Corbett A D, Gillan M G, Kosterlitz H W, McKnight A T, Paterson S J, Robson L E
Br J Pharmacol. 1984 Sep;83(1):271-9. doi: 10.1111/j.1476-5381.1984.tb10143.x.
The endogenous opioid ligands interact with more than one of the mu-, delta- and kappa-binding sites. By the use of binding assays and bioassays, enkephalin analogues have been assessed for their selectivity for binding at the delta-binding site and for their agonist and antagonist activities at the delta-receptor. The electrically-induced contractions of myenteric plexus-longitudinal muscle preparations of the guinea-pig ileum were inhibited by mu- and kappa-receptor ligands. Inhibitions were seen with mu-, delta- and kappa-receptor ligands in the mouse vas deferens, mainly with mu-receptor ligands in the rat vas deferens and only with kappa-receptor ligands in the rabbit vas deferens. From observations on a considerable number of [Leu5] enkephalin analogues, it has been concluded that [D-Pen2, D-Pen5] enkephalin and [D-Pen2, L-Pen5] enkephalin are the most selective delta-agonists and that N,N-diallyl-Tyr-Aib-Aib-Phe-Leu-OH is the most selective antagonist (Aib = alpha-aminoisobutyric acid). The binding of these peptides at the delta-site is 99% of the total binding. As to potency, the agonists are superior to the antagonists.
内源性阿片样物质配体与μ、δ和κ结合位点中的不止一个相互作用。通过结合测定和生物测定，已评估脑啡肽类似物在δ结合位点的结合选择性及其在δ受体上的激动剂和拮抗剂活性。豚鼠回肠肌间神经丛-纵肌标本的电诱导收缩受到μ和κ受体配体的抑制。在小鼠输精管中，μ、δ和κ受体配体均有抑制作用，在大鼠输精管中主要是μ受体配体起抑制作用，而在兔输精管中只有κ受体配体起抑制作用。通过对大量[亮氨酸5]脑啡肽类似物的观察得出结论，[D-青霉胺2，D-青霉胺5]脑啡肽和[D-青霉胺2，L-青霉胺5]脑啡肽是最具选择性的δ激动剂，而N，N-二烯丙基-Tyr-Aib-Aib-Phe-Leu-OH是最具选择性的拮抗剂（Aib=α-氨基异丁酸）。这些肽在δ位点的结合占总结合的99%。在效力方面，激动剂优于拮抗剂。
