大鼠脑中β-内啡肽受体的特性与定位

Properties and localization of beta-endorphin receptor in rat brain.

作者信息

Law P Y, Loh H H, Li C H

出版信息

Proc Natl Acad Sci U S A. 1979 Nov;76(11):5455-9. doi: 10.1073/pnas.76.11.5455.

DOI:10.1073/pnas.76.11.5455

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC411667/

Abstract

Stereospecific high-affinity binding sites for beta h-[3H]endorphin could be demonstrated in the P2 pellet of rat brain homogenate. Scatchard analysis of the binding data revealed binding sites with Kd values of 0.81 and 6.8 nM and density of 120 and 240 fmol/mg of protein. Distribution of beta h-[3H]endorphin binding in various brain regions parallels that of opiate receptor:striatum greater than thalamus greater than amygdala greater than hypothalamus, septum greater than cortex greater than midbrain, brainstem. Similar to their effect on 3H-labeled agonist binding, Na+ and other monovalent cations, GTP, trypsin, chymotrypsin, phospholipase A2, and N-ethylmaleimide all inhibited the specific binding of beta h-[3H]endorphin. In contrast to their action on alkaloid and enkephalin binding, Ca2+, Mg2+, and Mn2+ also inhibited beta h-[3H]endorphin binding. These data suggest a difference between beta h-endorphin and alkaloid/enkephalin binding sites.

摘要

在大鼠脑匀浆的P2沉淀中可证实存在βh-[³H]内啡肽的立体特异性高亲和力结合位点。对结合数据进行Scatchard分析显示，结合位点的解离常数（Kd）值分别为0.81和6.8 nM，蛋白质密度为120和240 fmol/mg。βh-[³H]内啡肽在不同脑区的结合分布与阿片受体相似：纹状体＞丘脑＞杏仁核＞下丘脑，隔区＞皮层＞中脑、脑干。与它们对³H标记激动剂结合的影响相似，Na⁺和其他单价阳离子、GTP、胰蛋白酶、糜蛋白酶、磷脂酶A2和N-乙基马来酰亚胺均抑制βh-[³H]内啡肽的特异性结合。与它们对生物碱和脑啡肽结合的作用相反，Ca²⁺、Mg²⁺和Mn²⁺也抑制βh-[³H]内啡肽的结合。这些数据表明βh-内啡肽与生物碱/脑啡肽结合位点之间存在差异。

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Electron affinity of the methyl radical: Structures of CH(3) and CH(3)-.甲基自由基的电子亲和势：CH₃和CH₃⁻的结构

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Proc Natl Acad Sci U S A. 1975 Jun;72(6):2404-7. doi: 10.1073/pnas.72.6.2404.

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(D-Ala2)-Met-enkephalinamide: a potent, long-lasting synthetic pentapeptide analgesic.（D-丙氨酸2）-甲硫氨酸脑啡肽酰胺：一种强效、长效的合成五肽镇痛药。

Science. 1976 Oct 15;194(4262):330-2. doi: 10.1126/science.968485.

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Comparative study on analgesic effect of Met5-enkephalin and related lipotropin fragments.蛋氨酸脑啡肽及相关促脂解素片段镇痛作用的比较研究

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