Su T P, Weissman A D, Yeh S Y
Life Sci. 1986 Jun 16;38(24):2199-210. doi: 10.1016/0024-3205(86)90572-2.
Two endogenous ligands which interact preferentially with the sigma opioid receptors were identified from the guinea-pig brain extract in a Sephadex G-50 fractionation. These two ligands inhibited more potently the binding of [3H]SKF-10047 to sigma opioid receptors than [3H]naloxone to mu opioid receptors, [3H]ethylketocyclazocine to kappa opioid receptors and [3H]DADLE to delta opioid receptors. In the phencyclidine receptor assay, these two ligands were almost inactive. Incubation of these ligands with trypsin destroyed at least 50% of the activities in the sigma opioid receptor assay. Both ligands inhibited the sigma binding in a dose-dependent manner. The inhibition could be eliminated when the two ligands were removed from incubation media by extensive washings. It is therefore concluded that sigma opioid receptors are not phencyclidine receptors and that endogenous ligands for sigma opioid receptors may exist in the brain.
在葡聚糖凝胶G - 50分级分离过程中，从豚鼠脑提取物中鉴定出两种与σ阿片受体优先相互作用的内源性配体。与[³H]纳洛酮与μ阿片受体、[³H]乙基酮环唑辛与κ阿片受体以及[³H]DADLE与δ阿片受体的结合相比，这两种配体对[³H]SKF - 10047与σ阿片受体结合的抑制作用更强。在苯环己哌啶受体试验中，这两种配体几乎没有活性。用胰蛋白酶孵育这些配体，在σ阿片受体试验中至少破坏了50%的活性。两种配体均以剂量依赖的方式抑制σ结合。当通过大量洗涤从孵育介质中去除这两种配体时，抑制作用可以消除。因此得出结论，σ阿片受体不是苯环己哌啶受体，并且大脑中可能存在σ阿片受体的内源性配体。
