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二苯甲酰硫胺可增强μ和δ阿片受体激动剂对背角神经元活动的抑制作用。

Depressive effects of mu and delta opioid receptor agonists on activities of dorsal horn neurones are enhanced by dibencozide.

作者信息

Villanueva L, Bing Z, Bouhassira D, Le Bars D

机构信息

Institut National de la Santé et de la Recherche Médicale U 161, Paris, France.

出版信息

J Pharmacol Exp Ther. 1991 Jun;257(3):1198-202.

PMID:1646326
Abstract

The effects on C fiber evoked activity in lumbar dorsal horn convergent neurones of i.v. morphine alone, of Tyr-D-Thr-Gly-Phe-Leu-Thr (DTLET) alone or of either of these drugs in association with 5-deoxyadenosylcobalamine (dibencozide) were investigated in anesthetized rats. Both morphine and DTLET depressed the neuronal responses in a dose-related fashion, with the former requiring lower doses. Although dibencozide alone was devoid of any effect, it significantly enhanced the depressive effects of all doses of morphine tested and of the lower two doses of DTLET. It is concluded that dibencozide enhances the spinal depression of nociceptive information elicited by mu and delta opioid agonists. This drug could provide a useful tool for the study of interactions between opioids and opioids receptors. It is also suggested that dibencozide could be useful in clinical practice for reducing the dosage of opioids.

摘要

在麻醉大鼠中,研究了静脉注射吗啡单独使用、酪氨酰-D-苏氨酰-甘氨酰-苯丙氨酰-亮氨酰-苏氨酸(DTLET)单独使用或这两种药物中的任何一种与5-脱氧腺苷钴胺素(二苯酰辅酶)联合使用对腰段背角汇聚神经元中C纤维诱发活动的影响。吗啡和DTLET均以剂量相关的方式抑制神经元反应,前者所需剂量较低。虽然单独使用二苯酰辅酶没有任何作用,但它显著增强了所有测试剂量吗啡以及较低的两个剂量DTLET的抑制作用。得出的结论是,二苯酰辅酶增强了由μ和δ阿片样激动剂引起的伤害性信息的脊髓抑制作用。这种药物可为研究阿片类药物与阿片受体之间的相互作用提供有用的工具。还表明二苯酰辅酶在临床实践中可能有助于减少阿片类药物的用量。

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Depressive effects of mu and delta opioid receptor agonists on activities of dorsal horn neurones are enhanced by dibencozide.二苯甲酰硫胺可增强μ和δ阿片受体激动剂对背角神经元活动的抑制作用。
J Pharmacol Exp Ther. 1991 Jun;257(3):1198-202.
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