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某些阿片类五肽类似物的体外概况

In vitro profile of some opioid pentapeptide analogues.

作者信息

Shaw J S, Turnbull M J

出版信息

Eur J Pharmacol. 1978 Jun 1;49(3):313-7. doi: 10.1016/0014-2999(78)90109-7.

Abstract

The opiate agonist potency of thirteen synthetic enkephalin pentapeptides has been examined on the electrically stimulated guinea pig ileum and mouse vas deferens preparations in comparison with methionine and leucine enkephalins, beta-endorphin and normorphine. Their antagonism by naloxone (Ke) was also assessed on each preparation. Our findings are compatible with, and are discussed in the context of, the hypothesis that these preparations possess at least two populations of receptors.

摘要

已对13种合成脑啡肽五肽在电刺激豚鼠回肠和小鼠输精管制剂上的阿片激动剂效力进行了检测,并与甲硫氨酸脑啡肽、亮氨酸脑啡肽、β-内啡肽和去甲吗啡作了比较。还在每种制剂上评估了纳洛酮(Ke)对它们的拮抗作用。我们的研究结果与这些制剂至少具有两类受体的假说相符,并在此背景下进行了讨论。

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