Target intelligence / Profile preview

Metabotropic Glutamate Receptor 7 (mGluR7)

Target
mGluR7
Molecular classification
G protein-coupled receptor, GPCR, Class C GPCR, Group III metabotropic glutamate receptor
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Overview

Metabotropic glutamate receptor 7 (mGluR7) is a G protein-coupled receptor (GPCR) encoded by the GRM7 gene in humans. It belongs to the group III metabotropic glutamate receptors. mGluR7 is highly expressed throughout the central nervous system (CNS), especially at presynaptic active zones of both excitatory (glutamatergic) and inhibitory (GABAergic) neurons. It functions as both an auto-receptor on glutamatergic terminals and a hetero-receptor on GABAergic terminals, modulating neurotransmitter release. mGluR7 is activated by L-glutamate but has much lower affinity compared to other metabotropic glutamate receptors. It couples primarily to Gi/o proteins upon activation and is implicated in several CNS disorders. Selective agonists/antagonists/allosteric modulators are under investigation as potential therapies targeting these conditions.

Other names
GRM7
02

Mechanism of action

Gi/o-coupled; inhibits cAMP production, opens GIRK potassium channels, inhibits voltage-gated calcium channels

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Biological functions

Signal transductionRegulation of synaptic transmissionRegulation of synaptic plasticityModulates neurotransmitter releaseRegulation of cognitionRegulation of emotionRegulation of stress responseFear processingLearning/memory formationAnxiety regulationNeurodevelopmental processesNeuroprotection against excitotoxicity
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Disease associations

Psychiatric disordersAnxiety disordersNeurodegenerative diseasesEpilepsyNeurodevelopmental impairments
05

Safety considerations

Challenges related to selectivity of agonists/antagonists/allosteric modulatorsIncomplete understanding of precise physiological roles

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