K-Ⅱ和U-50488H对κ阿片受体亲和力的比较  

COMPARATIVE STUDIES ON THE AFFINITIES OF K-Ⅱ AND U-50488H FOR KAPPA OPIATE RECEPTOR

作　　者：李建国[1] 马斯才 陆苏南[1] 王崇铨 

机构地区：[1]北京药物化学研究所,北京102205

出　　处：《药学学报》1991年第1期10-14,共5页Acta Pharmaceutica Sinica

摘　　要：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-pyrrolinyi)-cyclohexyl] benzenacetamide hydrochloride (K-Ⅱ) is a novel analogue of U-50488H. Previous studies have demonstrated that K-Ⅱ is more potent than U-50488H in analgesic activity in mice and in inhibitory effect on electrically induced contractions of the isolated rabbit vas deferens. In this paper, we determined the affinities of K-Ⅱ and U-50488H for kappa opiate receptor in guinea pig cerebellum and frontal cortex using radioreceptor binding assay (saturation studies and competition studies), and calculated Ki values of K-Ⅱ and U - 50488H by the Cheng - Prusoff equation. The results indicate that the affinity of K-Ⅱ for kappa opiate receptor is 6～42 times greater than that of U - 50488H. The selectivity of K-Ⅱ for opiate receptor subtypes is being studied.

关 键 词：K-Ⅱ U-50488H K阿片受体 

分 类 号：R966[医药卫生—药理学]