LY3020371 hydrochloride exerts an antidepressant-like signature in vivo. LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2 3 receptor (mGlu2 3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM.
Eglumegad is a highly effective and selective agonist of group II (mGlu2 3) receptor (IC50s: 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively).
LY3027788, a diester analog of LY3020371, an mGlu2 3 receptor antagonist, is a highly potent and orally active prodrug of LY3020371. Notably, LY3027788 exhibits significant antidepressant efficacy.