly enhanced by dermorphin. Under these conditions a significant increase in acid secretion from HP was recorded with dermorphin and morphine. Naloxone and N-methyl-levallorphan methanesulphonate, given during pentagastrin-stimulated secretion, significantly inhibited acid output 'per se' from GF and HP and prevented the stimulatory effect of dermorphin and morphine. Bethanechol-induced secretion from GF and HP was significantly increased by both dermorphin and morphine. The present results demonstrate that opioids have simultaneous yet opposite effects on acid secretion in the dog and that mu receptors are involved in both the excitatory and inhibitory effects. Excitatory effects do not seem to be mediated via a vagal pathway (peripheral ?), in contrast to the inhibitory effects (central ?). The inhibitory effects of opiate antagonists on pentagastrin-stimulated secretion suggest a physiological role of peripheral opioid receptors in gastric acid secretion.

摘要

在具有胃瘘(GF)和海登海因小胃(HP)的清醒犬中,研究了皮啡肽和吗啡对胃酸分泌的影响。在基础条件下,以分级剂量全身输注皮啡肽和吗啡,可使来自GF和HP的胃酸分泌显著增加。这种增加被纳洛酮、纳曲酮甲基溴和N-甲基左洛啡烷甲磺酸盐显著抑制。皮啡肽不改变2-脱氧-D-葡萄糖刺激的GF胃酸分泌量,而吗啡则显著抑制;相反,在该试验中,皮啡肽和吗啡均增加了HP的胃酸分泌。胃泌素刺激的GF胃酸分泌不受吗啡影响,而皮啡肽则显著增强。在这些条件下,皮啡肽和吗啡使HP的胃酸分泌显著增加。在胃泌素刺激分泌期间给予纳洛酮和N-甲基左洛啡烷甲磺酸盐,显著抑制了GF和HP“本身”的胃酸分泌量,并阻止了皮啡肽和吗啡的刺激作用。皮啡肽和吗啡均显著增加了氨甲酰甲胆碱诱导的GF和HP的分泌。目前的结果表明,阿片类药物对犬胃酸分泌具有同时但相反的作用,并且μ受体参与了兴奋和抑制作用。与抑制作用(中枢性?)相反,兴奋作用似乎不是通过迷走神经途径(外周性?)介导的。阿片类拮抗剂对胃泌素刺激分泌的抑制作用表明外周阿片受体在胃酸分泌中具有生理作用。

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