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Korean J Anesthesiol > Volume 47(6); 2004 > Article
Korean Journal of Anesthesiology 2004;47(6):877-882.
DOI: https://doi.org/10.4097/kjae.2004.47.6.877   
Studies of G Protein Activation of Orphanin FQ in the Cerebrum, Thalamus and Spinal Cord of Monkeys.
Heeseung Lee, Jong In Han
Department of Anesthesiology and Pain Medicine, College of Medicine, Ewha Womans University, Seoul, Korea. leehee@ewha.ac.kr
The aim of this in vitro study was to investigate [35S]GTP gamma S binding stimulated activation by orphanin FQ in monkey cerebral, thalamic, and spinal membranes.
A rhesus monkey (Macaca mulatta, female, n = 1) was euthanized to obtain cerebral, thalamic, and spinal cord membrane preparations. In the orphanin FQ-stimulated [35S]GTP gamma S binding dose-response curve, EC50 (effective concentration 50, nanomolar) and maximum stimulation (% over basal) were determined in the absence or presence of each opioid receptor antagonist, namely, naloxone (20 nM), nor-BNI (3 nM), naltrindole (3 nM), or J-113397 (10 nM) antagonists of the micron-, kappa-, delta-, and nociceptin- opioid receptors respectively.
The values of EC50 and maximum stimulation of [35S]GTP gamma S binding were as follows: cortex (5.1 +/- 1.4 nM / 55.6 +/- 8.2%), thalamus (8.5 +/- 1.3 nM / 27.8 +/- 4.9%), and spinal cord (11.3 +/- 0.2 nM / 15.2 +/- 4.5%). Maximum stimulation for these three membranes were significantly different (P < 0.05). J-113397 produced a 11.8 fold rightward shift in the OFQ-stimulated [35S]GTP gamma S binding dos0e-response curve, but the other opioid receptor antagonists had no effect.
Maximum stimulation of [35S]GTP gamma S binding by OFQ in each membrane showed significantly different profiles, suggesting different pharmacologic efficacies by region. The OFQ-stimulated [35S]GTP gamma S bindings in this study were mediated via nociceptin-opioid peptide receptor stimulation.
Key Words: GTP gamma S; monkey; opioid receptor antagonists; orphanin FQ
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