去甲丙咪嗪对α-肾上腺素能受体激动剂镇痛活性的影响：一种去甲肾上腺素能摄取的选择性抑制剂。

Modification of alpha-adrenoceptor agonist antinociceptive activity by nisoxetine: a selective inhibitor of noradrenergic uptake.

作者信息

Hynes M D, Henderson J K

出版信息

Pharmacol Biochem Behav. 1984 Mar;20(3):463-6. doi: 10.1016/0091-3057(84)90286-7.

Abstract

The alpha-adrenoceptor agonists, clonidine and xylazine, produced a dose-dependent antinociceptive effect in the mouse writhing assay as does morphine. Fluoxetine, a highly-specific inhibitor of serotonin uptake, enhanced the antinociceptive effect of morphine in this test but not that of clonidine or xylazine. In contrast, nisoxetine, a selective inhibitor of noradrenergic uptake, significantly potentiated the antinociceptive activity of morphine, clonidine, and xylazine. These findings strengthen the evidence for an involvement of a noradrenergic mechanism in the antinociceptive effects of alpha-adrenoceptor agonists.

摘要

α-肾上腺素能受体激动剂可乐定和赛拉嗪在小鼠扭体试验中产生了与吗啡一样的剂量依赖性镇痛作用。氟西汀是一种高度特异性的5-羟色胺摄取抑制剂，在该试验中增强了吗啡的镇痛作用，但对可乐定或赛拉嗪的镇痛作用无增强效果。相反，去甲肾上腺素能摄取的选择性抑制剂尼索西汀显著增强了吗啡、可乐定和赛拉嗪的镇痛活性。这些发现进一步证明了去甲肾上腺素能机制参与了α-肾上腺素能受体激动剂的镇痛作用。