Metabotropic glutamate receptor 2

Metabotropic glutamate receptor 2

Glutamate receptor, metabotropic 2, GluR2, also known as GRM2, is a human gene.


Subtype-selective potentiators

Although a number of group-II-selective (GluR2/3) ligands are known, ligands displaying high selectivity, including subtype-selectivity over GluR3, are currently rare (2008). Examples of subtype-selective ligands are the following allosteric potentiators. GluR2 potentiation is a new approach for the treatment of schizophrenia.

  • BINA: potent potentiator; modest direct agonist; robust in-vivo activity.
  • LY-487,379: devoid of orthosteric activity; along with related 3-pyridylmethylsulfonamides the first subtype-2-selective potentiator published (2003).

See also


Further reading

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  • Flor PJ, Lindauer K, Püttner I, et al. (1995). "Molecular cloning, functional expression and pharmacological characterization of the human metabotropic glutamate receptor type 2.". Eur. J. Neurosci. 7 (4): 622–9.
  • Scherer SW, Duvoisin RM, Kuhn R, et al. (1997). "Localization of two metabotropic glutamate receptor genes, GRM3 and GRM8, to human chromosome 7q.". Genomics 31 (2): 230–3.
  • Gomeza J, Mary S, Brabet I, et al. (1996). "Coupling of metabotropic glutamate receptors 2 and 4 to G alpha 15, G alpha 16, and chimeric G alpha q/i proteins: characterization of new antagonists.". Mol. Pharmacol. 50 (4): 923–30.
  • Snow BE, Hall RA, Krumins AM, et al. (1998). "GTPase activating specificity of RGS12 and binding specificity of an alternatively spliced PDZ (PSD-95/Dlg/ZO-1) domain.". J. Biol. Chem. 273 (28): 17749–55.
  • Malherbe P, Knoflach F, Broger C, et al. (2001). "Identification of essential residues involved in the glutamate binding pocket of the group II metabotropic glutamate receptor.". Mol. Pharmacol. 60 (5): 944–54.
  • Martí SB, Cichon S, Propping P, Nöthen M (2002). "Human metabotropic glutamate receptor 2 gene (GRM2): chromosomal sublocalization (3p21.1-p21.2) and genomic organization.". Am. J. Med. Genet. 114 (1): 12–4.
  • Krampfl K, Schlesinger F, Zörner A, et al. (2002). "Control of kinetic properties of GluR2 flop AMPA-type channels: impact of R/G nuclear editing.". Eur. J. Neurosci. 15 (1): 51–62.
  • Dietrich D, Kral T, Clusmann H, et al. (2002). "Presynaptic group II metabotropic glutamate receptors reduce stimulated and spontaneous transmitter release in human dentate gyrus.". Neuropharmacology 42 (3): 297–305.
  • Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903.
  • Kuwabara T, Hsieh J, Nakashima K, et al. (2004). "A small modulatory dsRNA specifies the fate of adult neural stem cells.". Cell 116 (6): 779–93.
  • Tang FR, Chia SC, Chen PM, et al. (2004). "Metabotropic glutamate receptor 2/3 in the hippocampus of patients with mesial temporal lobe epilepsy, and of rats and mice after pilocarpine-induced status epilepticus.". Epilepsy Res. 59 (2-3): 167–80.
  • Anneser JM, Chahli C, Ince PG, et al. (2004). "Glial proliferation and metabotropic glutamate receptor expression in amyotrophic lateral sclerosis.". J. Neuropathol. Exp. Neurol. 63 (8): 831–40.
  • Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).". Genome Res. 14 (10B): 2121–7.
  • {{cite journal | author=Cube RV, Vernier JM, Hutchinson JH, et al. |title=3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2). |journal=Bioorg. Med. Chem. Lett. |volume=15 |issue= 9 |pages= 2389-93 |year= 2005 |pmid= 15837331 |doi= 10.1016/j.bmcl.2005.02.078 }}
  • Rodd ZA, McKinzie DL, Bell RL, et al. (2006). "The metabotropic glutamate 2/3 receptor agonist LY404039 reduces alcohol-seeking but not alcohol self-administration in alcohol-preferring (P) rats.". Behav. Brain Res. 171 (2): 207–15.


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