metabotropic glutamate

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

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

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

LY-2300559 is an agonist of metabotropic glutamate receptor 2 (mGluR2) and can be used in studies about the treatment of migraine.

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

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

(-)-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.

STX-107 is a potent and selective mGluR5 agonist for the study of Fragile X Syndrome.

(2R,4R)-APDC, a selective group II metabotropic glutamate receptors (mGluRs) agonist, exhibits anticonvulsant and neuroprotective effects.

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.

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

(S)-3-Hydroxyphenylglycine is an agonist of group I metabotropic glutamate receptors (mGluRs).

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.

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.

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