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