For research use only. Not for therapeutic Use.
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability[1].
In vivo, mGluR2 antagonist 1 (Compound 25) reverses the effect of mGluR2 agonist LY379268 in amphetamine-induced hyperlocomotion and shows good efficacy in the mouse delayed non-match to position assay at 10 mg/kg.
| Catalog Number | I015278 |
| CAS Number | 1432728-49-8 |
| Synonyms | 7-[(2,5-dioxopyrrolidin-1-yl)methyl]-4-(4-fluorophenyl)quinoline-2-carboxamide |
| Molecular Formula | C21H16FN3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H16FN3O3/c22-14-4-2-13(3-5-14)16-10-18(21(23)28)24-17-9-12(1-6-15(16)17)11-25-19(26)7-8-20(25)27/h1-6,9-10H,7-8,11H2,(H2,23,28) |
| InChIKey | XSTBUOHORFUCIB-UHFFFAOYSA-N |
| SMILES | C1CC(=O)N(C1=O)CC2=CC3=C(C=C2)C(=CC(=N3)C(=O)N)C4=CC=C(C=C4)F |
| Reference | [1]. Youheng Shu,et al. Discovery of 4-arylquinoline-2-carboxamides, Highly Potent and Selective Class of mGluR2 Negative Allosteric Modulators: From HTS to Activity in Animal Models. Bioorg Med Chem Lett. 2020 May 1;30(9):127066. |
