1860797-76-7
1860797-76-7
Chemical Structure
VU6004909
- CAS No.: 1860797-76-7
- Formula:C21H15FN2O4
- Molecular Weight:378.35
InChIKey: OFLFGTPTGVETJG-UHFFFAOYSA-N
SMILES: O=C(C1=C(C)C=CO1)NC2=CC=C(N3C(C4=CC=C(C)C=C4C3=O)=O)C=C2F
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
VU6004909 | 99.40% | 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. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Dogra S, et al. Metabotropic Glutamate Receptors As Emerging Targets for the Treatment of Schizophrenia. Mol Pharmacol. 2022 May;101(5):275-285. [Content Brief]
- [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. [Content Brief]
- [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.
Keywords
