mglur2

mGluR2 modulator 2 (compound 2) can be used in antipsychotic research. mGluR2 modulator 2 is a potent, selective and orally bioavailable positive allosteric modulator of mGluR2 with an EC 50 value of 0.13 μM [1].

mGluR2 antagonist 1 is a potent and selective class of negative allosteric modulator targeting the metabotropic glutamate receptor 2 (mGluR2) with high oral bioavailability. It displays a remarkable affinity for mGluR2, with an IC50 value of 9 nM. Furthermore, it exhibits excellent permeability across the blood-brain barrier, making it a promising candidate for central nervous system-related studies or therapies.

mGluR2 modulator 4 (compound 47) is a highly potent positive allosteric modulator of mGluR2, exhibiting an EC 50 value of 0.8 μM. It holds the potential for investigating antipsychotic properties [1].

mGluR2 modulator 1 (compound 95) is a potent, blood-brain-barrier permeable modulator of mGluR2 (metabotropic glutamate receptor-2) positive transmutation (EC50: 0.03 μM). mGluR2 modulator 1 can be used in the study of psychiatric disorders.

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.

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

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].

LY3020371 is a highly potent and selective antagonist targeting the glutamate (mGlu) 2/3 receptor, showcasing excellent inhibition at Ki values of 5.26 nM and 2.50 nM for hmGluR2 and hmGluR3, respectively. With its remarkable affinity and specificity, LY3020371 serves as a valuable tool in depression research.

PHCCC ((-) PHCCC) is a Group I metabotropic glutamate receptor antagonist and a positive allosteric modulator of mGluR4. It also is a potent to antagonism for mGluR2 and mGluR8.

VU-29 is a positive allosteric mGlu5 receptor modulator with EC50=9 nM and Ki=244 nM for rmGluR5. It is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).

trans-ACPD ((±)-trans-ACPD) is an equimolecular mixture of (1S, 3R)- and (1R, 3S)-ACPD. trans-ACPD is a selective agonist of the mGluR (metabotropic glutamate receptor); active at the group I/II mGlu receptors (EC50: 2/15/23/800 μM, mGluR2/1/5/4).

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.

LY2794193 is a highly effective and selective agonist of the mGlu3 receptor (hmGlu3 Ki=0.927 nM,EC50=0.47 nM; hmGlu2 Ki=412 nM,EC50=47.5 nM).

MGS-0039 is a group II metabotropic glutamate receptor (mgluR2/3) antagonist. Antidepressant-like action of group II mGlu receptor antagonists does not depend on serotonergic system activation. However, the AMPA receptor seems to play a key role in the an

group I mGlu1a/1a receptor antagonist and mGluR2 agonist

LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). lY487379 enhances glutamate-stimulated [35 S] GTPγS binding to mGlu2 receptors (EC50: 1.7 μM) and mGlu3 receptors (EC50>10 μM). lY487379 induces cognitive flexibility and induces behavioural inhibition in a rat model. LY487379 can be used to study schizophrenia.

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).

LY404039 (pomaglumetad) is an effective agonist of recombinant human mGlu2(Ki =149 nM)/mGlu3(Ki =92 nM).

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

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.

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.

Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic activity. Oxomemazine is a selective antagonist of mycotoxins M1 receptors, showing high (Ki=84 nM, M1 receptors) and low (Ki=1.65 μM, M2 receptors) affinity sites 20 times the difference[1]. Oxomemazine is an antihistamine and anticholinergic agent used in studies related to cough studies[2].

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

(RS)-MCPG ((±)-MCPG) is a non-selective group I/II metabotropic glutamate receptor antagonist.

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.

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

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.

MK-8768 is a potent, selective, and orally bioavailable negative allosteric modulator of the mGluR2 class, exhibiting an IC50 of 9.6 nM and characterized by excellent brain permeability.

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

L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs, pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively).

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.

LY307452 is a selective antagonist of mGluR2/3.

Ro4491533 is a potent and selective negative allosteric modulator for group II of the metabotropic glutamate receptors (mGluR2/3).

Talaglumetad hydrochloride is a prodrug of Eglumegad which is the potent and selective agonist of the type II metabotropic glutamate receptor (mGluR2/3) to treat with psychiatric disorders.