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Target intelligence / Profile preview
Metabotropic Glutamate Receptor 8 (mGluR8)
- Target
- mGluR8
- Molecular classification
- G protein-coupled receptor, GPCR, Metabotropic glutamate receptor, Receptor
01
Overview
Metabotropic glutamate receptor 8 (mGluR8) is a G protein-coupled receptor activated by L-glutamate. It belongs to Group III mGluRs and is primarily Gi/o-coupled, inhibiting cAMP production. Highly expressed in limbic brain regions and the enteric nervous system, mGluR8 acts as a presynaptic autoreceptor, inhibiting glutamate release. It plays roles in learning, memory, anxiety, pain, and gut motility. Dysregulation is implicated in neuropsychiatric disorders, making it a potential therapeutic target.
- Other names
- Glutamate receptor metabotropic 8GRM8
02
Mechanism of action
Gi/o-coupled; inhibits adenylyl cyclase activity, leading to reduced cyclic AMP (cAMP) levels
03
Biological functions
NeurotransmissionSynaptic plasticityModulation of neuronal excitabilityPresynaptic inhibitionRegulation of neurotransmitter releaseSignal transduction
04
Disease associations
Anxiety disordersEpilepsyParkinson's diseaseDrug addictionChronic pain syndromes
05
Safety considerations
Potential for off-target effects due to widespread expression in the CNS and PNSComplexity of glutamatergic signaling makes targeted drug development challengingSelectivity of ligands can be an issue
06
Interacting drugs
(*S*)-3,4-DCPG
2 more in the full profile.
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