Moolten M S, Fishman J B, Chen J C, Carlson K R
Department of Pharmacology, University of Massachusetts Medical Center, Worcester 01655.
Life Sci. 1993;52(18):PL199-203. doi: 10.1016/0024-3205(93)90118-m.
Specific radioligand binding protocols were utilized to compare the affinity of morphine and the high-potency opioid etonitazene at mu 1, mu 2, delta, kappa 1 and sigma receptors. Both etonitazene and morphine displayed a mu 1-selective binding profile; however, etonitazene had a 2500-fold higher affinity at this receptor type. The latter result is consistent with the relative potencies or morphine and etonitazene in various behavioral tests.
采用特定的放射性配体结合实验方案,比较吗啡和高效阿片类药物依托尼秦对μ1、μ2、δ、κ1和σ受体的亲和力。依托尼秦和吗啡均呈现出μ1选择性结合模式;然而,依托尼秦对该受体类型的亲和力高2500倍。后一结果与吗啡和依托尼秦在各种行为测试中的相对效力一致。