Samovilova N N, Prokazova N V
Vopr Med Khim. 1995 Sep-Oct;41(5):9-13.
Whether there is an endogenous ligand for sigma receptors remains unknown. A total lipid fraction was isolated from the porcine liver, which was then subjected to chromatographic separation, yielding nine chromatographic fractions eluated at various chloroform/methanol ratios: each fraction was tested for its capacity of inhibiting the binding of (+)-[3H]SKF 10047 to hepatic sigma-receptors. The chromatographic fraction 7 + 7A (eluated at chloroform/methanol ratios of 60:40-10:90) which consisted mainly of phospholipids was found to have the highest activity. However, a complex analysis of this fraction revealed no relationship of its sigma-inhibiting activity to phospholipids. It is suggested that the non-competitive inhibition of (+)-[3H]SKF 10047 binding by the isolated active fraction is due to its presence of an endogenous ligand which, interacting with sigma-2 receptor, allosterically inhibits the binding of the labelled (+)-benzomorphan.
σ受体是否存在内源性配体仍然未知。从猪肝中分离出总脂质部分，然后对其进行色谱分离，得到九个以不同氯仿/甲醇比例洗脱的色谱级分：测试了每个级分抑制(+)-[³H]SKF 10047与肝σ受体结合的能力。主要由磷脂组成的色谱级分7 + 7A（以60:40 - 10:90的氯仿/甲醇比例洗脱）被发现具有最高活性。然而，对该级分的复杂分析表明其σ抑制活性与磷脂没有关系。有人提出，分离出的活性级分对(+)-[³H]SKF 10047结合的非竞争性抑制是由于其存在内源性配体，该配体与σ-2受体相互作用，变构抑制标记的(+)-苯并吗啡烷的结合。
