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GluR Inhibitors | Agonists | Antagonists | Modulators (17)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
S6001 LY404039 LY404039 is a potent agonist of recombinant human mGlu2/mGlu3 receptors with Ki of 149 nM/92 nM, shows >100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3.
  • Neuropharm, 2012, 62(7):2184-91
  • PLoS One, 2011, 6(7):e22235
  • Synapse, 2015, 70:45–48
S1245 Latrepirdine 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.
S2857 (-)-MK 801 maleate (-)-MK-801 (Dizocilpine) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.
  • Pharmacol Biochem Behav, 2016, 146-147:21-27
S2251 (-)-Huperzine A (HupA) (-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4.
S2876 (+)-MK 801 maleate (+)-MK-801 is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
S1614 Riluzole Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
S2861 CTEP (RO4956371) CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors.
S2690 ADX-47273 ADX47273 is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes.
S4091 Ifenprodil Tartrate Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM.
S8035 VU 0364439 VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S2860 IEM 1754 2HBr IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
S2809 MPEP MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.
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.
S7072 NMDA (N-Methyl-D-aspartic acid) NMDA(N-Methyl-D-aspartic acid)is a specific agonist for NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor. Phase 4.
S2862 VU 0364770 VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.
S2892 VU 0361737 VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS.
S3070 Piracetam Piracetam is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
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All GluR Products

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S6001 LY404039 <1 mg/mL 1 mg/mL <1 mg/mL
S1245 Latrepirdine <1 mg/mL 24 mg/mL 13 mg/mL
S2857 (-)-MK 801 maleate <1 mg/mL 67 mg/mL 7 mg/mL
S2251 (-)-Huperzine A (HupA) <1 mg/mL 0.66 mg/mL <1 mg/mL
S2876 (+)-MK 801 maleate <1 mg/mL 68 mg/mL <1 mg/mL
S1614 Riluzole <1 mg/mL 47 mg/mL 47 mg/mL
S2861 CTEP (RO4956371) <1 mg/mL 78 mg/mL 10 mg/mL
S2690 ADX-47273 <1 mg/mL 74 mg/mL 30 mg/mL
S4091 Ifenprodil Tartrate 9 mg/mL 95 mg/mL 62 mg/mL
S8035 VU 0364439 <1 mg/mL 85 mg/mL <1 mg/mL
S2860 IEM 1754 2HBr 82 mg/mL 82 mg/mL <1 mg/mL
S2809 MPEP <1 mg/mL 39 mg/mL 39 mg/mL
S2795 VU 0357121 <1 mg/mL 61 mg/mL 21 mg/mL
S7072 NMDA (N-Methyl-D-aspartic acid) 30 mg/mL 5 mg/mL <1 mg/mL
S2862 VU 0364770 <1 mg/mL 47 mg/mL 47 mg/mL
S2892 VU 0361737 <1 mg/mL 53 mg/mL <1 mg/mL
S3070 Piracetam 72 mg/mL 72 mg/mL <1 mg/mL
Tags: Glutamate receptor activation | Glutamate receptor signaling | mGlur signaling | mGlur pathway | Glutamate receptor cancer | mGlur5 signaling | mGlur5 pathway | mGlur signaling pathway | mGlur5 drugs | Glutamate receptor inhibitor review
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