mglur2

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.

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.

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.

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.

4 (compound 47) is a highly potent positive allosteric modulator of mGluR2, exhibiting an EC50 value of 0.8 μM, with 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) with an EC50 of 0.03 μM. mGluR2 modulator 1 can be used in the study of psychiatric disorders.

mGluR2 modulator 2 (compound 2) is a potent, selective, and orally bioavailable positive allosteric modulator of mGluR2 with an EC50 value of 0.13 μM [1], and can be used in antipsychotic research.

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.

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

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.

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

VU-29 is a positive allosteric mGlu5 receptor modulator with an EC50 of 9 nM and a Ki of 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].

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

MGS-0210 (also known as BCI-838) is an orally active prodrug of an mGluR2 3 receptor antagonist.

group I mGlu1a/1a receptor antagonist and mGluR2 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.

mG2N001, a negative allosteric modulator (NAM) of the metabotropic glutamate receptor mGluR2, has an IC50 of 93 nM and binds to mGluR2 as an antagonist with a Ki of 63 nM. This compound is microparticle- and plasma-stable, and its radioisotope [11C] mG2N001 can be utilized in PET imaging. [11C] mG2N001 exhibits good brain heterogeneity and penetration, selectively accumulating in mGluR2-rich regions to produce high-contrast brain images [1].

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

LY487379 is a selective human mGluR2 positive allosteric modulator (PAM) that 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 behavioral inhibition in a rat model and can be used to study schizophrenia.

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).

(S)-4CPG ((S)-4-Carboxyphenylglycine) is a competitive mGlu1 receptor antagonist that attenuates nociceptive hypersensitivity and nociceptive abnormalities associated with sciatic nerve constriction injuries in rats, and may be used in the study of neurological disorders.

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

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).