mglu2

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

Cloransulam-methyl is an effective herbicide that is often applied to soybean fields to control broadleaf weeds.Cloransulam-methyl is rapidly metabolised in the soybean plant but is present in the soil.CBiPES hydrochloride (CBiPES HCl) is a potent orthosteric modulator of the mGlu2 receptor.

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).

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).

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.

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.

Pomaglumetad methionil is an oral methionine prodrug of the potent specific agonist of mGlu2/3 receptor LY404039.

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.

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).

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.

Positive allosteric modulator of mGlu2 receptors

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.

mGlu2 antagonist

JNJ-40068782 is a potent, selective and systemically active positive allosteric modulator of the mGlu2 receptor.

JNJ-46356479 is a Selective and Orally Bioavailable mGlu2 receptor Positive Allosteric Modulator (PAM). JNJ-46356479 showed mGlu2 PAM EC50=78 nM; mGlu2 PAM Emax (%) = 256.

LY389795 is an agonist of group II (mGlu2/3) metabotropic glutamate receptor, it is used in inflammatory pain models.

TASP0433864 is a positive allosteric modulator of metabotropic glutamate 2 receptor with EC50 values of 199 and 206 nM at human and rat mGlu2 receptors, respectively, without exerting agonist activity at rat mGlu2 receptor.

VU6001192 is a negative allosteric modulator of mGlu2.

VU6001966 is a potent and selective mGlu2 inhibitor (mGlu2 IC50 = 78 nM) and negative allosteric modulator. VU6001966 exhibits excellent central nervous system (CNS) penetration.

RO5488608 is a new type of high-efficiency mGlu2/3 NAM.

LY3027788 hydrochloride is a diester analog of LY3020371, a selective antagonist of the metabotropic glutamate 2 and 3 receptors (mGlu2/3). It serves as a highly potent and orally bioavailable prodrug of LY3020371. Notably, LY3027788 hydrochloride exhibits antidepressant efficacy.