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Pharmacological analysis of a dopamine D2Short:Gαo fusion protein expressed in Sf9 cells
- Source :
- FEBS Letters; Jun2003, Vol. 545 Issue 2/3, p155, 6p
- Publication Year :
- 2003
-
Abstract
- A dopamine D<subscript>2Short</subscript> receptor:G<subscript>αo</subscript> fusion protein was expressed in Sf9 cells using the baculovirus expression system. [<superscript>3</superscript>H]Spiperone bound to D<subscript>2Short</subscript>:G<subscript>αo</subscript> with a pK<subscript>d</subscript>&ap;10. Dopamine stimulated the binding of [<superscript>35</superscript>S]guanosine-5′-O-(3-thio)triphosphate (GTPγS) to D<subscript>2Short</subscript>:G<subscript>αo</subscript> expressed with Gβ<subscript>1</subscript>γ<subscript>2</subscript> (E<subscript>max</subscript>>460%; pEC<subscript>50</subscript> 5.43±0.06). Most of the putative D<subscript>2</subscript> antagonists behaved as inverse agonists (suppressing basal [<superscript>35</superscript>S]GTPγS binding) at D<subscript>2Short</subscript>:G<subscript>αo</subscript>/Gβ<subscript>1</subscript>γ<subscript>2</subscript> although (−)-sulpiride and ziprasidone were neutral antagonists. Competition of [<superscript>3</superscript>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 μM). The D<subscript>2Short</subscript>:G<subscript>αo</subscript> fusion protein is therefore a good model for characterising D<subscript>2</subscript> receptors. [Copyright &y& Elsevier]
- Subjects :
- DOPAMINE
PHARMACOLOGY
Subjects
Details
- Language :
- English
- ISSN :
- 00145793
- Volume :
- 545
- Issue :
- 2/3
- Database :
- Complementary Index
- Journal :
- FEBS Letters
- Publication Type :
- Academic Journal
- Accession number :
- 9952277
- Full Text :
- https://doi.org/10.1016/S0014-5793(03)00520-9