| S6001 |
pomaglumetad (LY404039)
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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.
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Schizophr Bull, 2021, sbab047
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Neuropsychopharmacology, 2020, 10.1038/s41386-020-0764-2
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Sci Rep, 2019, 9(1):14247
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| S6266 |
(S)-Glutamic acid
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(S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist.
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Cell Biosci, 2024, 14(1):135
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Cancer Sci, 2022, 113-6:1955-1967
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CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
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| S4716 |
Evans Blue
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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.
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Cell Commun Signal, 2025, 23(1):420
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Int J Nanomedicine, 2024, 19:6677-6692
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J Biol Chem, 2022, 298(12):102699
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| S2861 |
CTEP (RO4956371)
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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.
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Sci Rep, 2025, 15(1):17364
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EBioMedicine, 2017, 20:120-126
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| S5137 |
O-Phospho-L-serine
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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.
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Int J Mol Sci, 2022, 23(18)10551
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Front Physiol, 2022, 13:1008073
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| S4774 |
Xanthurenic Acid
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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).
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Acta Pharmacol Sin, 2025, 10.1038/s41401-025-01495-w
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Cell Commun Signal, 2023, 21(1):141
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| S4721 |
L-Glutamic acid monosodium salt
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L-Glutamic acid monosodium salt is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods. This compound acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). It shows a direct activating effect on the release of DA from dopaminergic terminals.
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Heliyon, 2024, 10(1):e23945
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Acta Biomater, 2022, 152:255-272
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| S2690 |
ADX-47273
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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.
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J Biol Chem, 2014, 289(41):28460-77
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| S2795 |
VU 0357121
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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.
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Sci Rep, 2025, 15(1):17364
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| S2809 |
MPEP
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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.
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Mol Neurobiol, 2017, 54(7):5286-5299
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