新合成阿片受体配基对δ受体的激动作用

Effect of new synthesized opioid receptor ligands stimulate δ receptor

研究新合成的阿片受体配基对δ阿片受体的激动作用。采用生物鉴定的方法 ,检测新型阿片受体配基、DP DPE和吗啡对小白鼠输精管 (MVD)收缩的抑制作用和检测所激动的阿片受体亚型 ,以达到最大抑制作用的 5 0 %的药物浓度 (IC50 值 )评价效价强度。结果表明新型阿片受体配基、DPDPE和吗啡 (Mor)都可抑制MVD的电刺激收缩 ,显示纯激动剂作用。认为新型阿片受体配基与阿片受体的结合为可逆性结合。新型阿片受体配基A、C、D、E、F和G以及典型的阿片受体激动剂DPDPE和吗啡的IC50 值分别为 31 73± 3 5 4、15 92± 9 19、88 70± 16 2 6、10 74 0 0± 2 6 3 0 0、74 88± 5 8 6 9和 6 7 16± 8 4 9、3 2 0± 0 0 5、6 9 84± 2 7 5 8nmol L。竞争性拮抗剂纳洛酮 (Nal)可拮抗配基的激动作用 ,使新型阿片受体配基 ,DPDPE和吗啡的量效曲线平行右移。新型阿片受体配基可激动δ阿片受体 。

To determine the function of new opioid receptor ligands and onδopioid receptor. The effect of opioid receptor ligands on electrical stimulation induced contraction of mouse vas deferens (MVD) was used to determine the potency of the ligands and the value of IC 50 . The new opioid receptor ligands, DPDPE and Morphine inhibited electrical stimulation induced contraction of MVD as pure agonists and the effect could be reversed by opioid receptor antagonist naloxone. The IC 50 of new ligands A?C?D?E?F?G?DPDPE and morphine were 31.73±3.54?15.92±9.19?88.70±16.26?1074 00±263.00?74.88±58.69 and 67.16±8.49?3.20±0.05?69.84±27.58 nmol/L, respectively. In the presence of the competitive antagonist naloxone, all the dose response curves of new ligands shifted to the right. All the new opioid receptor ligands stimulated δ opioid receptor as a typical agonist.