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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
MGluR1
Available Sizes
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