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离体生物实验和小鼠在体实验已证实两个双价配基Binaltorphimine(BNI)相nor-Binaltorphimine(nor-BNI)为强效高选择性k-阿片受体拮抗剂,它们对μ-和δ-阿片受体的拮抗效应很弱,可以作为研究激动剂和k-阿片受体相互作用的有效工具药.BNI和nor-BNI在豚鼠迥肠纵肌(GPI)和小鼠输精管(MVD)上具有独特的阿片拮抗剂活性.在GPI上,这两个配基对k-激动剂如:乙基酮唑新(EKC)、U-50488H和Dynorphine(1-17)显示强的拮抗效应,且BNI比nor-BNI强,但对μ-激动剂吗啡只表现弱的拮抗效应.在MVD上,BNI和nor-BNI不影响吗啡
In vitro and in vivo experiments in mice have demonstrated that two bivalent ligands, the Binaltorphimine (BNI) phase nor-Binaltorphimine (nor-BNI), are potent and highly selective k-opioid receptor antagonists that antagonize μ- and The antagonism of δ-opioid receptor is very weak and can be used as an effective tool to study the interaction between agonist and k-opioid receptor.NGI and nor-BNI play an important role in the process of GPI and MVD in guinea pigs, Have unique antagonist activity at GPI.While GPIs exhibit potent antagonistic effects on k-agonists such as EKC, U-50488H and Dynorphine (1-17) And BNI was stronger than nor-BNI, but showed only a weak antagonistic effect on the mu-agonist morphine.MnI and nor-BNI did not affect morphine on MVD