Characterization of solubilized human and rat brain beta-endorphin-receptor complex.
Characterization of solubilized human and rat brain beta-endorphin-receptor complex.
复制标题
溶解的人和大鼠脑 β-内啡肽受体复合物的表征。
DOI：
10.1073/pnas.83.1.67
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发表时间：
1986
影响因子：
11.1
通讯作者：
Li,CH
中科院分区：
文献类型：
--
作者：
Helmeste,DM;Li,CH
阿片受体已从人纹状体和大鼠全脑膜溶解的3-[（3-胆酰胺丙基）二甲基铵]-1-丙磺酸（CHAPS）的使用。氚标记的人β-内啡肽（3 H-β h-EP）结合揭示了吗啡，纳洛酮和各种β-EP类似物的高亲和力竞争，表明主要是μ型结合。缺乏（+/-）-3，4-二氯-N-甲基-N-[2-（1-吡咯烷基）环己基]苯乙酰胺甲磺酸盐（U 50 -488，Upjohn）的高亲和力竞争，表明在这些条件下κ位点未被3 H-β h-EP标记。除了[Met]脑啡肽外，可溶性和膜制剂的亲和力相似，脑啡肽似乎被溶解的提取物迅速降解。通过排阻色谱法揭示了人和大鼠溶解的3 H-β h-EP-受体复合物之间的大小差异。
Opioid receptors have been solubilized from human striatal and rat whole-brain membranes by use of 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate (CHAPS). Tritiated human beta-endorphin (3H-beta h-EP) binding revealed high-affinity competition by morphine, naloxone, and various beta-EP analogues, suggesting predominantly mu-type binding. Lack of high-affinity competition by (+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneaceta mide methanesulfonate (U50-488, Upjohn) indicated that kappa sites were not labeled by 3H-beta h-EP under these conditions. Affinities were similar in both soluble and membrane preparations except for [Met]enkephalin, which appears to be rapidly degraded by the solubilized extract. Size differences between human and rat solubilized 3H-beta h-EP-receptor complexes were revealed by exclusion chromatography.