| 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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| 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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| S2645 |
SIB 1757
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SIB 1757 is a highly selective, noncompetitive antagonist of metabotropic glutamate receptor type 5 (mGluR5) with IC50 of 0.4 μM at hmGluR5 compared with >30 µM at hmGluR1b, hmGluR2, hmGluR4, hmGluR6, hmGluR7 and hmGluR8.
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MedComm (2020), 2023, 4(2):e242
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| S1245 |
Latrepirdine 2HCl
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Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.
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| E1259 |
DNQX
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DNQX is an AMPA receptor antagonist that prevents excess calcium influx via voltage-gated calcium channels.
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| E0484 |
CNQX
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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.
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| S8143 |
Mavoglurant
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Mavoglurant (AFQ056) is a structurally selective, non-competitive antagonist of mGlu5 receptor with an IC50 of 30 nM. It exhibits efficacy in treatment of L-dopa induced dyskinesia in Parkinson's disease and Fragile X syndrome.
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| E0535 |
WAY-303290
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WAY-303290 (GluR6 antagonist-1) is a benzothiophene derivative acting as an ionotropic glutamate receptor 6 (GluR6) antagonist, which can be used for researching acute and chronic neurological disorders.
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| S9686 |
NBQX (FG9202)
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NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
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| S1614 |
Riluzole
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Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
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Neurotherapeutics, 2023, none
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J Endocr Soc, 2023, 7(10):bvad117
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Front Bioeng Biotechnol, 2022, 10:855755
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