mglur2 antagonist 1

mGluR2 antagonist 1 is a potent and selective class of negative allosteric modulator targeting the metabotropic glutamate receptor 2 (mGluR2) with high oral bioavailability. It displays a remarkable affinity for mGluR2, with an IC50 value of 9 nM. Furthermore, it exhibits excellent permeability across the blood-brain barrier, making it a promising candidate for central nervous system-related studies or therapies.

1-Benzyl-APDC acts as an agonist for mGluR6 in CHO cells, exhibiting an EC50 of 20 μM. Additionally, it functions as a weak antagonist for mGluR2, with an IC50 of 200 μM.

mG2N001, a negative allosteric modulator (NAM) of the metabotropic glutamate receptor mGluR2, has an IC50 of 93 nM and binds to mGluR2 as an antagonist with a Ki of 63 nM. This compound is microparticle- and plasma-stable, and its radioisotope [11C] mG2N001 can be utilized in PET imaging. [11C] mG2N001 exhibits good brain heterogeneity and penetration, selectively accumulating in mGluR2-rich regions to produce high-contrast brain images [1].