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GluR antagonists/agonists

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Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S6001 pomaglumetad (LY404039) Pomaglumetad (LY404039) is a potent agonist of recombinant human mGlu2/mGlu3 receptors with Ki of 149 nM/92 nM, and it shows >100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. This compound has reached Phase 3.
Synapse, December 2008, 902-908
Schizophrenia Bulletin, 2021, 1688–1697
Schizophr Bull, 2021, sbab047
Verified customer review of pomaglumetad (LY404039)
S5137 O-Phospho-L-serine O-Phospho-L-serine (Dexfosfoserine), a molecule that mimics the phosphatidylserine head group and partially blocks microglial phagocytosis of apoptotic cells, is a specific group III metabotropic glutamate receptor (mGluR) agonist.
International Journal of Molecular Sciences, 2022, 10551
Int J Mol Sci, 2022, 23(18)10551
Front Physiol, 2022, 13:1008073
S6266 (S)-Glutamic acid (S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist.
Cell Biosci, 2024, 14(1):135
Cancer Sci, 2022, 113-6:1955-1967
CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S4716 Evans Blue Evans Blue (Direct Blue 53,C.I.23860) is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist.
Cell Commun Signal, 2025, 23(1):420
Int J Nanomedicine, 2024, 19:6677-6692
J Biol Chem, 2022, 298(12):102699
S2861 CTEP (RO4956371) CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and it shows >1000-fold selectivity over other mGlu receptors.
Sci Rep, 2025, 15(1):17364
Scientific Reports, 2025, 17364
EBioMedicine, 2017, 20:120-126
S2690 ADX-47273 ADX47273 (BA 94673139) is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes.
Journal of Biological Chemistry, 2014, 28460-28477
J Biol Chem, 2014, 289(41):28460-77
S2795 VU 0357121 VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes.
Sci Rep, 2025, 15(1):17364
PLoS One, 2020, e0228189
S2809 MPEP MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, and this compound exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.
Nature, 2025, 1-10
Mol Neurobiol, 2017, 54(7):5286-5299
Verified customer review of MPEP
E0484 CNQX CNQX (6-cyano-7-nitroquinoxaline-2,3-dione) is an AMPA and kainate receptor antagonist with IC50 values are 0.3 μM and 1.5 μM for AMPA and kainate receptors, respectively. This compound is also an antagonist at the glycine modulatory site on the NMDA receptor complex (IC50 = 25 μM). It shows neuroprotective effects in models of ischemia and inhibits seizure-like activity in hippocampal neurons.
Advanced Science, November 21, 2025, e05663
Frontiers in Cellular Neuroscience, March 06, 2020, 24
S4774 Xanthurenic Acid Xanthurenic acid (xanthurenate, 8-Hydroxykynurenic acid, 4,8-Dihydroxyquinaldic acid), a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2/3 Metabotropic glutamate receptors (mGlu2 and mGlu3).
Acta Pharmacologica Sinica, 2025, Online ahead of print
Acta Pharmacol Sin, 2025, 10.1038/s41401-025-01495-w
Cell Communication and Signaling, 2023, 141

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