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[在重组干扰素存在的情况下,大鼠脑中阿片受体对μ和δ配体的特异性结合]

[Specific binding of mu- and delta-ligands by opiate receptors in the rat brain in the presence of reaferon].

作者信息

Panchenko L F, Aliab'eva T N, Petrichenko O B, Bumialis V V, Balashov A M

出版信息

Biull Eksp Biol Med. 1988 Sep;106(9):307-9.

PMID:2844322
Abstract

The ability of recombinant alpha 2-interferon (reaferon) to compete for opiate binding sites with mu- and delta-selective compounds was determined. Reaferon was found to inhibit the binding of 3H-D-ala2, D-leu5-enkephalin, and Ki value calculated was equal to 8.5 +/- 2.6 U.10(-3)/ml. The mu-agonists reception levels were decreased in the presence of reaferon at concentrations above 500 U/ml; the Ki values for 3H-morphine, 3H-dihydromorphine, 3H-RX 783006 were found to be 3.25 +/- 0.35, 4.28 +/- 0.81 and 6.51 +/- 1.27 U.10(-4)/ml, respectively. When reaferon was added into reaction medium at concentrations more than 5.10(3) U/ml the specific receptor binding of opiate antagonist 3H-naloxone was demonstrated to be increased and this effect was reversed with 100 mM NaCl. The existence of allosteric reaferon binding site which coupled with naloxone sensitive receptor was suggested to explain the results obtained.

摘要

测定了重组α2干扰素(重组干扰素)与μ和δ选择性化合物竞争阿片类结合位点的能力。发现重组干扰素能抑制3H-D-ala2、D-leu5-脑啡肽的结合,计算出的Ki值等于8.5±2.6 U·10(-3)/ml。在重组干扰素浓度高于500 U/ml时,μ激动剂的受体水平降低;发现3H-吗啡、3H-二氢吗啡、3H-RX 783006的Ki值分别为3.25±0.35、4.28±0.81和6.51±1.27 U·10(-4)/ml。当重组干扰素以高于5×10(3) U/ml的浓度加入反应介质中时,阿片类拮抗剂3H-纳洛酮的特异性受体结合被证明增加,且这种效应可被100 mM NaCl逆转。为了解释所得结果,提示存在与纳洛酮敏感受体偶联的变构重组干扰素结合位点。

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