glur-2

Primidone (NCI-C56360) is a potent anticonvulsant agent. It is a neuronal voltage-gated sodium channel blocker and has value in the study of epilepsy, essential tremor, and psychiatric disorders.

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.

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.

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.

MNI 137 is a negative allosteric modulator of mGlu2. MNI 137 inhibits glutamate-induced calcium mobilization with IC50s of 8.3 and 12.6 nM for human and rat.

JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).

AZD-8529 is a highly selective, and orally bioavailable positive allosteric modulator of mGluR2 (EC50: 285 nM). It shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

AZD-8529 mesylate is a highly selective, and orally bioavailable positive allosteric modulator of mGluR2 (EC50: 285 nM). It shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

DCG-IV is an effective agonist of class II mGluR. DCG-IV has anticonvulsant and neuroprotective effects. The EC50 of mGlu2R and mGlu3R are 0.35 and 0.09 μM, respectively. DCG-IV is also a competitive antagonist of Group I (IC50: mGlu1 / 5R = 389/630 μM) a

L-Cysteinesulfinic acid is an endogenous neurotransmitter with agonistic effects on a variety of metabotropic glutamate receptors (mGluRs), including mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, with a pEC50 = 2.7 to 4.0. L- Cysteinesulfinic acid is a pld-coupled agonist of metabotropic excitatory amino acid (EAA) receptors.

LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells.

LY2140023 has the potential for schizophrenia.LY2140023 is an orally active prodrug of LY404039. LY404039 is a selective metabotropic glutamate 2/3 receptor agonist.

LY3020371 hydrochloride exerts an antidepressant-like signature in vivo. LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM.

Biphenylindanone A is a selective potentiator of human mGluR2 (hmGluR2),and for the treatment of neurological disorders.

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

JNJ-46281222 is a metabotropic glutamate (mGlu) 2-selective, highly potent positive allosteric modulator (PAM) with nanomolar affinity (Kd = 1.7 nM) and high modulatory potency (pEC50 = 7.71).

LY2794193, a potent and selective mGlu3 (metabotropic glutamate 3) receptor agonist, Ki=0.927 nM, EC50=0.47 nM, reduces akathisia seizures and depressive-like behaviors and increases GAT1, GLAST and GLT-1 protein levels in rats.

LY2812223 is a highly effective and functionally selective mGlu2 receptor agonist. It has a mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively).

LY2979165 (mGlu2 agonist) is an orthosteric agonist of mGluR2 and can be used in studies about serving as an anti-depressant.

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.

Eglumegad is a highly effective and selective agonist of group II (mGlu2/3) receptor (IC50s: 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively).

mGluR2 modulator5 (Compound 11) is a selective negative allosteric modulator with oral activity, exhibiting an IC50 of 8.9 nM. Pharmacokinetic studies in rats have demonstrated its effective penetration through the blood-brain barrier. This compound is utilized in research related to cognitive and neurological functions in mood disorders, contributing to the field of neurological diseases.

1-Benzyl-APDC acts as an agonist for mGluR6 in CHO cells, exhibiting an EC50 of 20 μM. Additionally, it functions as a weak antagonist for mGluR2, with an IC50 of 200 μM.

LBG30300 is a subtype-selective mGlu2 receptor agonist with an EC50 of 0.6 nM. It is capable of crossing the blood-brain barrier.