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关于人胎盘阿片受体的生化与药理学研究。

Biochemical and pharmacological studies on the opiate receptors from human placenta.

作者信息

Ahmed M S, Abdelhamid E E, Turner D

出版信息

Life Sci. 1983;33 Suppl 1:207-10. doi: 10.1016/0024-3205(83)90479-4.

Abstract

The effect of different enzymatic treatments on the specific binding of 3H-Etorphine to the membrane bound opiate receptors from human placenta was studied. Phospholipase A2 inhibited etorphine binding, suggesting either that phospholipids are essential for ligand binding or that products of the phospholipase A2 reaction, either lysophospholipids or fatty acids, disrupt the membrane integrity because of their detergent like properties. Trypsin and alpha-chymotrypsin had no effect, suggesting that the receptors binding site was not accessible to these proteolytic enzymes. We also find that the placental villus upon in vitro stimulation with potassium releases acetylcholine. The inhibitory effect of morphine on acetylcholine release was investigated.

摘要

研究了不同酶处理对3H-埃托啡与人胎盘膜结合阿片受体特异性结合的影响。磷脂酶A2抑制埃托啡结合,这表明磷脂对于配体结合至关重要,或者磷脂酶A2反应的产物,即溶血磷脂或脂肪酸,因其类似去污剂的性质而破坏膜的完整性。胰蛋白酶和α-糜蛋白酶没有作用,这表明这些蛋白水解酶无法接近受体结合位点。我们还发现,体外经钾刺激后胎盘绒毛会释放乙酰胆碱。研究了吗啡对乙酰胆碱释放的抑制作用。

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