| Identification | Back Directory | [Name]
N-[4-(1,3-Dihydro-5-methyl-1,3-dioxo-2H-isoindol-2-yl)-2-fluorophenyl]-3-methyl-2-furancarboxamide | [CAS]
1860797-76-7 | [Synonyms]
| [Molecular Formula]
C21H15FN2O4 | [MOL File]
1860797-76-7.mol | [Molecular Weight]
378.35 |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
Human mGluR1: 25.7 nM (EC50); rat mGluR1: 31 nM (EC50) | [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. DOI:10.1124/molpharm.121.000460
[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. DOI:10.1016/j.bmcl.2015.12.104
[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. |
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