Interaction of ketamine with mu2 opioid receptors
in SH-SY5Y human neuroblastoma cells
Hirota K, Sikand KS, Lambert DG.
University Department of Anaesthesia,
Leicester Royal Infirmary,
Leicester LE1 5WW, UK.
J Anesth. 1999;13(2):107-9.
ABSTRACTPURPOSE: Ketamine is known to interact with opioid receptors. However, because this agent does not produce opioid-like respiratory depression, it might not interact with mu(2) opioid receptors. Therefore, we have studied the interaction of ketamine with mu(2) 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 [(3)H][D-Ala(2),MePhe(4),Gly(ol)(5)] enkephalin (DAMGO) binding to mu(2) opioid receptors and of forskolin (1 microM)-stimulated cyclic AMP (cAMP) formation. RESULTS: Ketamine displaced [(3)H]DAMGO binding in SH-SY5Y cells with a K(i) of 12.1 microM. However, this concentrations did not inhibit forskolin-stimulated cAMP formation, although at supraclinical concentrations, significant inhibition was observed with an estimated IC(50) of 700 microM. CONCLUSION: The present study indicates that a clinically relevant concentration of ketamine interacts with mu(2) opioid receptors. However, no agonist activity was observed.
Ketamine and pain management
Ketamine to treat fibromyalgia?
Ketamine and opiate withdrawal
Ketamine and the nucleus accumbens
Ketamine: medical and non-medical use
Ketamine and the glutaminergic hypothesis of schizophrenia
Low-dose ketamine as a fast-onset, long-acting antidepressant
and further reading
The Abolitionist Project
The Hedonistic Imperative
The Reproductive Revolution
Critique of Huxley's Brave New World
The Good Drug Guide
The Responsible Parent's Guide
To Healthy Mood Boosters For All The Family