Takemori A E, Schwartz M M, Portoghese P S
Department of Pharmacology, Medical School, University of Minnesota, Minneapolis.
J Pharmacol Exp Ther. 1988 Dec;247(3):971-4.
The effects of nor-binaltorphimine (nor-BNI) and beta-funaltrexamine (beta-FNA) were studied on the diuretic activities in rats of several kappa opioid agonists including ethylketazocine, tifluadom, bremazocine and U50,488H. Nor-BNI suppressed the diuretic activity of all kappa agonists, whereas beta-FNA failed to alter the diuresis. On the other hand, beta-FNA treatment completely blocked the morphine-induced antidiuresis, whereas nor-BNI had no effect. The present data add further evidence that nor-BNI is a highly selective antagonist of kappa opioid agonists.
研究了去甲二氢吗啡酮(nor-BNI)和β-芬基曲马胺(β-FNA)对几种κ阿片受体激动剂(包括乙基酮佐辛、替氟朵、布瑞马佐辛和U50,488H)在大鼠体内利尿活性的影响。Nor-BNI抑制了所有κ激动剂的利尿活性,而β-FNA未能改变利尿作用。另一方面,β-FNA处理完全阻断了吗啡诱导的抗利尿作用,而nor-BNI则没有效果。目前的数据进一步证明nor-BNI是κ阿片受体激动剂的高度选择性拮抗剂。