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纳洛酮的血管效应是否归因于防腐剂甲基对羟基苯甲酸酯和丙基对羟基苯甲酸酯?

Are the vascular effects of naloxone attributable to the preservatives methyl- and propylparaben?

作者信息

Brandt L, Andersson K E, Hindfelt B, Ljunggren B, Pickard J D

出版信息

J Cereb Blood Flow Metab. 1983 Sep;3(3):395-8. doi: 10.1038/jcbfm.1983.58.

Abstract

In vitro, the Nalonee preparation of naloxone caused a concentration-dependent relaxation of human pial cortical arteries contracted by potassium, noradrenaline, serotonin, prostaglandin F2 alpha (PGF2 alpha), and haemorrhagic cerebrospinal fluid, or inhibited contractions elicited by these agents. However, the preservatives in the Nalonee preparation, methyl- and propylparaben, had similar effects. Pure naloxone alone had no effect on potassium or PGF2 alpha-induced contractions. It is suggested that the relaxant effects on vascular smooth muscle of Nalonee can be attributed to the alkylparabens rather than to naloxone. The pronounced relaxations induced by the alkylparabens had a rapid onset, and they were stable and could easily be cleared after rinsing.

摘要

在体外,纳洛酮的Nalonee制剂可使由钾、去甲肾上腺素、血清素、前列腺素F2α(PGF2α)和出血性脑脊液引起收缩的人软脑膜皮质动脉产生浓度依赖性舒张,或抑制这些药物引起的收缩。然而,Nalonee制剂中的防腐剂对羟基苯甲酸甲酯和对羟基苯甲酸丙酯也有类似作用。单独使用纯纳洛酮对钾或PGF2α诱导的收缩无影响。提示Nalonee对血管平滑肌的舒张作用可归因于对羟基苯甲酸烷基酯而非纳洛酮。对羟基苯甲酸烷基酯引起的明显舒张起效迅速,且效果稳定,冲洗后易于清除。

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