mglu5

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.

LSN2463359 is a positive allosteric modulators of the mGlu5 receptor.

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.

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

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.

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.

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.

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.

Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist. Mavoglurant (racemate) is the racemate of mavoglurant.

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

VU0364770 hydrochloride is a potent and selective mGlu4 positive allosteric modulator (PAM) (EC50s: 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively).

VU0652835 is a negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGlu5) (IC50: 81 nM).

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

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).

JNJ-46778212 (VU 0409551) is a potent and selective mGlu5 allosteric modulator (EC50: 260 nM) used for neurodissection studies.

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

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

VU6043653 is an effective, selective, and blood-brain barrier-permeable negative allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGlu5), with an IC50 value of 325 nM against h mGlu5.

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

VU6033685 is an orally effective positive allosteric modulator (PAM) of mGlu1, capable of positively modulating human mGlu1 and mGlu5, with EC50 values of 39 nM and 3960 nM, respectively. Additionally, VU6033685 inhibits CYP1A2, CYP2C9, and CYP2D6 with IC50 values of 26, 22.3, and 23.8 μM. It reverses amphetamine-induced hyperactivity in rats and protects against MK-801-induced cognitive deficits. VU6033685 demonstrates favorable pharmacokinetic properties in rats, with an oral bioavailability of 42.8%.

A-841720 is a potent, selective, and non-competitive antagonist of the mGlu1 receptor, exhibiting an IC 50 value of 10 nM specifically for the human mGlu1 receptor. It demonstrates a 34-fold greater selectivity for mGlu1 over mGlu5 (IC 50 of 342 nM), with negligible activity across a spectrum of other neurotransmitter receptors, ion channels, and transporters. Additionally, A-841720 possesses analgesic potential within a certain dose range [1] [2].

mGlu5 receptor antagonist

allosteric potentiator of mGlu5