Peers E, Shaw J S, Rance M J, Barnard E A
Neuropeptides. 1986 Nov-Dec;8(4):317-25. doi: 10.1016/0143-4179(86)90003-x.
The C-terminal chloromethyl ketone derivative of D-Ala2-Leu5-enkephalin (DALECK) has previously been shown to act as an affinity reagent at opioid receptors. The specificity of this derivative in its reversible interaction with functional opioid receptors has been examined here in a set of four field-stimulated isolated tissue preparations; the mouse, rat and rabbit vas deferens and the guinea pig ileum. Agonist potencies relative to selective reference agonists and Schild analysis were used to elucidate the overall activity of DALECK when interacting reversibly with opiate receptors under normal physiological conditions in the isolated tissue preparations. Under these conditions the ligand shows a very strong mu-selectivity. Data obtained in the guinea pig ileum suggest that DALECK is more potent than Tyr-D-Ala-Gly-N(CH3)Phe-Gly-ol (DAGO) when acting through mu-receptors. In contrast in the mouse vas deferens DALECK is at least 70-fold less potent than the delta-ligand D-Thr2-Leu5-enkephalin-Thr (DTLET). DALECK shows little interaction with kappa-receptors.
D - 丙氨酸2 - 亮氨酸5 - 脑啡肽（DALECK）的C末端氯甲基酮衍生物先前已被证明可作为阿片受体的亲和试剂。在此，我们在一组四种场刺激的离体组织标本中研究了该衍生物与功能性阿片受体可逆相互作用的特异性，这些标本包括小鼠、大鼠和兔的输精管以及豚鼠回肠。通过相对于选择性参考激动剂的激动剂效力和希尔德分析，来阐明在离体组织标本的正常生理条件下，DALECK与阿片受体可逆相互作用时的总体活性。在这些条件下，该配体表现出很强的μ选择性。在豚鼠回肠中获得的数据表明，当通过μ受体起作用时，DALECK比酪氨酸 - D - 丙氨酸 - 甘氨酸 - N（CH3）苯丙氨酸 - 甘氨酸醇（DAGO）更有效。相比之下，在小鼠输精管中，DALECK的效力比δ配体D - 苏氨酸2 - 亮氨酸5 - 脑啡肽 - 苏氨酸（DTLET）至少低70倍。DALECK与κ受体几乎没有相互作用。
