芬太尼抑制培养的神经元细胞对[3H]去甲肾上腺素的摄取。

Fentanyl inhibits the uptake of [3H]noradrenaline in cultured neuronal cells.

作者信息

Atcheson R, Rowbotham D J, Lambert D G

机构信息

University Department of Anaesthesia, Leicester Royal Infirmary.

出版信息

Br J Anaesth. 1993 Oct;71(4):540-3. doi: 10.1093/bja/71.4.540.

DOI:10.1093/bja/71.4.540

PMID:8260304

Abstract

We have examined how fentanyl modulates [3H]noradrenaline uptake in two cultured neuronal cell preparations, the human neuroblastoma SH-SY5Y and the rat phaeochromocytoma PC12. Fentanyl produced a significant, dose-dependent inhibition of [3H]noradrenaline uptake at concentrations in excess of 0.1 mumol litre-1 (P < 0.05) and 0.3 mumol litre-1 (P < 0.05) for PC12 and SH-SY5Y cells, respectively. However, these values exceed the serum concentration of fentanyl required to produce analgesia. At the maximum concentration examined (100 mumol litre-1), fentanyl produced 85-95% inhibition of uptake. This effect was not antagonized by naloxone, implying a nonopioid mechanism of action. Imipramine 1 mumol litre-1 reduced [3H]noradrenaline uptake by 65-70% but morphine, in contrast to fentanyl, had no effect (P > 0.1).

摘要

我们研究了芬太尼如何调节两种培养的神经元细胞制剂（人神经母细胞瘤SH-SY5Y和大鼠嗜铬细胞瘤PC12）中[3H]去甲肾上腺素的摄取。对于PC12和SH-SY5Y细胞，芬太尼在浓度分别超过0.1μmol/L（P<0.05）和0.3μmol/L（P<0.05）时，对[3H]去甲肾上腺素的摄取产生了显著的、剂量依赖性的抑制作用。然而，这些值超过了产生镇痛所需的芬太尼血清浓度。在所检测的最大浓度（100μmol/L）下，芬太尼对摄取的抑制率为85%-95%。这种作用未被纳洛酮拮抗，这意味着其作用机制是非阿片类的。1μmol/L的丙咪嗪使[3H]去甲肾上腺素的摄取减少了65%-70%，但与芬太尼不同的是，吗啡没有作用（P>0.1）。