Metabotropic glutamate receptor 4
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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]
- 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%[8]
- ML-128: EC50 = 240 nM, Emax = 182%[9][10]
- Valiglurax (AP-472) (VU0652957)[11]
- VU-0418506[12][13]
- VU-001171: EC50 = 650 nM, Emax = 141%, 36-fold shift[14]
- VU0155041: subtype-selective PAM, intrinsic allosteric agonist activity, robust in-vivo activity[15]
- VU0364770
- PHCCC: PAM of mGluR4, negative allosteric modulator of mGluR1,[16] direct agonist at mGluR6[17]
- TC-N 22A
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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