Berzetei I P, Fong A, Yamamura H I, Duckles S P
Department of Pharmacology, College of Medicine, University of California, Irvine 92717.
Eur J Pharmacol. 1988 Jul 14;151(3):449-55. doi: 10.1016/0014-2999(88)90542-0.
Quantitative characterization of the kappa opioid receptor in the rabbit ear artery was carried out using three kappa-selective agonist compounds, dynorphin-(1-13), U-69593 and ethylketocyclazocine. Kinetic analysis was performed using the antagonist, MR 2266. Two other in vitro preparations were studied for comparison: the mouse was deferens and rabbit was deferens. To avoid mu receptor action in the mouse was deferens the irreversible mu receptor antagonist, beta-funaltrexamine, was used. It was demonstrated that, using the highly selective kappa agonist compound U-69593, Ke values for MR 2266 obtained in the three assay systems were not significantly different. These results suggest that kappa receptors present in these three tissues share identical properties.
使用三种κ-选择性激动剂化合物强啡肽-(1-13)、U-69593和乙基酮环唑辛对兔耳动脉中的κ阿片受体进行了定量表征。使用拮抗剂MR 2266进行动力学分析。为作比较研究了另外两种体外制剂:小鼠输精管和兔输精管。为避免小鼠输精管中μ受体的作用,使用了不可逆的μ受体拮抗剂β-芬太尼。结果表明,使用高选择性κ激动剂化合物U-69593时,在这三种测定系统中获得的MR 2266的Ke值无显著差异。这些结果表明,这三种组织中存在的κ受体具有相同的特性。