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3,4-二氯-N-甲基-N-[反式-2-(1-△~3-吡咯啉基)环己基]苯乙酰胺(K-Ⅱ)是新合成的U-50488H类似物,其对小鼠的镇痛效应和对离体兔输精管的抑制作用均比U-50488H强。本文用放射受体结合试验方法对这两种化合物在富含x阿片受体的豚鼠小脑和大脑皮层前叶上的亲和力进行了比较,并求出这两种化合物的Ki值.结果表明K-Ⅱ对k阿片受体的亲和力比U-50488H强6～42倍。K-Ⅱ对阿片受体亚型选择性比较研究正在进行中。
3,4-Dichloro-N-methyl-N- [trans-2- (1-Δ 3 -pyrrolinyl) cyclohexyl] benzeneacetamide (K-II) is a newly synthesized U-50488H Its analgesic effect on mice and the inhibitory effect on vas deferens in isolated rabbits are stronger than that of U-50488H. In this paper, the binding affinity of these two compounds in the anterior lobe of cerebellar and cerebral cortex of x-opiate-rich guinea pigs was compared by radioligand binding assay and the Ki values of the two compounds were calculated.The results showed that K- Ⅱ k opioid receptor affinity than U-50488H 6 to 42 times stronger. Selective comparison of opioid receptor subtypes with K-II is underway.