[D-苏氨酸2，噻唑5]-和[D-蛋氨酸2，噻唑5]-脑啡肽酰胺的阿片受体结合活性

Opiate receptor-binding activity of [D-Thr2,Thz5]-and [D-Met2,Thz5]-enkephalinamides.

作者信息

Ferrara P, Li C H

出版信息

Eur J Pharmacol. 1981 Jul 17;73(1):69-73. doi: 10.1016/0014-2999(81)90146-1.

Abstract

The binding characteristics of two highly potent analgesic enkephalin analogs, [D-Thr2, Thz5]-and [D-Met2, Thz5]-enkephalinamide, to the rat brain membrane preparation have been investigated using tritiated Leu-enkephalin, human beta-endorphin or dihydromorphine as the primary ligand. Concentrations for 50% inhibiting activity of the enkephalin analogs are much lower in displacing tritiated dihydromorphine in comparison with that for the other two tritiated ligands. In addition, a correlation between analgesic potency and capacity to displace tritiated dihydromorphine is observed. These data may explain the high antinociceptive activity of the enkephalin analogs and support the hypothesis that the mu-receptor is involved with analgesia.

摘要

使用氚标记的亮氨酸脑啡肽、人β-内啡肽或二氢吗啡作为主要配体，研究了两种高效镇痛脑啡肽类似物[D-苏氨酸²，噻唑⁵]-和[D-蛋氨酸²，噻唑⁵]-脑啡肽酰胺与大鼠脑膜制剂的结合特性。与其他两种氚标记配体相比，脑啡肽类似物50%抑制活性的浓度在置换氚标记二氢吗啡时要低得多。此外，观察到镇痛效力与置换氚标记二氢吗啡的能力之间存在相关性。这些数据可能解释了脑啡肽类似物的高抗伤害感受活性，并支持μ-受体参与镇痛的假说。