Yeadon M, Kitchen I
Department of Biochemistry, University of Surrey, Guildford, U.K.
Neuropharmacology. 1988 Apr;27(4):345-8. doi: 10.1016/0028-3908(88)90141-4.
The comparative binding characteristics of the mu opioid receptor selective ligand [3H]-[D-Ala2-MePhe4-glyol5]enkephalin [( 3H]-DAGO) and of the delta receptor ligand [3H]-[D-Pen2, D-Pen5]enkephalin[( 3H]-DPDPE) have been studied in homogenates of both whole brain and of pons/medulla regions from the rat. The receptor affinities of five 4-anilinopiperidine drugs (fentanyl derivatives) and of morphine have been determined by inhibition studies, using [3H]-DAGO and [3H]-DPDPE as markers of the mu and delta opioid binding sites, respectively. The concentration of delta opioid sites in pons/medulla was found to be approximately one third that of mu sites. The concentrations of both mu and delta sites in whole brain were similar to that of mu sites in pons/medulla. The rank order of affinities of the unlabelled drugs was dissimilar at the mu and delta sites. The most potent fentanyl derivatives exhibited negligible preference for the mu or delta sites, in contrast to the least potent compound, alfentanil which showed an extremely high mu-site selectivity.
已在大鼠全脑匀浆以及脑桥/延髓区域匀浆中研究了μ阿片受体选择性配体[³H]-[D-Ala²-MePhe⁴-glyol⁵]脑啡肽([³H]-DAGO)和δ受体配体[³H]-[D-Pen², D-Pen⁵]脑啡肽([³H]-DPDPE)的比较结合特性。通过抑制研究确定了五种4-苯胺基哌啶药物（芬太尼衍生物）和吗啡的受体亲和力，分别使用[³H]-DAGO和[³H]-DPDPE作为μ和δ阿片结合位点的标志物。发现脑桥/延髓中δ阿片位点的浓度约为μ位点浓度的三分之一。全脑中μ和δ位点的浓度与脑桥/延髓中μ位点的浓度相似。未标记药物在μ和δ位点的亲和力排序不同。与效力最低的化合物阿芬太尼相比，效力最强的芬太尼衍生物对μ或δ位点的选择性可忽略不计，阿芬太尼表现出极高的μ位点选择性。
