Smith C F, Carter A
Arch Int Pharmacodyn Ther. 1986 Dec;284(2):181-92.
The effects of the delta-selective antagonist ICI 174864 and naltrexone on the dose-response curves to the mu-selective agonist RX 783006 and D-ala-D-leucine enkephalin (DADL) have been investigated in the rat isolated vas deferens preparation (RVD) set up in Krebs solution containing half the normal Ca++ concentration. The results obtained provide very strong evidence for the existence of both mu- and delta-receptors in this preparation. The Ke values of a number of opioid antagonists v. DADL in the RVD have been determined and compared to the Ke values obtained in the mouse vas deferens assay (MVD). The very good correlation (slope = 1.01, r = 0.98) obtained between the Ke values from the 2 preparations confirms the presence of a delta-receptor in the RVD.
在含有正常钙离子浓度一半的 Krebs 溶液中制备的大鼠离体输精管标本(RVD)中,研究了 δ 选择性拮抗剂 ICI 174864 和纳曲酮对 μ 选择性激动剂 RX 783006 和 D - 丙氨酸 - D - 亮氨酸脑啡肽(DADL)剂量反应曲线的影响。所获得的结果为该标本中同时存在 μ 和 δ 受体提供了非常有力的证据。已测定了多种阿片类拮抗剂与 RVD 中 DADL 的平衡解离常数(Ke)值,并与在小鼠输精管试验(MVD)中获得的 Ke 值进行比较。两种标本的 Ke 值之间获得的良好相关性(斜率 = 1.01,r = 0.98)证实了 RVD 中存在 δ 受体。