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Isoform-selective Inhibitors

GluR Products

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  • GluR Inhibitors (3)
  • GluR Activator (1)
  • GluR Antagonists (6)
  • GluR Agonists (13)
  • GluR Modulators (3)
  • New GluR Products
Catalog No. Product Name Information Product Use Citations Product Validations
S2860 IEM 1754 2HBr IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
S4716 Evans Blue Evans Blue (Direct Blue 53) is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist.
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.
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).
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.
S1614 Riluzole (PK 26124) Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Front Bioeng Biotechnol, 2022, 10:855755
Adv Biol (Weinh), 2022, e2101184
Mol Genet Metab, 2021, S1096-7192(21)00826-X
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.
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
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
S9686 NBQX (FG9202) NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
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).
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
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.
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 (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
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.
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.
S5222 Coluracetam Coluracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects.
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
S6266 (S)-Glutamic acid (S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist.
CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S6803 1-BCP 1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents.
S8035 VU 0364439 VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
Antioxidants (Basel), 2018, 10.3390/antiox7110150
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.
S6618 JNJ-42153605 JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.
S6804 CX546 CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator.
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.
S4716 Evans Blue Evans Blue (Direct Blue 53) is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist.
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.
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).
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.
S1614 Riluzole (PK 26124) Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Front Bioeng Biotechnol, 2022, 10:855755
Adv Biol (Weinh), 2022, e2101184
Mol Genet Metab, 2021, S1096-7192(21)00826-X
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.
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
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
S9686 NBQX (FG9202) NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
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).
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
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.
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 (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
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.
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.
S5222 Coluracetam Coluracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects.
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
S6266 (S)-Glutamic acid (S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist.
CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S6803 1-BCP 1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents.
S8035 VU 0364439 VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
Antioxidants (Basel), 2018, 10.3390/antiox7110150
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.
S6618 JNJ-42153605 JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.
S6804 CX546 CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator.
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