δ-阿片受体激动剂对克隆的人δ-阿片受体的相对效能

Relative efficacies of delta-opioid receptor agonists at the cloned human delta-opioid receptor.

作者信息

Quock R M, Hosohata Y, Knapp R J, Burkey T H, Hosohata K, Zhang X, Rice K C, Nagase H, Hruby V J, Porreca F, Roeske W R, Yamamura H I

机构信息

Department of Pharmacology, University of Arizona, Tucson 85724, USA.

出版信息

Eur J Pharmacol. 1997 May 12;326(1):101-4. doi: 10.1016/s0014-2999(97)83488-7.

DOI:10.1016/s0014-2999(97)83488-7

PMID:9178661

Abstract

The present study was conducted to determine the relative efficacies of the selective delta-opioid receptor agonists SNC80 ((+)-4-[(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl )-3-methoxybenzyl]-N,N-diethylbenzamide), pCl-DPDPE (cyclic[D-Pen2,4'-ClPhe4,D-Pen5]enkephalin) and (-)-TAN67 ((-)-2-methyl-4a alpha-(3-hydroxyphenyl)-1,2,3,4,4a,5,12,12a alpha-octahydro-quinolino-[2,3,3-g]isoquinoline). Experiments compared the abilities of the three drugs to competitively inhibit [3H]naltrindole binding and also stimulate [35S]GTPgammaS binding in membranes prepared from stably transfected Chinese hamster ovary (CHO) cells that express the cloned human delta-opioid receptor. Efficacy was determined according to the formula: efficacy = (E(max-A)/Emax)(A'/A + 1) X 0.5. Results show that SNC80 and pCl-DPDPE had efficacy values that were about 6-7 times greater than that of (-)-TAN67.

摘要

本研究旨在确定选择性δ-阿片受体激动剂SNC80（(+)-4-[(αR)-α-((2S,5R)-4-烯丙基-2,5-二甲基-1-哌嗪基)-3-甲氧基苄基]-N,N-二乙苯甲酰胺）、对氯-DPDPE（环[D-青霉胺2,4'-氯苯丙氨酸4,D-青霉胺5]脑啡肽）和(-)-TAN67（(-)-2-甲基-4aα-(3-羟基苯基)-1,2,3,4,4a,5,12,12aα-八氢喹啉并-[2,3,3-g]异喹啉）的相对效力。实验比较了这三种药物竞争性抑制[3H]纳曲吲哚结合以及刺激稳定转染表达克隆人δ-阿片受体的中国仓鼠卵巢（CHO）细胞膜中[35S]GTPγS结合的能力。效力根据以下公式确定：效力 = (E(max - A)/Emax)(A'/A + 1)×0.5。结果表明，SNC80和对氯-DPDPE的效力值比(-)-TAN67大约高6 - 7倍。