GluR

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.

L-Glutamine (L-Glutamic acid 5-amide) , a non-essential amino acid, is synthesized from glutamic acid and ammonia.

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

L-Glutamic acid monosodium salt (MSG) (Monosodium glutamate) is an activator of mGlu1 receptor.

Kynurenic acid (Quinurenic acid) is an endogenous tryptophan active metabolite, a triple antagonist of NMDA, glutamate, α7 nicotinic acetylcholine receptor, and an agonist of GPR35/CXCR8 with neuroprotective and anticonvulsant properties. It has neuroprotective and anticonvulsant properties and can be used to study neurodegeneration and metabolism-related diseases.

PI-linked metabotropic glutamate receptors agonist

VU 0285683 is a specific negative allosteric modulator of mGluR5 with a high affinity for the MPEP binding site. VU 0285683 shows anxiolytic-like activity.

gamma-DGG acetate(6729-55-1 free base) (γ-D-Glutamylglycine) is a competitive blocker of AMPA receptor.

CHPG hydrochloride is a selective agonist of mGluR5.

Pep2-EVKI acetate is a cell-permeable peptide. Pep2-EVKI acetate interferes the interaction between protein interacting with C-kinase (PICK1) and GluR2 AMPA receptor subunits.

LY339434 HCl is a low affinity GluR5 erythrocyte receptor agonist.LY339434 HCl causes rapid neuronal death primarily by affecting N-methyl-D-aspartate (NMDA) receptors.

CBiPES hydrochloride (CBiPES HCl) is a potent orthosteric modulator of the mGlu2 receptor with an EC50 value of 92.8 nM.CBiPES hydrochloride blocks the action of WT and mGlu(3) receptors.CBiPES hydrochloride can be used to study neurological disorders like epilepsy and Parkinson's syndrome. CBiPES hydrochloride can be used to study neurological disorders like epilepsy and Parkinson's syndrome.

DMeOB (3,3'-Dimethoxybenzaldazine) is a negative regulator with mGluR5 agonist activity and can be used to study neurological diseases.

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

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

HexylHIBO is a type I mGluR antagonist that inhibits mGlu1a and mGlu5a, with Kb values of 140 and 110 μM, respectively.HexylHIBO decreases sEPSC in rats.

LY-2300559 is an agonist of metabotropic glutamate receptor 2 (mGluR2) and can be used in studies about the treatment of migraine.

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.

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.

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

KRP-199 sodium sodium is highly potent and selective for AMPA-R in vitro and exhibits good neuroprotection in vivo.

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.

TAT-GluA2 3Y acetate is an inhibitor of AMPA receptor endocytosis.Systemic administration of Tat-GluA2(3Y) during the induction phase of d-amphetamine blocked maintenance of behavioural sensitization and attenuated the maintenance of neurochemical sensitization of rat.

(S)-3-Hydroxyphenylglycine is an agonist of group I metabotropic glutamate receptors (mGluRs).

(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.

(S)-3,4-DCPG HCl ((S)-3,4-Dicarboxyphenylglycine HCl) is a selective metabotropic glutamate receptor 8a (mGluR8a) agonist that has an effect on human mGluR8-expressing AV12-664 cells with an EC50 of 31 nM.

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.

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

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

AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux.

AMPA receptor modulator-2 (Example 134) is a 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.

VU6012962 is an orally bioavailable negative allosteric modulator of CNS-penetrant metabotropic glutamate receptor 7(mGlu7; IC50: 347 nM).

Methoxy-PEPy is a potent and selective mGlu5 receptor inhibitor with an IC50 value of 1 nM.

Dipraglurant (ADX48621) is a negative alteration modulator (NAM) of mGluR5 that inhibits dyskinesia in the LID macaque model.

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

CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases.

IEM 1754 2HBr (IEM 1754 dihydrobromide) is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.

S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors, showcasing cognitive-enhancing properties in rodents. It induces the release of noradrenaline and acetylcholine in the rat hippocampus, leading to enhanced object-recognition memory.

L-APB is an effective and specific agonist for the group III mGluRs (EC50s: 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6, and mGlu7 receptors, respectively).

7-Chlorokynurenic acid (7-chloro-4-hydroxy-2-carboxyquinoline) is an effecitve and selective antagonist of NMDA receptor with IC50 of 0.56 μM for the glycine B coagonist site. 7-Chlorokynurenic acid inhibits the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM and shows antinociceptive actions after neuraxial delivery.

CHPG sodium salt is a selective agonist of mGluR5 and activates the ERK and Akt signaling pathways. CHPG sodium salt can be used in studies about traumatic brain injury.

Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.

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).

VU-1545 is mGlu5 positive allosteric modulator.

KM02894 is a glutamate release inhibitor. Cancer cells release high levels of glutamate that can disrupt normal bone turnover, which can lead to cancer-induced bone pain.KM02894 may be used in the study of tumor-related diseases.

FTIDC is a highly potent and selective allosteric antagonist of mGluR1 receptors and shows very weak potency against human and rat mGluR5 receptors. The inhibition of FTIDC for mGluR1 receptors is shown to be in noncompetitive manner and displays IC50 val

Ro0711401 is an agonist of mGlu1 receptor.

DNQX (FG 9041) is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.5 and 0.1 μM for AMPA and kainate receptors, respectively)

L-Cysteic acid monohydrate (3-Sulfo-L-alanine Monohydrate) is an oxidation product of L-cysteine that may be used as a competitive inhibitor of the bacterial aspartate: alanine antiporter (AspT) exchange of aspartate and in other aspartate biological systems. L-Cysteic acid monohydrate is used in monomeric surfactant development. L-Cysteic acid monohydrate may be used in studies of excitatory amino acids in the brain, such as those that bind to cysteine sulfinic acid receptors. It is a useful agonist at several rat metabotropic glutamate receptors (mGluRs).

Transtorine (1,4-DIHYDRO-4-OXOQUINOLINE-2-CARBOXYLIC ACID) is a GluR and NMDA inhibitor.