rat mglur5

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).

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

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].

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.

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

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

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

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

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

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].

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.

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].