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两种μ型和δ型阿片样物质配体对大鼠丘脑腹侧基底复合体神经元对伤害性刺激反应的差异性抑郁作用。

Differential depressive action of two mu and delta opioid ligands on neuronal responses to noxious stimuli in the thalamic ventrobasal complex of rat.

作者信息

Benoist J M, Kayser V, Gacel G, Zajac J M, Gautron M, Roques B, Guilbaud G

出版信息

Brain Res. 1986 Nov 19;398(1):49-56. doi: 10.1016/0006-8993(86)91248-5.

Abstract

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.

摘要

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。

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