摘要 |
The present invention provides an isolated GABA<SUB>B </SUB>receptor protein comprising at least one GABA<SUB>B</SUB>R1a subunit and at least one GABA<SUB>B</SUB>R2a subunit, characterized in that said GABA<SUB>B </SUB>receptor has one high affinity agonist binding site and one low affinity agonist binding site. In particular the isolated recombinant GABA<SUB>B </SUB>receptor protein expressed by the hGABA<SUB>B</SUB>R1a/GABA<SUB>B</SUB>R2 CHO cell line deposited at the Belgian Coordinated Collections of Microorganisms (BCCM) as CHO-K1 h-GABA-b R1a/R2 clone on Aug. 22, 2003 with the accession number LMBP 6046CB. It is thus an object of the present invention to provide the hGABA<SUB>B</SUB>R1a/GABA<SUB>B</SUB>R2 CHO cell line deposited at the Belgian Coordinated Collections of Microorganisms (BCCM) as CHO-K1 h-GABA-b R1a/R2 clone on Aug. 22, 2003 with the accession number LMBP 6046CB. The invention also provides the use of the aforementioned cell line in a method to identify GABA<SUB>B </SUB>receptor agonists using a functional or a binding assay. In particular in a radioligand-binding assay comprising the use of radiolabeled agonists such as for example <SUP>3</SUP>H-GABA or <SUP>3</SUP>H-baclofen. In a particular embodiment the present invention provides the use of the aforementioned GABA<SUB>B </SUB>receptor in a method to identify a high affinity GABA<SUB>B </SUB>receptor agonist using a functional or a binding assay. In particular in a radioligand-binding assay comprising the use of radiolabeled agonists such as for example <SUP>3</SUP>H-GABA or <SUP>3</SUP>H-baclofen. Alternatively, the aforementioned binding assays are performed on cellular extracts, in particular cellular membrane preparations of the aforementioned cells.
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