GluR Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
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 blocker for GluR1 and GluR3 with an 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 of 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 ischaemia 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 the 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 an EC50 of 1.1 μM, exhibiting insignificant activity at 68 other receptors, including other mGlu subtypes.
S2892	VU 0361737	VU 0361737 is a selective positive allosteric modulator (PAM) for the mGlu4 receptor with an 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, and can penetrate into the 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.
E5887^New	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 anaesthetic qualities.	Neurotherapeutics, 2023, none J Endocr Soc, 2023, 7(10):bvad117 Front Bioeng Biotechnol, 2022, 10:855755
S2251	(-)-Huperzine A (HupA)	(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with K_i 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.