mGluR5 modulator 1 is a compound that acts as a positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5). Its primary application lies in the field of schizophrenia and cognitive impairment research.

mGluR5 antagonist-1 (compound 10) is a potent mGluR5 inhibitor exhibiting an IC50 of 11.5 nM and demonstrates antidepressant effects [1].

mGluR3 modulator-1 (1-ethyl-3-(morpholin-4-yl)-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile) is a positive allosteric modulator of mGluR3 and can be used in studies about the treatment of Parkinson's disease.

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.

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].

L-Glutamine (L-Glutamic acid 5-amide) , a non-essential amino acid, is synthesized from glutamic acid and ammonia.

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.

HexylHIBO is a type I mGluR antagonist that inhibits mGlu1a and mGlu5a, with Kb values of 140 and 110 μM, respectively.HexylHIBO decreases sEPSC in rats.

VU6012962 is an orally bioavailable negative allosteric modulator of CNS-penetrant metabotropic glutamate receptor 7(mGlu7; IC50: 347 nM).

BMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM).

Basimglurant (CTEP Derivative) is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 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).

FTIDC is a highly potent and selective allosteric antagonist of mGluR1 receptors and shows very weak potency against human and rat mGluR5 receptors. The inhibition of FTIDC for mGluR1 receptors is shown to be in noncompetitive manner and displays IC50 val

VU-1545 is mGlu5 positive allosteric modulator.

Ro0711401 is an agonist of mGlu1 receptor.

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].

AMN082 free base is a metabotropic glutamate receptor 7 allosteric agonist.

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.

(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator(EC50 of 168 nM for potentiation ).

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).

E4CPG is a novel group I/II metabotropic glutamate receptor antagonist, more potent than (RS)-MCPG.

DCB (3,3'-dichlorobenzaldazine) is an allosteric ligand for mGluR5 and shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB). DCB blocks the positive allosteric regulation of mGluRs with the help of 3,3′-difluorobenzaldazine (DFB).

VU0357121, a positive allosteric modulator of mGlu5 (EC50: 33 nM), is inactive or very weakly antagonizing at other mGlu receptor subtypes.

Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).

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).

VU0155041 is an effective and positive allosteric modulator/allosteric agonist at mGlu4 receptors (EC50: 798/693 nM, at human/rat).

XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm[1].

CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist (IC50: 2.6 nM). The selectivity of CFMTI to mGluR1 is higher 2000-fold than mGluR5.

VU 0364439 is a mGlu4 positive allosteric modulator (C50: 19.8 nM).

MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.

(-)-Camphoric acid (L-Camphoric acid) is a less active enantiomer of Camphoric acid which induces GluR expression.

JNJ-40411813 (ADX-71149) (ADX-71149) is a new positive allosteric modulator of the metabotropic glutamate 2 receptor (mGlu2R, EC50: 147 nM).

CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5).

Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors. No activity at human mGlu1 receptors. Potentiates glutamate-induced calcium release with EC 50 of 60.1 nM.

MSOP is a selective antagonist of group III metabotropic glutamate receptor (KD of 51 μM for the L-AP4-sensitive presynaptic mGluR).

ADX88178 is a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4) with EC50 of 4 nM for human mGluR4.

CTEP (RO 4956371) (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors.

MPEP hydrochloride is an effective and highly specific non-competitive antagonist at the mGlu5 receptor subtype (IC50: 36 nM).

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].

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.

TCN238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4with an EC50 of 1 μM).

VU0650786 is a selective and potent CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM) (IC50: 392 nM), with antidepressant and anxiolytic activity in rodents.

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

ADX-47273 (BA 94673139) is a positive and selective allosteric modulator for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).

O-Phospho-L-serine (Phosphoserine) is the phosphoric acid ester of serine.

MMPIP hydrochloride is a selective antagonist of allosteric mGluR7. MMPIP hydrochloride can be used in research on the roles of mGluR7 on central nervous system functions.

ML254 competitively interacts with the MPEP allosteric binding site. ML254 is highly selective for mGlu5 versus other mGlu receptors, has a clean ancillary Ricerca profile, and suitable dystrophia myotonica protein kinase (DMPK) properties for systemic dosing in rodents.

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).