mglur5

mGluR5 antagonist-1 (compound 10) is a potent mGluR5 inhibitor exhibiting an IC50 of 11.5 nM and demonstrates antidepressant effects [1].

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.

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.

VU 0285683 is a specific negative allosteric modulator of mGluR5 with a high affinity for the MPEP binding site. VU 0285683 shows anxiolytic-like activity.

CHPG hydrochloride is a selective agonist of mGluR5.

5-(2-aminoethyl)-4-methyl-1,3-thiazol-2-amine dihydrochloride is a potent and selective antagonist of metabotropic glutamate receptor 5 (mGluR5). It has been shown to be effective in several neurological disorders, including fragile X syndrome, autism spectrum disorders, and addiction.

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

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.

DL-Willardiine (2-amino-3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)propanoic acid) is an unnatural amino acid, a derivative of glutamate. It is an agonist of mGluR5, which regulates the activity of enzymes involved in neurotransmitter synthesis and catabolism, and affects the activity of ion channels and other membrane proteins.

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

CHPG sodium salt is a selective agonist of mGluR5 and activates the ERK and Akt signaling pathways. CHPG sodium salt can be used in studies about traumatic brain injury.

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

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

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

CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5).

FTIDC is a highly potent and selective allosteric antagonist of mGluR1 receptors and shows very weak potency against human and rat mGluR5 receptors. The inhibition of FTIDC for mGluR1 receptors is shown to be in noncompetitive manner and displays IC50 val

VU-1545 is mGlu5 positive allosteric modulator.

L-Cysteinesulfinic acid monohydrate is a potent agonist at rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively[1].

(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator(EC50 of 168 nM for potentiation ).

VU-29 is a positive allosteric mGlu5 receptor modulator with EC50=9 nM and Ki=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).

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).

CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist (IC50: 2.6 nM). The selectivity of CFMTI to mGluR1 is higher 2000-fold than mGluR5.

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.

(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC 50 >1μM for mGluR5 receptor [1] . BMS-984923 is a potent mGluR5 silent allosteric modulator [2] .

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).

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).

(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 .

VU0357121, a positive allosteric modulator of mGlu5 (EC50: 33 nM), is inactive or very weakly antagonizing at other mGlu receptor subtypes.

CHPG is a selective agonist of mGluR5. In BV2 microglial cells, it attenuates SO2-induced oxidative stress and inflammation through the TSG-6/NF-κB pathway.

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

AZD 2066 hydrate is a selective, orally active, and brain-penetrant antagonist of mGluR5. It exhibits antinociceptive effects [1].

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

NPS2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 (IC50 of 5.2 and 82 nM, respectively)

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.

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.

VU0029251 serves as a partial antagonist of mGluR5, exhibiting a binding affinity with a K i of 1.07 μM. It also attenuates glutamate-induced calcium mobilization in HEK293 cell membranes that express rat mGluR5, demonstrating an IC 50 of 1.7 μM [1].

(RS)-MCPG ((±)-MCPG) is a non-selective group I/II metabotropic glutamate receptor antagonist.

Auglurant is a novel and selective mGlu5 antagonist (IC50: 11 nM (rat) and an IC50: 14 nM (human)). Auglurant has an acceptable CNS penetration.

ADX-47273 (BA 94673139) is a positive and selective allosteric modulator for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).

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

MTEP, a potent, non-competitive, and highly selective antagonist of mGluR5, exhibits an IC50 value of 5 nM and a K_i value of 16 nM. Demonstrating antidepressant and anxiolytic-like effects, MTEP is utilized in Parkinson's disease research.

GRN-529 is a selective negative allosteric modulator of the mGluR5 receptor.

L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs, pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively).

GSK2210875 is a mGluR5 antagonist with oral activity.

AZD 2066 is a selective, orally active, and brain-penetrant mGluR5 antagonist with analgesic 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.

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

BMS-984923 is an orally available and blood-brain barrier permeable mGluR5 silencing allosteric modulator that inhibits β-amyloid oligomer-induced aberrant synaptic signaling, and can be used to study Alzheimer's disease.

MRZ-8676 is an orally bioavailable and negative allosteric modulator of subtype 5 metabotropic glutamate receptors (mGluR5).

Fenobam hydrate is a noncompetitive antagonist and inverse agonist of metabotropic glutamate receptor 5 (mGluR5). It inhibits intracellular calcium mobilization induced by the glutamate analog quisqualate and inhibits basal activity of mGluR5. Fenobam reduces stress-induced hyperthermia, exhibits anxiolytic-like activity, and may induce analgesia.