mglur5

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.

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.

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).

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.

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 with an IC50 of 11.5 nM, demonstrating antidepressant effects [1].

CHPG sodium salt is a selective agonist of mGluR5 that activates ERK and Akt signaling pathways and is utilized in studies on traumatic brain injury.

CHPG hydrochloride is a selective agonist of mGluR5.

Methoxy-PEPy is a potent and selective mGlu5 receptor inhibitor, exhibiting an IC50 value of 1 nM.

Dipraglurant (ADX48621) is a negative alteration modulator (NAM) of mGluR5 that inhibits dyskinesia in the LID macaque model.

LY382884 is a selective and potent GluR5 kainate receptor antagonist with anxiolytic activity.LY382884 blocks blockade of mossy fibre LTP induction.

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.

Topiramate (RWJ 17021) is a unique antiseizure medication that is used in the treatment of partial and generalized seizures. Topiramate has been rarely associated with hepatic injury and largely when used in combination with other anticonvulsant medications.