Kachur J F, Miller R J
Eur J Pharmacol. 1982 Jul 9;81(2):177-83. doi: 10.1016/0014-2999(82)90435-6.
Several opioid peptides and narcotic drugs reduced transepithelial potential difference (PD) and short circuit current (Isc) in guinea-pig ileal mucosa measured in vitro in Ussing chambers. [D-Ala2,D-Leu5]enkephalin was the most potent peptide tested. Enkephalin analogues with altered C-terminal amino acids were less potent, as were beta-endorphin and dermorphin. Etorphine produced potent effects whereas morphine and SKF 10,047 were inactive. Ethylketazocine produced a biphasic dose-response curve. When added by themselves diprenorphine and naloxone produced small increases in Isc. This effect was not seen when Cl- and HCO3- in the Ringer were replaced by SO42-. Diprenorphine and naloxone were able to shift the dose response curves for all agonists to the right, with the exception of that for ethylketazocine. Diprenorphine was a more potent antagonist than naloxone. SKF 10,047 also acted as a pure antagonist. Morphine and ethylketazocine had no antagonist effects. It is concluded that the opiate receptor in the guinea-pig ileal mucosa is similar to a delta-opiate receptor as defined by ligand binding studies, but that some differences also exist.
几种阿片肽和麻醉药物降低了在乌斯琴氏小室中体外测量的豚鼠回肠粘膜的跨上皮电位差（PD）和短路电流（Isc）。[D-丙氨酸2，D-亮氨酸5]脑啡肽是所测试的最有效的肽。C末端氨基酸改变的脑啡肽类似物活性较低，β-内啡肽和强啡肽也是如此。埃托啡产生强效作用，而吗啡和SKF 10,047无活性。乙基酮唑辛产生双相剂量反应曲线。单独添加时，二丙诺啡和纳洛酮使Isc略有增加。当林格氏液中的Cl-和HCO3-被SO42-取代时，未观察到这种效应。二丙诺啡和纳洛酮能够将所有激动剂的剂量反应曲线向右移动，但乙基酮唑辛除外。二丙诺啡是比纳洛酮更有效的拮抗剂。SKF 10,047也作为纯拮抗剂起作用。吗啡和乙基酮唑辛没有拮抗作用。结论是，豚鼠回肠粘膜中的阿片受体与配体结合研究定义的δ-阿片受体相似，但也存在一些差异。
