Marastoni M, Tomatis R, Balboni G, Salvadori S, Lazarus L H
Department of Pharmaceutical Sciences, University of Ferrara, Italy.
Farmaco. 1991 Nov;46(11):1273-9.
The peptidase-resistance of deltorphins (DEL-A, H-Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2) and (DEL-C, H-Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2), highly selective and potent agonists of the delta opioid receptor, were investigated in vitro. DEL-C was fully resistant to degradation by rat plasma and strongly resistant to degradation by rat brain homogenates. DEL-A was cleaved with a half-life of 131.6 min upon incubation with plasma, and 57.4 min with rat brain homogenates. N-terminal truncated sequences of DEL-A and -C with free carboxyl groups, were also analyzed for receptor binding activity using [3H] DADLE for delta sites and [3H] DAGO for mu sites. The high enzymatic stability associated with deltorphins and their degradation products may make them prime candidates to characterize the role of delta-receptors in vivo.
在体外研究了强啡肽（DEL-A，H-Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2）和（DEL-C，H-Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2）的肽酶抗性，它们是δ阿片受体的高选择性和强效激动剂。DEL-C对大鼠血浆降解完全抗性，对大鼠脑匀浆降解具有强抗性。DEL-A与血浆孵育时的半衰期为131.6分钟，与大鼠脑匀浆孵育时为57.4分钟。还使用用于δ位点的[3H] DADLE和用于μ位点的[3H] DAGO分析了具有游离羧基的DEL-A和-C的N端截短序列的受体结合活性。强啡肽及其降解产物相关的高酶稳定性可能使它们成为表征δ受体在体内作用的主要候选物。
