Metabotropic glutamate receptor 4
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]
Contents
Ligands
Orthosteric
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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