Characterization of metabotropic glutamate receptors coupled to a pertussis toxin sensitive G‐protein in bovine brain coated vesicles

FEBS Letters

Martín, Mairena¹  Sanz, Juana M.¹  Cubero, Ana¹ 

[1] Departamento de Inorgánica, Orgánica y Bioquímica, Facultadde Químicas, Universidad de Castilla-La Mancha, 13071 Ciudad Real, Spain

关键词: Coated vesicle;    Metabotropic glutamate receptor;    G-protein;    trans-(±)-1-Aminocyclopentane 1;    3-dicarboxilic acid;    Quisqualic acid;    Radioligand binding;   

DOI  :  10.1016/0014-5793(93)81213-J

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Glutamate metabotropic receptors (mGluRs) in bovine brain coated vesicles have been characterized by pharmacological and kinetic binding experiments. Saturation experiments revealed a single binding site with a K _d = 607.9 ± 78.5 nM and a B _max = 6.45 ± 0.88 pmol/mg protein. The specific binding of l-[³H]glutamate to mGluRs is regulated by guanine nucleotides. Guanosine-5'-triphosphate (GTP; 100 μM) shifts the agonist competition curves to the right, increasing the IC₅₀ values. Pertussis toxin treatment produces a pharmacological binding profile for quisqualate similar to that obtained in the presence of 100μM GTP. These results indicate the presence of metabotropic glutamate receptors in coated vesicles and its coupling to a pertussis toxin sensitive G-protein.

【 授权许可】

Unknown