mglu5

CHPG hydrochloride is a selective agonist of mGluR5.

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.

ML353 (VU0478006) is a selective activator of TREK-1 and TREK-2 and a selective ligand (Ki =18.2 nM) for the mGlu5 Silencing Allosteric Modulator (SAM). ML353 has potential as a solution to the intrinsic activity or pharmacological blockade of SAM in vivo.

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

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.

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.

SIB-1757 (6-methyl-2-[(E)-phenyldiazenyl]pyridin-3) is a selective antagonist of mGlu5 metabotropic glutamate receptor subtype (hmGlu5, IC50 : 0.4 μM)

LSN2463359 is a positive allosteric modulators of the mGlu5 receptor.

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.

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].

NCFP is a mGlu5 positive allosteric modulator. It positively modulates mGlu5 without the induction of long-term potentiation and long-term depression in the hippocampus.

Raseglurant (ADX-10059) is an mGlu5 negative allosteric modulator. It effectively counters migraines and alleviates haloperidol-induced catalepsy in mice.

VU-1545 is mGlu5 positive allosteric modulator.

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.

allosteric potentiator of mGlu5

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

HTL14242 is a mGlu5 Negative Allosteric Modulator.

VU0404251 is a positive allosteric modulator of mGlu5.

VU0366248, a negative allosteric modulator of mGlu5, [5-(1,3-Diphenyl-1H-pyrazol-4-yl)-8-ethoxy-3-(4-isopropyl-phenyl)-6-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine], serves to inhibit the metabotropic glutamate receptor 5 (mGlu5), potentially impacting conditions associated with mGlu5 activity.

SIB-1893 is a highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype; displays an IC50 value of 0.3 μM at hmGlu5, compared with > 100 μM at hmGlu1b, hmGlu2, hmGlu6, hmGlu7 and hmGlu8. It positive allosteric modulator at mGlu4 receptors.

AZD-2066 hydrochloride is an mGlu5 antagonist.

LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu 5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC 50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). In vivo EEG studies demonstrated that LSN2463359 has marked wake-promoting properties with minimal rebound hypersomnolence, and it can be used for schizophrenia research [1].

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

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.