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GluR Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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. This compound 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
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
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.
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.
E1400 Kainic acid Kainic acid (algakaininso) is a potent neuroexcitatory compound derived from the red alga Digenea simplex, which acts as an agonist for AMPA/kainate-type ionotropic glutamate receptors. It induces excitotoxicity by promoting excessive Ca²⁺ influx, leading to oxidative stress, mitochondrial dysfunction, and selective neuronal death.
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. 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.
S6804 CX546 CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator.
S8143 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.
E4619 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.
E5810 Ro 67-7476 Ro 67‑7476 is a potent positive allosteric modulator (PAM) of mGluR1, enhancing glutamate‑evoked responses in calcium mobilization assays with an EC50 of 60.1 nM. It also exhibits intrinsic agonist activity, inducing ERK1/2 phosphorylation in the absence of exogenous glutamate with an EC50 of 163.3 nM.
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 and exhibits potential for the treatment of 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. This compound 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.
E1773 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.
E5887New Osavampator Osavampator (TAK-653, NBI-1065845) is a positive allosteric modulator (PAM) of AMPA receptors. It enhances glutamate-induced calcium influx in CHO cells expressing human AMPA receptors with an EC50 of 3.3 µM and potentiates AMPA receptor-mediated currents in rat primary hippocampal neurons with an EC50 of 4.4 µM.
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
Verified customer review of Riluzole
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
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.