mglur 5

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

CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases.

AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux.

LY339434 HCl is a low affinity GluR5 erythrocyte receptor agonist.LY339434 HCl causes rapid neuronal death primarily by affecting N-methyl-D-aspartate (NMDA) receptors.

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).

S-Sulfo-L-cysteine sodium salt shows a weak affinity for mGluR1α and mGluR5a at high concentrations and has potential antioxidant activity.

ABP688 is a non-competitive and selective mGluR5 antagonist(Ki = 1.7 nM). ABP688 can be used as a PET tracer for clinical imaging.

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).

GET73 (Gamma hydroxybutyric acid analogue) is an negative allosteric modulator of mGluR5. GET73 is a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties.

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

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

VU-1545 is mGlu5 positive allosteric modulator.

AZD6538 is an mGluR5 negative allosteric modulator used in the study of CNS-related diseases such as Alzheimer's disease.

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

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.

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.

DHPG ((RS)-3,5-DHPG) is an effective antagonist of mGluR linked to phospholipase D. As an amino acid, it serves as a selective and potent agonist for Group I mGluR (mGluR 1 and mGluR 5) without affecting Group II or Group III mGluRs.

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].

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.