mglu3

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

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).

VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of the mGlu4 receptor with an EC50 of 240 nM for human receptors and 110 nM for rat receptors. It exhibits weak activity at mGlu5 and mGlu8 receptors and is inactive at mGlu1, mGlu2, mGlu3, mGlu6, and mGlu7 receptors. The compound can penetrate the CNS.

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.

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.

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).

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).

LY2389575 hydrochloride is an mGlu3 negative allosteric modulator (NAM) that is selective and non-competitive, with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in the level of Mrc1, which amplifies the toxicity of β-amyloid (Aβ), and can be used to study Alzheimer's disease. It can be used to study Alzheimer's disease.

ML289 (VU0463597) is a potent, selective, and CNS-penetrant negative allosteric modulator of mGlu3 (IC50=0.66 μM), with over 15-fold selectivity compared to mGlu2 and no activity against mGlu5.

ML337 is a negative allosteric modulator of mGlu3 with an IC50 of 593 nM.

MGS0274, an ester-based lipophilic prodrug of the metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, demonstrates enhanced oral bioavailability and holds promise for schizophrenia research applications.

VU6010572 is a highly potent and selective negative allosteric modulator of mGlu3, exhibiting an IC50 of 245 nM. Additionally, VU6010572 displays high central nervous system penetrance [1] [2].

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.

Eglumegad (LY354740) hydrochloride is a potent, selective agonist for group II (mGlu2/3) receptors, showing IC50 values of 5 nM for mGlu2 and 24 nM for mGlu3 receptors in transfected human cells. This compound provides neuroprotection against NMDA-induced toxicity and exhibits anxiolytic- and antipsychotic-like properties [1].