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.
[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.