Pharmacological analysis of a dopamine D(2Short):G(alphao) fusion protein expressed in Sf9 cells.
FEBS Lett
; 545(2-3): 155-60, 2003 Jun 19.
Article
en En
| MEDLINE
| ID: mdl-12804767
ABSTRACT
A dopamine D(2Short) receptorG(alphao) fusion protein was expressed in Sf9 cells using the baculovirus expression system. [(3)H]Spiperone bound to D(2Short)G(alphao) with a pK(d) approximately 10. Dopamine stimulated the binding of [(35)S]guanosine-5'-O-(3-thio)triphosphate (GTPgammaS) to D(2Short)G(alphao) expressed with Gbeta(1)gamma(2) (E(max)>460%; pEC(50) 5.43+/-0.06). Most of the putative D(2) antagonists behaved as inverse agonists (suppressing basal [(35)S]GTPgammaS binding) at D(2Short)G(alphao)/Gbeta(1)gamma(2) although (-)-sulpiride and ziprasidone were neutral antagonists. Competition of [(3)H]spiperone binding by dopamine and 10,11-dihydroxy-N-n-propylnorapomorphine revealed two binding sites of different affinities, even in the presence of GTP (100 micro M). The D(2Short)G(alphao) fusion protein is therefore a good model for characterising D(2) receptors.
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Bases de datos:
MEDLINE
Asunto principal:
Proteínas Recombinantes de Fusión
/
Apomorfina
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Receptores de Dopamina D2
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Proteínas de Unión al GTP
Límite:
Animals
/
Humans
Idioma:
En
Revista:
FEBS Lett
Año:
2003
Tipo del documento:
Article
País de afiliación:
Reino Unido