Maliukova I V, Zakharova L A, Metaksa E E
Biokhimiia. 1996 Mar;61(3):440-4.
The naloxone-dependent modulating effect of synthetic analogs of myelopeptides, MP1 and MP2, on pain sensitivity in mice was determined at doses 10(-13) and 10(-8) g/animal. Binding of the peptides to opioid receptors of mouse brain membranes was studied by the radioligand assay. For MP1, the displacement of [3H]DAGO (selective mu-agonist) by IC50 = 7.3 x 10(-5) M and [3H]DSLET (selective delta-agonist) with IC50 = 7.0 x 10(-5) M. The data obtained suggest that the hypoalgesic effect of the peptides cannot be due to their direct interaction with opioid receptors. However, the naloxone dependence provides a possibility of mediated involvement of the opioidergic system in the realization of this effect.
在剂量为10(-13)和10(-8)克/动物时，测定了骨髓肽MP1和MP2的合成类似物对小鼠痛觉敏感性的纳洛酮依赖性调节作用。通过放射性配体分析法研究了这些肽与小鼠脑膜阿片受体的结合。对于MP1，[3H]DAGO（选择性μ激动剂）的IC50为7.3×10(-5)M，[3H]DSLET（选择性δ激动剂）的IC50为7.0×10(-5)M时可将其置换。所得数据表明，这些肽的镇痛作用并非由于它们与阿片受体的直接相互作用。然而，纳洛酮依赖性为阿片能系统介导参与这一作用的实现提供了可能性。
