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Isoform-selective Products

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GluR Signaling Pathway

GluR Products

  • All (36)
  • GluR Inhibitors (4)
  • GluR Activators (2)
  • GluR Antagonists (10)
  • GluR Agonists (14)
  • GluR Modulators (4)
  • New GluR Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1614 Riluzole Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Neurotherapeutics, 2023, none
J Endocr Soc, 2023, 7(10):bvad117
Front Bioeng Biotechnol, 2022, 10:855755
S6001 pomaglumetad (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.
Schizophr Bull, 2021, sbab047
Neuropsychopharmacology, 2020, 10.1038/s41386-020-0764-2
Sci Rep, 2019, 9(1):14247
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.
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.
Cancer Sci, 2022, 113-6:1955-1967
CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
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.
Acta Pharmacol Sin, 2019, 10.1038/s41401-018-0206-4
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.
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.
J Biol Chem, 2014, 289(41):28460-77
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.
Mol Neurobiol, 2017, 54(7):5286-5299
S8035 VU 0364439 VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
Antioxidants (Basel), 2018, 10.3390/antiox7110150
S6906 Capric acid Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.
Pharmaceuticals (Basel), 2023, 16(5)692
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).
Cell Commun Signal, 2023, 21(1):141
S2645 SIB 1757 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.
MedComm (2020), 2023, 4(2):e242
MedComm (2020), 2023, 4(2):e242
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.
Int J Nanomedicine, 2024, 19:6677-6692
J Biol Chem, 2022, 298(12):102699
S4721 L-Glutamic acid monosodium salt L-Glutamic acid monosodium salt is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods. L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
Heliyon, 2024, 10(1):e23945
Acta Biomater, 2022, 152:255-272
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.
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.
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.
S2860 IEM 1754 2HBr IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
E1259 DNQX DNQX is an AMPA receptor antagonist that prevents excess calcium influx via voltage-gated calcium channels.
E1257 (R,S)-3,5-DHPG Hydrochloride (R,S)-3,5-DHPG hydrochloride (DHPG, Dihydroxy phenylglycine) is a salt of free amino acid dihydroxy phenylglycine (DHPG) which acts as a selective and potent agonist of group I metabotropic glutamate receptors (mGluR) (mGluR 1 and mGluR 5).
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. CNQX is also an antagonist at the glycine modulatory site on the NMDA receptor complex (IC50 = 25 μM). CNQX shows neuroprotective effects in models of ischemia and inhibits seizure-like activity in hippocampal neurons.
S3070 Piracetam Piracetam (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
S6804 CX546 CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator.
S8143New Mavoglurant 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.
E4619New Basimglurant Basimglurant(RG7090, CTEP Derivative) is a potent and selective negative allosteric modulator of mGlu5, with a Kd of 1.1 nM, It inhibits the function of mGluR5, thereby regulating glutamatergic neurotransmission.
S1970 VU-29 VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor, with EC50 of 9 nM and Ki=244 nM for rat mGluR5, which is selective for mGluR5 relative to other mGluR subtypes.
E0535 WAY-303290 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.
S6618 JNJ-42153605 JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.
S0165 Ampalex (CX-516) Ampalex (CX-516, Ampakine CX 516, BDP-12, SPD 420) is a positive allosteric modulator of AMPA receptor. Ampalex exhibits potential treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
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.
S2434 IDRA-21 IDRA-21 is a partial allosteric modulator of AMPA receptor desensitization. IDRA-21 is a potent cognition-enhancing drug virtually devoid of neurotoxic liability.
S9686 NBQX (FG9202) NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
S6803 1-BCP 1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents.
E1773New Fasoracetam (NS 105) Fasoracetam (NS 105) is a metabotropic glutamate receptor activator with a potential to treat vascular dementia.
S5222 Coluracetam Coluracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects.
S6906 Capric acid Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.
Pharmaceuticals (Basel), 2023, 16(5)692
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.
Int J Nanomedicine, 2024, 19:6677-6692
J Biol Chem, 2022, 298(12):102699
S2860 IEM 1754 2HBr IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
E4619New Basimglurant Basimglurant(RG7090, CTEP Derivative) is a potent and selective negative allosteric modulator of mGlu5, with a Kd of 1.1 nM, It inhibits the function of mGluR5, thereby regulating glutamatergic neurotransmission.
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).
Cell Commun Signal, 2023, 21(1):141
E1773New Fasoracetam (NS 105) Fasoracetam (NS 105) is a metabotropic glutamate receptor activator with a potential to treat vascular dementia.
S1614 Riluzole Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Neurotherapeutics, 2023, none
J Endocr Soc, 2023, 7(10):bvad117
Front Bioeng Biotechnol, 2022, 10:855755
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.
EBioMedicine, 2017, 20:120-126
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.
Mol Neurobiol, 2017, 54(7):5286-5299
S2645 SIB 1757 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.
MedComm (2020), 2023, 4(2):e242
MedComm (2020), 2023, 4(2):e242
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.
E1259 DNQX DNQX is an AMPA receptor antagonist that prevents excess calcium influx via voltage-gated calcium channels.
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. CNQX is also an antagonist at the glycine modulatory site on the NMDA receptor complex (IC50 = 25 μM). CNQX shows neuroprotective effects in models of ischemia and inhibits seizure-like activity in hippocampal neurons.
S8143New Mavoglurant 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.
E0535 WAY-303290 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.
S9686 NBQX (FG9202) NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
S6001 pomaglumetad (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.
Schizophr Bull, 2021, sbab047
Neuropsychopharmacology, 2020, 10.1038/s41386-020-0764-2
Sci Rep, 2019, 9(1):14247
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.
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.
Cancer Sci, 2022, 113-6:1955-1967
CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
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.
J Biol Chem, 2014, 289(41):28460-77
S8035 VU 0364439 VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
Antioxidants (Basel), 2018, 10.3390/antiox7110150
S4721 L-Glutamic acid monosodium salt L-Glutamic acid monosodium salt is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods. L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
Heliyon, 2024, 10(1):e23945
Acta Biomater, 2022, 152:255-272
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.
E1257 (R,S)-3,5-DHPG Hydrochloride (R,S)-3,5-DHPG hydrochloride (DHPG, Dihydroxy phenylglycine) is a salt of free amino acid dihydroxy phenylglycine (DHPG) which acts as a selective and potent agonist of group I metabotropic glutamate receptors (mGluR) (mGluR 1 and mGluR 5).
S3070 Piracetam Piracetam (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
S0165 Ampalex (CX-516) Ampalex (CX-516, Ampakine CX 516, BDP-12, SPD 420) is a positive allosteric modulator of AMPA receptor. Ampalex exhibits potential treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
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.
S6803 1-BCP 1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents.
S5222 Coluracetam Coluracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects.
S6804 CX546 CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator.
S1970 VU-29 VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor, with EC50 of 9 nM and Ki=244 nM for rat mGluR5, which is selective for mGluR5 relative to other mGluR subtypes.
S6618 JNJ-42153605 JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.
S2434 IDRA-21 IDRA-21 is a partial allosteric modulator of AMPA receptor desensitization. IDRA-21 is a potent cognition-enhancing drug virtually devoid of neurotoxic liability.
S8143New Mavoglurant 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.
E4619New Basimglurant Basimglurant(RG7090, CTEP Derivative) is a potent and selective negative allosteric modulator of mGlu5, with a Kd of 1.1 nM, It inhibits the function of mGluR5, thereby regulating glutamatergic neurotransmission.
E1773New Fasoracetam (NS 105) Fasoracetam (NS 105) is a metabotropic glutamate receptor activator with a potential to treat vascular dementia.

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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