GluR

Sigaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1614 Riluzole <1 mg/mL 46 mg/mL 46 mg/mL
S6001 LY404039 <1 mg/mL 1 mg/mL <1 mg/mL
S1245 Latrepirdine 2HCl <1 mg/mL 24 mg/mL 13 mg/mL
S2251 (-)-Huperzine A (HupA) <1 mg/mL 0.66 mg/mL <1 mg/mL
S2861 CTEP (RO4956371) <1 mg/mL 78 mg/mL 10 mg/mL
S4716 Evans Blue 100 mg/mL 100 mg/mL <1 mg/mL
S2690 ADX-47273 <1 mg/mL 74 mg/mL 30 mg/mL
S2795 VU 0357121 <1 mg/mL 61 mg/mL 21 mg/mL
S2809 MPEP <1 mg/mL 39 mg/mL 39 mg/mL
S8035 VU 0364439 <1 mg/mL 85 mg/mL <1 mg/mL
S1893 D-glutamine 9 mg/mL <1 mg/mL <1 mg/mL
S2860 IEM 1754 2HBr 82 mg/mL 82 mg/mL <1 mg/mL
S3070 Piracetam 72 mg/mL 72 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

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S4716New

Evans Blue

Evans Blue is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist.

S2860

IEM 1754 2HBr

IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.

S1893

D-glutamine

D-glutamine is a D type stereoisomer of glutamine which is one of the 20 amino acids encoded by the standard genetic code.

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.

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.

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.

S8035

VU 0364439

VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.

S3070

Piracetam

Piracetam is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.

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.

S1614

Riluzole

Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.

S1245

Latrepirdine 2HCl

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
S4716New

Evans Blue

Evans Blue is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist.

S2860

IEM 1754 2HBr

IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.

Catalog No. Information Product Use Citations Product Validations
S1614

Riluzole

Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.

2016, 17(3):357

2013, 8(5):1098-105

S1245

Latrepirdine 2HCl

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
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.

2012, 62(7):2184-91

2011, 6(7):e22235

2015, 70:45–48

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.

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.

S8035

VU 0364439

VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.

S3070

Piracetam

Piracetam is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.

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.

Catalog No. Information Product Use Citations Product Validations
S1893

D-glutamine

D-glutamine is a D type stereoisomer of glutamine which is one of the 20 amino acids encoded by the standard genetic code.

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