Agonists of metabotropic glutamate receptors and uses thereof

Details Agonists of metabotropic glutamate receptors and uses thereof Agonists of metabotropic glutamate receptors and uses thereof

C - Chemistry, Metallurgy

12

Q

C12Q 1/02 (2006.01) A61K 31/00 (2006.01) G01N 33/53 (2006.01)

Patent

CA 2315540

Astrocytes protect neurons from excitotoxic injury by maintaining low extra- cellular glutamate concentrations ([Glu]o). Compromised astrocytic glutamate uptake has been implicated in acute and chronic neuroligical conditions, including Parkinson's disease. This invention provides evidence that [Glu]o is modulated in a feed-back manner through activation of metabotropic glutamate receptors (mGluRs), particularly group II mGluRs. Furthermore, ACPD effects were mimicked by glutamate, suggesting that astrocytic glutamate transport is dynamically regulated with mGluRs acting as sensors for changes in [Glu]. Consequently, agonists of mGluR receptors are potent drugs to modulate extracellular glutamate levels in ways that are neuroprotective.

Les astrocytes protègent les neurones des lésions excitotoxiques en maintenant de faibles concentrations extracellulaires de glutamate ([Glu]¿0?). Une captation affaiblie de glutamate par les astrocytes joue un rôle dans les affections neurologiques aiguës et chroniques, y compris la maladie de Parkinson. La présente invention apporte la preuve que le [Glu]¿0? est modulé de façon rétroactive via l'activation des récepteurs de glutamate métabotropes(mGluRs), en particulier les mGluRs du groupe II. En outre, les effets de l'ACPD ont été mimés par le glutamate, ce qui laisse à penser que le transport du glutamate par les astrocytes est régulé de façon dynamique, les mGluRs agissant comme capteurs des modifications du [Glu]. Les agonistes des récepteurs mGluR constituent par conséquent des médicaments efficaces qui permettent de moduler les niveaux de glutamate extracellulaire de manière neuroprotectrice.

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