VU6004909

VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC50s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy[1][2][3].

Product Specifications

CAS Number

[1860797-76-7]

UNSPSC

12352005

Target

MGluR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/vu6004909.html

Purity

99.40

Solubility

DMSO : 6.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=C(C)C=CO1)NC2=CC=C(N3C(C4=CC=C(C)C=C4C3=O)=O)C=C2F

Molecular Formula

C21H15FN2O4

Molecular Weight

378.35

References & Citations

[1]Dogra S, et al. Metabotropic Glutamate Receptors As Emerging Targets for the Treatment of Schizophrenia. Mol Pharmacol. 2022 May;101 (5) :275-285.|[2]Garcia-Barrantes PM, et al. Lead optimization of the VU0486321 series of mGlu (1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool. Bioorg Med Chem Lett. 2016 Feb 1;26 (3) :751-756.|[3]Samantha E. Yohn, et al. Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators. Mol Psychiatry. 2020; 25 (11) : 2786–2799.