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.
Ligands
Orthosteric Cinnabarinic acid, a tryptophan metabolite LSP1-2111: agonist LSP4-2022: agonist LSP2-9166: mixed agonist at mGluR4 and mGluR7
Positive allosteric modulators (PAMs) ADX88178 Foliglurax (PXT-002331, DT-1687) Tricyclic thiazolopyrazole derivative 22a: EC50 = 9 nM, Emax = 120% ML-128: EC50 = 240 nM, Emax = 182% Valiglurax (AP-472) (VU0652957) VU-0418506 VU-001171: EC50 = 650 nM, Emax = 141%, 36-fold shift VU0155041: subtype-selective PAM, intrinsic allosteric agonist activity, robust in-vivo activity VU0364770 PHCCC: PAM of mGluR4, negative allosteric modulator of mGluR1, direct agonist at mGluR6 TC-N 22A
References
Further reading