mglur

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

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

(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) is a non-essential amino acid that exists in large quantities in the human body and participates in many metabolic processes. L-Glutamine provides a carbon source for oxidation in certain cells.

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

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).

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

VU0155094 (ML 397) is a positive allosteric modulator with differential activity at the various group III mGluRs.

(S)-MCPG ((+)-MCPG) is a class I II metabotropic glutamate receptors (mGluRs) antagonist that blocks spatial learning and long-term enhancement of the dentate gyrus in vivo in rats, and can be used to study neurological disorders.

Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3, developed as an antidepressant.

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.

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.

(E/Z)-SIB-1893 (SIB 1893) is the racemate of (E)-SIB-1893 and (Z)-SIB-1893. (E)-SIB-1893 is a selective, noncompetitive mGluR5 antagonist with anticonvulsant activity .

VU-1545 is mGlu5 positive allosteric modulator.

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].

VU0360172 is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM).