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Philanthotoxin 74 dihydrochloride is an antagonist of AMPAR with IC50s of 263 and 296 nM for GluR3 and GluR1.

UBP310 (UBP 310) is a GLUK5 kainate receptor antagonist

Topiramate-D12 is a deuterium labeled Topiramate. Topiramate (T0675) is an agent of broad-spectrum antiepileptic. Topiramate (T0675) is an antagonist of GluR5 receptor.

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].

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.

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.

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

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

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

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.

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.

DMeOB (3,3'-Dimethoxybenzaldazine) is a negative regulator with mGluR5 agonist activity and can be used to study neurological diseases.

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

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.

DCG-IV is an effective agonist of class II mGluR. DCG-IV has anticonvulsant and neuroprotective effects. The EC50 of mGlu2R and mGlu3R are 0.35 and 0.09 μM, respectively. DCG-IV is also a competitive antagonist of Group I (IC50: mGlu1 / 5R = 389/630 μM) a

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.

L-Cysteinesulfinic acid is an endogenous neurotransmitter with agonistic effects on a variety of metabotropic glutamate receptors (mGluRs), including mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, with a pEC50 = 2.7 to 4.0. L- Cysteinesulfinic acid is a pld-coupled agonist of metabotropic excitatory amino acid (EAA) receptors.

Mavoglurant (AFQ056) is a potent, selective, non-competitive, and orally active metabotropic glutamate receptor 5 (mGluR5) antagonist with an IC50 of 30 nM, demonstrating greater than 300-fold selectivity over 238 tested targets, and it is widely applied in research on Fragile X syndrome and L-dopa-induced dyskinesias in Parkinson’s disease, while Mavoglurant incorporated alkyne functional group, which enables copper-catalyzed azide–alkyne cycloaddition click chemistry, facilitating target engagement and molecular tracking studies.

MFZ 10-7 hydrochloride is a highly potent and selective negative allosteric modulator of mGluR5 (NAM).

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