1860797-76-7
1860797-76-7
Chemical Structure
VU6004909
- CAS 番号: 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].
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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. | ||||||||||||||||||||
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Structural Analogs
-
Similarity Score 0.65
HY-118179VU0486321 -
Similarity Score 0.54
HY-150234LabMol-319 -
Similarity Score 0.54
HY-15706H2L 5765834 -
Similarity Score 0.52
HY-115796VU0477886 -
Similarity Score 0.51
HY-123643Brilliant sulfaflavine -
Similarity Score 0.50
HY-163109Carbonic anhydrase inhibitor 16 -
Similarity Score 0.50
HY-W0754055-(1,3-Dioxoisoindolin-2-yl)isophthalic acid -
Similarity Score 0.50
HY-14612CPPHA -
Similarity Score 0.49
HY-W8562105-(5-(3-Nitrophenoxy)-1,3-dioxoisoindolin-2-yl)isophthalic acid -
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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.
