Interaction of ketamine with μ2 opioid receptors in SH-SY5Y human neuroblastoma cells

被引：16

作者：

Hirota K. ^{[1
]}

Sikand K.S. ^{[1
]}

Lambert D.G. ^{[1
]}

机构：

[1] University Department of Anaesthesia, Leicester Royal Infirmary

来源：

Journal of Anesthesia | 1999年 / 13卷 / 2期

关键词：

μ2 opioid receptors; Ketamine; SH-SY5Y human neuroblastoma cells;

D O I：

10.1007/s005400050035

中图分类号：

学科分类号：

摘要：

Purpose. Ketamine is known to interact with opioid receptors. However, because this agent does not produce opioid-like respiratory depression, it might not interact with μ2 opioid receptors. Therefore, we have studied the interaction of ketamine with μ2 opioid receptors expressed in SH-SY5Y cells. Methods. SH-SY5Y cells (passage 70-80) were used to obtain ketamine dose-response curves for inhibition of 0.4 nM [3H] [D-Ala2,MePhe4,Gly(ol)5] enkephalin (DAMGO) binding to μ2 opioid receptors and of forskolin (1 μM)-stimulated cyclic AMP (cAMP) formation. Results. Ketamine displaced [3H]DAMGO binding in SH-SY5Y cells with a K(i) of 12.1 μM. However, this concentrations did not inhibit forskolin-stimulated cAMP formation, although at supraclinical concentrations, significant inhibition was observed with an estimated IC50 of 700 μM. Conclusion. The present study indicates that a clinically relevant concentration of ketamine interacts with μ2 opioid receptors. However, no agonist activity was observed.

引用

页码：107 / 109

页数：2