Pfeiffer A, Herz A
Eur J Pharmacol. 1982 Feb 5;77(4):359-61. doi: 10.1016/0014-2999(82)90145-5.
The interaction of the delta-opiate agonist [D-Ala2,D]Leu5]enkephalin (DADL) with the mu-opiate ligands dihydromorphine (DHM) and naloxone and the kappa-opiate ligand ethylketocyclazocine (EK) was studied in rat diencephalic membranes which contain mainly mu-opiate binding sites. Saturation binding experiments performed with tritiated DADL in the presence of DHM and naloxone were indicative of mixed type inhibition whereas EK behaved as a competitive inhibitor. This result indicates differences in the interaction of mu-, delta- and kappa-ligands with mu-opiate binding sites.
在主要含有μ-阿片受体结合位点的大鼠间脑细胞膜中，研究了δ-阿片激动剂[D-丙氨酸2，D-亮氨酸5]脑啡肽（DADL）与μ-阿片配体二氢吗啡（DHM）、纳洛酮以及κ-阿片配体乙基酮环唑辛（EK）之间的相互作用。在DHM和纳洛酮存在的情况下，用氚标记的DADL进行的饱和结合实验表明为混合型抑制，而EK表现为竞争性抑制剂。这一结果表明μ-、δ-和κ-配体与μ-阿片受体结合位点相互作用存在差异。
