Portoghese P S, Lipkowski A W, Takemori A E
Life Sci. 1987 Mar 30;40(13):1287-92. doi: 10.1016/0024-3205(87)90585-6.
The opioid antagonist activities of two bivalent ligands, BNI and nor-BNI, have been evaluated in smooth muscle preparations and in mice. Both ligands are highly potent and selective as kappa opioid receptor antagonists, with relatively feeble blocking activity at mu and delta opioid receptors. BNI and nor-BNI represent the first highly selective kappa opioid receptor antagonists and should be of great utility as molecular probes for identifying the interaction of agonist ligands with kappa opioid receptors in vitro and in vivo.
两种二价配体BNI和去甲BNI的阿片样物质拮抗剂活性已在平滑肌制剂和小鼠中进行了评估。两种配体作为κ阿片样物质受体拮抗剂都具有高效力和选择性，对μ和δ阿片样物质受体的阻断活性相对较弱。BNI和去甲BNI是首批高选择性κ阿片样物质受体拮抗剂，作为分子探针，在体外和体内鉴定激动剂配体与κ阿片样物质受体的相互作用方面应具有很大用途。
