Metabotropic glutamate receptor 4

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Lua error in Module:Infobox_gene at line 33: attempt to index field 'wikibase' (a nil value). Metabotropic glutamate receptor 4 is a protein that in humans is encoded by the GRM4 gene.[1][2][3]

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.[3] 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.[4]

Ligands

Orthosteric

  • Cinnabarinic acid, a tryptophan metabolite[5]
  • LSP1-2111: agonist[6]
  • LSP4-2022: agonist[7]

Positive allosteric modulators (PAMs)

  • Tricyclic thiazolopyrazole derivative 22a: EC50 = 9 nM, Emax = 120%[8]
  • ML-128: EC50 = 240 nM, Emax = 182%[9][10]
  • VU-001171: EC50 = 650 nM, Emax = 141%, 36-fold shift[11]
  • VU-0155041: subtype-selective PAM, intrinsic allosteric agonist activity, robust in-vivo activity[12]
  • PHCCC: PAM of mGluR4, negative allosteric modulator of mGluR1,[13] direct agonist at mGluR6[14]

References

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Further reading

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This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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