Metabotropic glutamate receptor 7

Metabotropic glutamate receptor 7
	according to PDB 2E4Z
Properties of human protein
Mass / length primary structure	915 amino acids , 102,251 Da
Identifier
External IDs	GeneCards : GRM7 ; OMIM : 604101 ; UniProt : Q14831 ;
	Orthologue (human)
Entrez	2917
Ensemble	ENSG00000196277
UniProt	Q14831
Refseq (mRNA)	NM_000844.3
Refseq (protein)	NP_000835.1
PubMed search	2917

Metabotropic glutamate receptor 7 (GRM 7, mGluR7) is a protein from the group of metabotropic glutamate receptors .

properties

The metabotropic glutamate receptor 7 is a G protein-coupled receptor . It is produced in large quantities in the cerebral cortex , hippocampus and cerebellum . Outside the brain, only isoforms 3 and 4 are formed. Together with mGluR4 , mGluR6 and mGluR8 it forms group III of the metabotropic glutamate receptors. After binding of glutamate , a change in conformation takes place , which causes signal transduction via G proteins (from the G _i family ). As a result, adenylyl cyclase is inhibited. The metabotropic glutamate receptor 7 has disulfide bridges and is glycosylated and phosphorylated .

Ligands

Agonist

AMN082 : allosteric agonist, causes endocytosis , non-glutamatergic

antagonist

MMPIP : allosteric antagonist / inverse agonist

Negative allosteric modulator

ADX-71743

Individual evidence

↑ ^a ^b ^c ^d GRM7 - Metabotropic glutamate receptor 7 precursor - Homo sapiens (Human) - GRM7 gene & protein. In: uniprot.org. September 12, 2018, accessed November 6, 2018 .
↑ Li X, Gardner EL, Xi ZX: The Metabotropic Glutamate Receptor 7 (mGluR7) Allosteric Agonist AMN082 Modulates Nucleus Accumbens GABA and Glutamate, but not Dopamine, in Rats . In: Neuropharmacology . 54, No. 3, 2008, pp. 542-51. doi : 10.1016 / j.neuropharm.2007.11.005 . PMID 18155073 . PMC 2410088 (free full text).
↑ ^a ^b Palucha A, Klak K, Branski P, van der Putten H, Flor PJ, Pilc A: Activation of the mGlu7 receptor elicits antidepressant-like effects in mice . In: Psychopharmacology . 194, No. 4, 2007, pp. 555-62. doi : 10.1007 / s00213-007-0856-2 . PMID 17622518 .
↑ Pelkey KA, Yuan X, Lavezzari G, Roche KW, McBain CJ: mGluR7 undergoes rapid internalization in response to activation by the allosteric agonist AMN082 . In: Neuropharmacology . 52, No. 1, 2007, pp. 108-17. doi : 10.1016 / j.neuropharm.2006.07.020 . PMID 16914173 .
↑ Suzuki G, Tsukamoto N, Fushiki H, Kawagishi A, Nakamura M, Kurihara H, Mitsuya M, Ohkubo M, Ohta H: In vitro pharmacological characterization of novel isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists . In: J. Pharmacol. Exp. Ther. . 323, No. 1, 2007, pp. 147-56. doi : 10.1124 / jpet.107.124701 . PMID 17609420 .
↑ Kalinichev M, Rouillier M, Girard F, etal: ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7: in vitro and in vivo characterization . In: J. Pharmacol. Exp. Ther. . 344, No. 3, 2013, pp. 624-36. doi : 10.1124 / jpet.112.200915 . PMID 23257312 .

[uniprot-14831-1] GRM7 - Metabotropic glutamate receptor 7 precursor - Homo sapiens (Human) - GRM7 gene & protein. In: uniprot.org. September 12, 2018, accessed November 6, 2018 .

[2] Li X, Gardner EL, Xi ZX: The Metabotropic Glutamate Receptor 7 (mGluR7) Allosteric Agonist AMN082 Modulates Nucleus Accumbens GABA and Glutamate, but not Dopamine, in Rats . In: Neuropharmacology . 54, No. 3, 2008, pp. 542-51. doi : 10.1016 / j.neuropharm.2007.11.005 . PMID 18155073 . PMC 2410088 (free full text).

[pmid17622518-3] Palucha A, Klak K, Branski P, van der Putten H, Flor PJ, Pilc A: Activation of the mGlu7 receptor elicits antidepressant-like effects in mice . In: Psychopharmacology . 194, No. 4, 2007, pp. 555-62. doi : 10.1007 / s00213-007-0856-2 . PMID 17622518 .

[4] Pelkey KA, Yuan X, Lavezzari G, Roche KW, McBain CJ: mGluR7 undergoes rapid internalization in response to activation by the allosteric agonist AMN082 . In: Neuropharmacology . 52, No. 1, 2007, pp. 108-17. doi : 10.1016 / j.neuropharm.2006.07.020 . PMID 16914173 .

[5] Suzuki G, Tsukamoto N, Fushiki H, Kawagishi A, Nakamura M, Kurihara H, Mitsuya M, Ohkubo M, Ohta H: In vitro pharmacological characterization of novel isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists . In: J. Pharmacol. Exp. Ther. . 323, No. 1, 2007, pp. 147-56. doi : 10.1124 / jpet.107.124701 . PMID 17609420 .

[pmid23257312-6] Kalinichev M, Rouillier M, Girard F, etal: ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7: in vitro and in vivo characterization . In: J. Pharmacol. Exp. Ther. . 344, No. 3, 2013, pp. 624-36. doi : 10.1124 / jpet.112.200915 . PMID 23257312 .