Journal article
Dynorphin A (1-17) was Selective toµ-Opioid Receptor in Agonist-Stimulated [35S] GTPγS Binding in Cortical and Thalamic Membranes of Monkey
Korean Journal of Anesthesiology, Vol.48(4), p.412
2005
DOI: 10.4097/kjae.2005.48.4.412
Abstract
BACKGROUND
Dynorphin A (1-17) is conceived as an endogenous opioid peptide with a high degree of selectivity forkappa- opioid receptor even though it has been reported to sometimes act like amicro- opioid agonist. The aim of this study was to investigate [35S] GTPgammaS binding stimulated activation by dynorphin A (1-17) in the cerebral and thalamic membranes of a rhesus monkey.
METHODS
The rhesus monkey (Macaca mulatta, male, n = 1) was euthanized for the preparation of the cerebral and thalamic membranes. Protein concentrations were determined by the Bradford method. In the dynorphin A (1-17)-stimulated [35S] GTPgammaS binding dose-response curve, EC50 (effective concentration 50 nM) and maximum stimulation (% over basal) were determined in the absence or presence of themicro-andkappa-opioid receptor antagonists naloxone (20 nM) and norbinaltorphimine (nor-BNI, 3 nM), respectively. E2078-stimulated [35S] GTPgammaS binding was also determined in the absence or presence ofmicro-andkappa-opioid receptor antagonists in the cortical membrane and compared with dynorphin A (1-17).
RESULTS
Values of EC50 and maximum stimulation of dynorphin A (1-17)-stimulated [35S] GTPgammaS binding were as follows: cortex (474 nM/32.0%) and thalamus (423 nM/45.3%). Nor-BNI (3 nM) did not antagonize dynorphin A (1-17)-stimulated [35S] GTPgammaS binding at all in cortical or thalamic membrane, but naloxone (20 nM) produced a 12.2 fold rightward shift of the dynorphin A (1-17)-stimulated [35S] GTPgammaS binding dose-response curve in the thalamic membrane. The EC50 and the maximum stimulation of E2078-stimulated [35S] GTPgammaS binding were 65.6 nM and 22.7%, respectively. In E2078-stimulated [35S] GTPgammaS binding, the dose-response curve was antagonized not by nor-BNI but by naloxone but in the cortical membrane (a 14.2 times rightward shift).
CONCLUSIONS
Dynorphin A (1-17) is selective formicro-opioid receptor in agonist-stimulated [35S] GTPgammaS binding in the cortical and thalamic membranes of rhesus monkey.
Key Words: dynorphin A (1-17); GTPgammaS; monkey; opioid receptor
Details
- Title: Subtitle
- Dynorphin A (1-17) was Selective toµ-Opioid Receptor in Agonist-Stimulated [35S] GTPγS Binding in Cortical and Thalamic Membranes of Monkey
- Creators
- Heeseung Lee - Department of Anesthesiology and Pain Medicine, College of Medicine, Ewha Womans University, Seoul, KoreaSung Ae Lee - Department of Anesthesiology and Pain Medicine, College of Medicine, Ewha Womans University, Seoul, KoreaSin Young Kang - Department of Anesthesiology and Pain Medicine, College of Medicine, Ewha Womans University, Seoul, KoreaDong Yeon Kim - Department of Anesthesiology and Pain Medicine, College of Medicine, Ewha Womans University, Seoul, KoreaChi Hyo Kim - Department of Anesthesiology and Pain Medicine, College of Medicine, Ewha Womans University, Seoul, Korea
- Resource Type
- Journal article
- Publication Details
- Korean Journal of Anesthesiology, Vol.48(4), p.412
- DOI
- 10.4097/kjae.2005.48.4.412
- ISSN
- 0302-5780
- Language
- English
- Date published
- 2005
- Academic Unit
- Anesthesia
- Record Identifier
- 9984006308902771
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