Investigation of Orphanin FQ-stimulated 35SGTPgammaS Binding in the Whole Brain of Mice: Does Orphanin FQ Have Anti-opioid Effect in the Level of Receptor-ligand Interaction and 35SGTPgammaS Activation? / 대한마취과학회지
Korean Journal of Anesthesiology
;
: 91-96, 2007.
Artículo
en Coreano
| WPRIM
| ID: wpr-200355
ABSTRACT
BACKGROUND:
This study was examined whether or not the orphanin FQ (OFQ)-stimulated [35S]GTPgammaS activity interact with DAMGO in the whole brain of mice.METHODS:
ICR mice (male, n = 20, 20-25 g) were euthanized for the membrane preparations. In the agonist-stimulated [35S]GTPgammaS binding dose-response curves by OFQ, Ro-64-6198 and DAMGO, the EC50 (effective concentration 50, nM) and maximum stimulation (% over basal) were determined in the presence or absence of J-113397 (10 nM), a NOP (nociceptin-opioid peptide) receptor antagonist. OFQ (1micrometer), Ro-64-6198 (10micrometer), DAMGO (10micrometer) and their combination cocktail were used to determine the interaction between the NOP and MOP (micron-opioid peptide) receptor.RESULTS:
The values of EC50 and maximum stimulation of [35S]GTPgammaS binding were as follows OFQ (9.2 +/- 0.2 nM/17.9 +/- 0.1%), Ro-64-6198 (143.5 +/- 0.5 nM/18.1 +/- 0.4%), and DAMGO (680.6 +/- 0.7 nM/18.1 +/- 0.5%). J-113397 produced a 8.7 and 7.1 fold rightward shifting in the OFQ and Ro-64-6198-stimulated [35S]GTPgammaS binding dose-response curve respectively, but not in the DAMGO. OFQ combined with DAMGO-stimulated [35S]GTPgammaS binding had an additive effect, but not in the OFQ combined with Ro-64-6198.CONCLUSIONS:
OFQ, Ro-64-6198 and DAMGO-stimulated [35S]GTPgammaS binding in the brain of mice has receptor selectivity. The [35S]GTPgammaS stimulation of OFQ and DAMGO had an additive effect rather than an anti-opioid effect on the level of intracellular signal transduction through agonist-stimulated [35S]GTPgammaS bindings.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Encéfalo
/
Transducción de Señal
/
Guanosina 5'-O-(3-Tiotrifosfato)
/
Encefalina Ala(2)-MeFe(4)-Gli(5)
/
Membranas
/
Ratones Endogámicos ICR
Límite:
Animales
Idioma:
Coreano
Revista:
Korean Journal of Anesthesiology
Año:
2007
Tipo del documento:
Artículo
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