Berzetei I P, Fong A, Duckles S P
Department of Pharmacology, College of Medicine, University of California, Irvine 92717.
NIDA Res Monogr. 1986;75:105-8.
Delta and kappa opioid receptors have been characterized in the central ear artery of the rabbit. The delta selective D-Pen2,D-Pen5-enkephalin and the highly selective delta antagonist ICI 174864 have been used for the delta opioid receptors. Ke values were determined and compared to that of the electrically stimulated mouse vas deferens preparation. In case of kappa opioid receptors, Dynorphin (1-13) and Ethylketazocine were used as agonists and Mr 2266 as kappa antagonist. Because of the relatively low selectivity of the kappa antagonist (it is only twice as active at the kappa than at the mu receptor sites) the Ke values obtained in the rabbit ear artery were compared to both the normal and beta-funaltrexamine treated vasa deferentia. In the rabbit ear artery, the Ke values of Mr 2266 were also determined in the presence of the delta selective antagonist ICI 174864. The Ke values for the delta receptors were close in the two assay systems, suggesting that the delta receptors have similar properties in rabbit ear artery and mouse vas deferens. As for the kappa receptors, the Ke values in the rabbit ear artery were not significantly different in the presence or absence of the delta antagonist compound, nor were they different from the Ke values obtained on the normal mouse vas deferens. However, they were significantly different from that of the beta-funaltrexamine treated mouse vas deferens. Further experiments need to be done to interpret the meaning of these results.
δ和κ阿片受体已在兔中耳动脉中得到表征。δ选择性的D- Pen2,D- Pen5 -脑啡肽以及高选择性的δ拮抗剂ICI 174864已被用于δ阿片受体研究。测定了平衡解离常数(Ke)值,并与电刺激小鼠输精管标本的Ke值进行比较。对于κ阿片受体,强啡肽(1 - 13)和乙基酮佐辛用作激动剂,Mr 2266用作κ拮抗剂。由于κ拮抗剂的选择性相对较低(其在κ受体位点的活性仅为μ受体位点的两倍),因此将兔耳动脉中获得的Ke值与正常和经β-氟纳曲胺处理的输精管的Ke值进行比较。在兔耳动脉中,还在存在δ选择性拮抗剂ICI 174864的情况下测定了Mr 2266的Ke值。两种测定系统中δ受体的Ke值相近,表明δ受体在兔耳动脉和小鼠输精管中具有相似的特性。至于κ受体,在存在或不存在δ拮抗剂化合物的情况下,兔耳动脉中的Ke值无显著差异,也与在正常小鼠输精管上获得的Ke值无差异。然而,它们与经β-氟纳曲胺处理的小鼠输精管的Ke值有显著差异。需要进行进一步的实验来解释这些结果的意义。