δ脑啡肽，酪氨酰-D-苏氨酰-甘氨酰-苯丙氨酰-亮氨酰-苏氨酸：一种新型高效且完全特异性的阿片δ受体激动剂。

Deltakephalin, Tyr-D-Thr-Gly-Phe-Leu-Thr: a new highly potent and fully specific agonist for opiate delta-receptors.

作者信息

Zajac J M, Gacel G, Petit F, Dodey P, Rossignol P, Roques B P

出版信息

Biochem Biophys Res Commun. 1983 Mar 16;111(2):390-7. doi: 10.1016/0006-291x(83)90318-2.

Abstract

Deltakephalin, Tyr-D-Thr-Gly-Phe-Leu-Thr (DTLET) was rationally designed as pure delta-probe from proposed models of mu and delta opiate receptors. On peripheral organs, deltakephalin displays a 3000 times higher inhibitory potency on the electrically stimulated mouse vas deferens (IC50 = 0.15 nM) as on the guinea pig ileum (IC50 = 460 nM). As expected [3H]deltakephalin interacts at 35 degrees C in rat brain tissue to a single class of binding sites (delta) (Bmax = 0.115 pmole/mg protein) with a high affinity: KD = 1.35 nM from equilibrium measurements and KD = 0.43 nM from kinetic determinations. Deltakephalin occurs as the most specific ligand for delta-binding sites as shown by the following discrimination ratios KI(mu)/KI(delta): 0.31 for D-Ala2-D-Leu5-enkephalin; 0.15 for D-Ser2-Thr6-Leu-enkephalin and 0.05 for deltakephalin.

摘要

强啡肽，酪氨酰-D-苏氨酰-甘氨酰-苯丙氨酰-亮氨酰-苏氨酸（DTLET）是根据μ和δ阿片受体的模型合理设计的纯δ探针。在周围器官上，强啡肽对电刺激的小鼠输精管的抑制效力（IC50 = 0.15 nM）比对豚鼠回肠的抑制效力（IC50 = 460 nM）高3000倍。正如预期的那样，[3H]强啡肽在35℃下与大鼠脑组织中的一类单一结合位点（δ）相互作用（Bmax = 0.115 pmol/mg蛋白质），具有高亲和力：通过平衡测量得出KD = 1.35 nM，通过动力学测定得出KD = 0.43 nM。如下所示的鉴别率KI（μ）/KI（δ）表明，强啡肽是δ结合位点最特异的配体：D-Ala2-D-Leu5-脑啡肽为0.31；D-Ser2-Thr6-亮氨酸-脑啡肽为0.15，强啡肽为0.05。