Girish Mahajan (Editor)

Metabotropic glutamate receptor 4

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Species
  
Human

Entrez
  
2914

Human
  
Mouse

Ensembl
  
ENSG00000124493

Metabotropic glutamate receptor 4

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.

Contents

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, Emax = 120%
  • ML-128: EC50 = 240 nM, Emax = 182%
  • VU-0418506
  • VU-001171: EC50 = 650 nM, Emax = 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