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Abstract
A recently identified novel Gαolf variant, XLGαolf, is shown to functionally couple to the human adenosine A2A receptor (A2AR). In Sf9 cells expressing A2AR, β1, and γ2, co-expression of XLGαolf increased NECA-induced [35S]GTPγS binding from approximately 130% to 300% of basal levels. Pharmacological characteristics of A2AR ligands on these cells were evaluated by using [3H]ZM241385- and [35S]GTPγS- binding assays. The rank order of the equilibrium binding constants (Kd or Ki) of adenosine receptor ligands were [3H]ZM241385 ≈ CGS15943 < MRS1220 < < CV1808 ≈ NECA < CGS21680 ≈ adenosine < IBMECA < HEMADO ≈ CPA ≈ CCPA. The rank order of EC50 values for agonists were CV1808 ≈ NECA < adenosine ≈ CGS26180 < IBMECA < HEMADO ≈ CPA ≈ CCPA. This pharmacology is consistent with the literature for A2AR and suggests that Sf9 cells co-expressing A2AR, β1, γ2, and XLGαolf could serve as a heterologous expression system for A2AR drug screening.
| ABBREVIATIONS: | ||
| ADA | = | adenosine deaminase |
| CCPA | = | 2-Chloro- N6-cyclopentyladenosine |
| CGS15943 | = | 9-Chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine |
| CGS21680 | = | 2- p-(2-carboxyethyl)phenethylamino-5′N-ethylcarboxamidoadenosine |
| CPA | = | N6-cyclopentyladenosine |
| CV1808 | = | 2-phenylaminoadenosine |
| GDP | = | guanosine diphosphate |
| GTPγS | = | guanosine5′-[γ-thio]triphosphate |
| HEMADO | = | 2-(1-Hexynyl)-N-methyladenosine |
| MRS1220 | = | N-[9-Chloro-2-(2-furanyl)[1,2,4]-triazolo[1,5-c]quinazolin-5-yl]benzene |
| MRS1706 | = | N-(4-Acetylphenyl)-2 [4[(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1Hpurin-8-yl)phenoxy]acetamide |
| NECA | = | N-ethylcarboxamidoadenosine |
| IB-MECA | = | 1-deoxy-1-[6[(3-idophenyl)ethyl] amino-9H-purin-9-yl]-N-methyl-β-D-ribofuranuronamide |
| DPCPX | = | 8-cyclopentyl-1,3-dipropylxanthine |
| ZM241385 | = | 4-(2-[7-amino-2(2-furyl)[1,2,4]triazolo [2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol. |
| ABBREVIATIONS: | ||
| ADA | = | adenosine deaminase |
| CCPA | = | 2-Chloro- N6-cyclopentyladenosine |
| CGS15943 | = | 9-Chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine |
| CGS21680 | = | 2- p-(2-carboxyethyl)phenethylamino-5′N-ethylcarboxamidoadenosine |
| CPA | = | N6-cyclopentyladenosine |
| CV1808 | = | 2-phenylaminoadenosine |
| GDP | = | guanosine diphosphate |
| GTPγS | = | guanosine5′-[γ-thio]triphosphate |
| HEMADO | = | 2-(1-Hexynyl)-N-methyladenosine |
| MRS1220 | = | N-[9-Chloro-2-(2-furanyl)[1,2,4]-triazolo[1,5-c]quinazolin-5-yl]benzene |
| MRS1706 | = | N-(4-Acetylphenyl)-2 [4[(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1Hpurin-8-yl)phenoxy]acetamide |
| NECA | = | N-ethylcarboxamidoadenosine |
| IB-MECA | = | 1-deoxy-1-[6[(3-idophenyl)ethyl] amino-9H-purin-9-yl]-N-methyl-β-D-ribofuranuronamide |
| DPCPX | = | 8-cyclopentyl-1,3-dipropylxanthine |
| ZM241385 | = | 4-(2-[7-amino-2(2-furyl)[1,2,4]triazolo [2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol. |