mglur

(R)-3,4-DCPG HCl is a potent and selective mGlu8a receptor agonist that activates metabotropic glutamate receptors on primary afferent terminals in the neonatal rat spinal cord.

(S)-3,4-DCPG HCl ((S)-3,4-Dicarboxyphenylglycine HCl) is a selective metabotropic glutamate receptor 8a (mGluR8a) agonist that has an effect on human mGluR8-expressing AV12-664 cells with an EC50 of 31 nM.

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

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

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).

L-Cysteic acid monohydrate (3-Sulfo-L-alanine Monohydrate) is an oxidation product of L-cysteine that may be used as a competitive inhibitor of the bacterial aspartate: alanine antiporter (AspT) exchange of aspartate and in other aspartate biological systems. L-Cysteic acid monohydrate is used in monomeric surfactant development. L-Cysteic acid monohydrate may be used in studies of excitatory amino acids in the brain, such as those that bind to cysteine sulfinic acid receptors. It is a useful agonist at several rat metabotropic glutamate receptors (mGluRs).

VU0364770 (VU 0364770)(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.

VU6005649 is an agonist of CNS penetrant mGlu7 8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively).

PI-linked metabotropic glutamate receptors agonist

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).

VU0483605 is an effective and selective positive allosteric modulator of mGluR1 with EC50s of 390 and 356 nM for human and rat, respectively.

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.

MFZ 10-7 is anegative allosteric modulator of the mGluR5.

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.

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

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].

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

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

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.

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 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 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.

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.