Porreca F, Takemori A E, Sultana M, Portoghese P S, Bowen W D, Mosberg H I
Department of Pharmacology, University of Arizona Health Sciences Center, Tucson.
J Pharmacol Exp Ther. 1992 Oct;263(1):147-52.
Recently, subtypes of the opioid delta receptor have been identified. It is not known, however, if a subtype of opioid delta receptor can be associated with the known modulatory action of delta agonists on mu-mediated antinociception. Thus, the present study has used the delta subtype-selective antagonists, [D-Ala2,Leu5,Cys6]enkephalin (DALCE) (delta 1 antagonist) and naltrindole-5'-isothiocyanate (5'-NTII) (delta 2 antagonist) in an effort to determine whether the positive and negative modulation of morphine antinociception produced by opioid delta agonists was the result of activity at specific subtypes of opioid delta receptors. Intracerebroventricular morphine produced a dose-related antinociceptive effect which was not antagonized by coadministration of the delta antagonist, ICI 174,864, or by pretreatment 24 hr before testing with the DALCE or 5'-NTII. Coadministration with morphine of a nonantinociceptive dose of DPDPE or [D-Ala2,Glu4]deltorphin resulted in a leftward displacement of the morphine dose-effect curve (i.e., positive modulation), whereas coadministration of a nonantinociceptive dose of [Met5]enkephalin with morphine resulted in a rightward displacement of the morphine dose-effect curve (i.e., negative modulation). Both the positive and the negative modulatory actions were antagonized when the experiment was conducted in the presence of the delta antagonist, ICI 174,864, or when the mice were pretreated with the delta 2 antagonist, 5'-NTII. In contrast, pretreatment with the delta 1 antagonist, DALCE, failed to affect either the positive or the negative modulatory actions of these delta agonists on morphine antinociception. The data suggest the involvement of an opioid delta 2 receptor in the modulation of morphine antinociception.
最近,阿片δ受体的亚型已被鉴定出来。然而,尚不清楚阿片δ受体的某一亚型是否与δ激动剂对μ介导的镇痛作用的已知调节作用相关。因此,本研究使用了δ亚型选择性拮抗剂,[D - Ala2,Leu5,Cys6]脑啡肽(DALCE)(δ1拮抗剂)和纳曲吲哚 - 5'-异硫氰酸盐(5'-NTII)(δ2拮抗剂),以确定阿片δ激动剂对吗啡镇痛作用产生的正向和负向调节是否是阿片δ受体特定亚型活性的结果。脑室内注射吗啡产生了剂量相关的镇痛作用,该作用不会被δ拮抗剂ICI 174,864共同给药所拮抗,也不会被在测试前24小时用DALCE或5'-NTII预处理所拮抗。与吗啡共同给药非镇痛剂量的DPDPE或[D - Ala2,Glu4]强啡肽导致吗啡剂量 - 效应曲线向左移位(即正向调节),而与吗啡共同给药非镇痛剂量的[Met5]脑啡肽则导致吗啡剂量 - 效应曲线向右移位(即负向调节)。当在δ拮抗剂ICI 174,864存在下进行实验时,或者当小鼠用δ2拮抗剂5'-NTII预处理时,正向和负向调节作用均被拮抗。相比之下,用δ1拮抗剂DALCE预处理未能影响这些δ激动剂对吗啡镇痛作用的正向或负向调节作用。数据表明阿片δ2受体参与了吗啡镇痛作用的调节。