阿片肽、脑啡肽和内啡肽的体外药理学。

In vitro pharmacology of the opioid peptides, enkephalins and endorphins.

作者信息

Waterfield A A, Smokcum R W, Hughes J, Kosterlitz H W, Henderson G

出版信息

Eur J Pharmacol. 1977 May 15;43(2):107-16. doi: 10.1016/0014-2999(77)90123-6.

Abstract

In the guinea-pig ileum methionine-enkephalin, normorphine and morphine are equipotent in depressing electrically evoked contractions; leucine-enkephalin has about 25% of the activity. The mouse vas deferens is more sensitive to the enkephalins which are 30 to 60 times more potent than morphine. Fragments of beta-lipotropin61-91 (beta-endorphin) having sequences up to LPH76 are more potent in the mouse vas deferens than in the guinea-pig ileum but beta-endorphin is about equipotent in the two preparations. None of the peptides has antagonist activity. Methionine-enkephalin and normorphine are equipotent in inhibiting [3H]-naloxone binding by homogenate of guinea-pig brain in the absence of Na+ while leucine-enkephalin has only 25% of this activity. In the guinea-pig ileum, naloxone antagonises normorhine and the enkephalins equally well whereas in the mouse vas deferens about ten times more naloxone is required for the enkophalins that for normorphine. Methionine-enkephalin depresses output of acetylcholine in the guinea-pig ileum and of noradrenaline in the mouse vas deferens.

摘要

在豚鼠回肠中，甲硫氨酸脑啡肽、去甲吗啡和吗啡在抑制电诱发收缩方面具有同等效力；亮氨酸脑啡肽的活性约为它们的25%。小鼠输精管对脑啡肽更为敏感，脑啡肽的效力比吗啡强30至60倍。β-促脂素61 - 91片段（β-内啡肽），其序列至LPH76，在小鼠输精管中比在豚鼠回肠中更有效，但β-内啡肽在这两种制剂中的效力大致相当。这些肽均无拮抗活性。在无钠离子存在的情况下，甲硫氨酸脑啡肽和去甲吗啡在抑制豚鼠脑匀浆与[³H] - 纳洛酮的结合方面具有同等效力，而亮氨酸脑啡肽的这种活性仅为它们的25%。在豚鼠回肠中，纳洛酮对去甲吗啡和脑啡肽的拮抗作用同样有效，而在小鼠输精管中，脑啡肽所需的纳洛酮量约为去甲吗啡的十倍。甲硫氨酸脑啡肽可抑制豚鼠回肠中乙酰胆碱的释放以及小鼠输精管中去甲肾上腺素的释放。