Benoist J M, Kayser V, Gacel G, Zajac J M, Gautron M, Roques B, Guilbaud G
Brain Res. 1986 Nov 19;398(1):49-56. doi: 10.1016/0006-8993(86)91248-5.
In the present investigation the effects of selective agonists for mu (Tyr-D-Ala-Me-Phe-Gly-ol (DAGO)) and delta (Tyr-D-Thr-Gly-Phe-Leu-Thr (DTLET)) opioid receptors on neuronal activities induced by noxious cutaneous stimuli in the rat ventrobasal (VB) thalamus were analyzed. The two agonists produced a clear depressive action on thermal as well as mechanical noxious stimuli. The depressive action of DTLET (3 mg/kg i.v.) was lower and of shorter duration than that of DAGO (2 mg/kg i.v.). However, this effect is unambiguously related to the selective stimulation of opioid receptors since a consistent effect was also observed for a dose as low as 1.5 mg/kg i.v. of DTLET. Moreover, DTLET effect needs a high concentration of naloxone (0.5 mg/kg i.v.) to be reversed, while DAGO effect is totally reversed with 0.1 mg/kg i.v.
在本研究中，分析了μ阿片受体选择性激动剂（酪氨酰-D-丙氨酰-甲基苯丙氨酰-甘氨醇（DAGO））和δ阿片受体选择性激动剂（酪氨酰-D-苏氨酰-甘氨酰-苯丙氨酰-亮氨酰-苏氨酸（DTLET））对大鼠腹侧基底（VB）丘脑由伤害性皮肤刺激诱导的神经元活动的影响。这两种激动剂对热和机械伤害性刺激均产生明显的抑制作用。DTLET（静脉注射3mg/kg）的抑制作用比DAGO（静脉注射2mg/kg）弱且持续时间短。然而，这种效应明确与阿片受体的选择性刺激有关，因为静脉注射低至1.5mg/kg的DTLET也观察到了一致的效应。此外，DTLET的效应需要高浓度的纳洛酮（静脉注射0.5mg/kg）才能逆转，而DAGO的效应静脉注射0.1mg/kg就能完全逆转。
