Metabotropic glutamate receptor 4

Updated on Dec 08, 2024

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Species Human Entrez 2914		Human Mouse Ensembl ENSG00000124493

Aliases GRM4, GPRC1D, MGLUR4, mGlu4, glutamate metabotropic receptor 4 External IDs MGI: 1351341 HomoloGene: 20230 GeneCards: GRM4

Metabotropic glutamate receptor 4 is a protein that in humans is encoded by the GRM4 gene.

Together with GRM6, GRM7 and GRM8 it belongs to group III of the metabotropic glutamate receptor family. Group III receptors are linked to the inhibition of the cyclic AMP cascade. Activation of GRM4 has potential therapeutic benefits in the treatment of parkinson's disease. Splice variant "taste-GRM4" is involved in the perception of umami taste.

Orthosteric

Cinnabarinic acid, a tryptophan metabolite

LSP1-2111: agonist

LSP4-2022: agonist

Positive allosteric modulators (PAMs)

Tricyclic thiazolopyrazole derivative 22a: EC₅₀ = 9 nM, E_max = 120%

ML-128: EC₅₀ = 240 nM, E_max = 182%

VU-0418506

VU-001171: EC₅₀ = 650 nM, E_max = 141%, 36-fold shift

VU-0155041: subtype-selective PAM, intrinsic allosteric agonist activity, robust in-vivo activity

PHCCC: PAM of mGluR4, negative allosteric modulator of mGluR1, direct agonist at mGluR6

References

Metabotropic glutamate receptor 4 Wikipedia

(Text) CC BY-SA

Contents

Orthosteric

Positive allosteric modulators (PAMs)

References