GluR

NBQX (FG9202) is a potent, selective and competitive AMPA receptor antagonist. Neuroprotective and anticonvulsant; active in vivo.

Caroverine hydrochloride (Caroverine HCL) is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. It is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action, and can be used for the research of inner ear tinnitus.

Dasolampanel (NGX-426) is an orally available ionotropic glutamate receptor AMPA and Kainate receptor antagonist for the study of chronic pain disorders, including neuropathic pain and migraine.

MMPIP hydrochloride is a selective antagonist of allosteric mGluR7. MMPIP hydrochloride can be used in research on the roles of mGluR7 on central nervous system functions.

MTEP hydrochloride (MTEP) is non-competitive mGlu5 antagonist (IC50 and Ki of 5 nM and 16 nM, respectively)

EGLU ((2S)-α-Ethylglutamic acid) is a competitive mGluR-2 receptor antagonist with antidepressant activity and anti-injury effects, which can be used in the study of arthritis.

DCB (3,3'-dichlorobenzaldazine) is an allosteric ligand for mGluR5 and shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB). DCB blocks the positive allosteric regulation of mGluRs with the help of 3,3′-difluorobenzaldazine (DFB).

Evans blue (C.I. 23860) is an azo dye, inhibits L-glutamate uptake via the membrane-bound excitatory amino acid transporter (EAAT).

TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases.

DHPG ((RS)-3,5-DHPG) is an effective antagonist of mGluR linked to phospholipase D. As an amino acid, it serves as a selective and potent agonist for Group I mGluR (mGluR 1 and mGluR 5) without affecting Group II or Group III mGluRs.

AZD6538 is an mGluR5 negative allosteric modulator used in the study of CNS-related diseases such as Alzheimer's disease.

LY382884 is a selective and potent GluR5 kainate receptor antagonist with anxiolytic activity.LY382884 blocks blockade of mossy fibre LTP induction.

CX 717 is a positive allosteric modulator of the AMPA receptor with antidepressant-like effects and potential use in adult attention deficit hyperactivity disorder (ADHD) research [1] [2].

Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3, developed as an antidepressant.

Xanthurenic Acid (8-Hydroxykynurenic acid), a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2 3 Metabotropic glutamate receptors (mGlu2 and mGlu3).

Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors. No activity at human mGlu1 receptors. Potentiates glutamate-induced calcium release with EC 50 of 60.1 nM.

YM90K (6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-) hydrochloride is an antagonist of AMPA receptor.

GET73 (Gamma hydroxybutyric acid analogue) is an negative allosteric modulator of mGluR5. GET73 is a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties.

BMS-984923 is an orally available and blood-brain barrier permeable mGluR5 silencing allosteric modulator that inhibits β-amyloid oligomer-induced aberrant synaptic signaling, and can be used to study Alzheimer's disease.

CNQX (FG9065) is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.3 and 1.5 μM for AMPA and kainate receptors, respectively)

NBQX Disodium (FG9202 disodium) is a highly selective, competitive AMPA receptor antagonist with neuroprotective and anticonvulsant activity. NBQX Disodium is a salt of NBQX. NBQX is a potent and selective AMPA rhodosinate receptor antagonist that can be used to antagonize the excitatory toxicity of glutamate. It has anticonvulsant effects in rodent models.

CHPG hydrochloride is a selective agonist of mGluR5.

JNJ-40411813 (ADX-71149) (ADX-71149) is a new positive allosteric modulator of the metabotropic glutamate 2 receptor (mGlu2R, EC50: 147 nM).

NS-102 is a glutamate receptor and NMDA receptor antagonist that inhibits erythrocyanine (GluK2), which reduces glur6 receptor-mediated currents, and inhibits specific binding to the glur6 receptor.

VU 0469650 is a potent and selective negative allosteric modulator of mGluR1 (IC50 = 99 nM).

LY341495 is a potent metabotropic glutamate receptor antagonist that exhibits high activity against a wide range of glutamate receptor subtypes and can be used for the study of neurological disorders.

AMPA receptor modulator-2 (Example 134) is an AMPA receptor modulator with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor[1]. pIC50 = -lgIC50. [1]. BERRY CYNTHIA G B (US), et al. AZABENZIMIDAZOLES AND THEIR USE AS AMPA RECEPTOR MODULATORS. Patent. WO2016176460.

S-Sulfo-L-cysteine sodium salt shows a weak affinity for mGluR1α and mGluR5a at high concentrations and has potential antioxidant activity.

Memantine hydrochloride (Memantine HCl) is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent.

VU0155094 (ML 397) is a positive allosteric modulator with differential activity at the various group III mGluRs.

VU0650786 is a selective and potent CNS-penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM) (IC50: 392 nM), exhibiting antidepressant and anxiolytic activity in rodents.

XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm[1].

1H-Pyrrolo[2,1-c][1,2,4]benzothiadiazine, 2,3,3a,4-tetrahydro-, 5,5-dioxide, (3aR)- is a low activity isomer of S 18986. S 18986 is a AMPA receptor positive modulator with EC2 (Concentration that doubles the intensity of the AMPA-induced current) of 35 μM.

JNJ16259685 (TN.T 16259685) is a selective mGluR1 antagonist, and inhibits the synaptic activation of mGluR1 in a concentration-dependent manner with IC50 of 19 nM.

AMN082 is an mGluR7 agonist with antidepressant effects. AMN082 has a neuroprotective effect on neuronal apoptosis in rats with traumatic brain injury and attenuates cocaine- and morphine-induced locomotor sensitization and cross-sensitization in mice.

ADX88178 is a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4) with EC50 of 4 nM for human mGluR4.

(R)-3,4-DCPG HCl is a potent and selective mGlu8a receptor agonist that activates metabotropic glutamate receptors on primary afferent terminals in the neonatal rat spinal cord.

3-MATIDA is an effective mGluR-1 antagonist (IC50: 6.3 μM, rat mGluR-1a). Displays ≥ 40-fold selectivity over other receptors: mGluR-5, mGluR-2, mGluR-4 (mGluR-4a) (IC50 > 300 μM), NMDA and GluR (AMPA) (IC50 = 250 μM). 3-MATIDA act as a neuroprotectant in cultured murine cortical cells and rat hippocampal slice cultures in vitro.

ML254 competitively interacts with the MPEP allosteric binding site. ML254 is highly selective for mGlu5 versus other mGlu receptors, has a clean ancillary Ricerca profile, and suitable dystrophia myotonica protein kinase (DMPK) properties for systemic dosing in rodents.

Pomaglumetad methionine hydrochloride (LY2140023 hydrochloride) is a methionine prodrug of LY404039 with oral activity. LY404039 is a selective mGlu2 3 receptor agonist. Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) has research value in schizophrenia.

FPTQ is a highly effective antagonist of mGluR 1, displaying IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively [1]. In addition to its robust inhibitory properties, FPTQ exhibits notable antioxidant and anti-inflammatory effects in both in vitro and in vivo settings [2].

Pep2-SVKI acetate(pep2-SVKI acetate (328944-75-8 free base)) is a synthetic peptide salt that prevents internalization of AMPA-type glutamate receptor.

(E Z)-SIB-1893 (SIB 1893) is the racemate of (E)-SIB-1893 and (Z)-SIB-1893. (E)-SIB-1893 is a selective, noncompetitive mGluR5 antagonist with anticonvulsant activity .

L-Cysteinesulfinic acid monohydrate is a potent agonist at rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively [1].

(S)-ATPO is Competitive antagonist at GluR1-4 (AMPA-preferring) receptors.

Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptorsthat potently inhibits AMPA receptor desensitization, positively modulating its response to glutamic acid (EC50 = 3.8 M).

Philanthotoxin 74 dihydrochloride is an antagonist of AMPAR with IC50s of 263 and 296 nM for GluR3 and GluR1.

BMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM).