Metabotropic glutamate receptor 4

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

Together with GRM6, GRM7 and GRM8 it belongs to group III of the is_associated_with::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 is_associated_with::parkinson's disease. is_associated_with::Splice variant "taste-GRM4" is involved in the perception of is_associated_with::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%
 * is_associated_with::ML-128: EC50 = 240 nM, Emax = 182%
 * VU-001171: EC50 = 650 nM, Emax = 141%, 36-fold shift
 * VU-0155041: subtype-selective PAM, intrinsic allosteric agonist activity, robust in-vivo activity
 * is_associated_with::PHCCC: PAM of mGluR4, negative allosteric modulator of is_associated_with::mGluR1, direct agonist at is_associated_with::mGluR6