Background:

DFMTI can completely block the rmGlu1 L757V glutamate response.In vitro: DFMTI can completely block the rmGlu1 L757V glutamate response, although significantly higher concentrations were required to induce blockade.In vivo: DFMTI is efficacious in disrupting prepulse inhibition when dosed orally in rats. DFMTI exhibits a moderate decrease in human potency of approximately 3-fold when compared to rat, exemplified by DFMTI.

[1]. Cho HP et al. A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors. ACS Chem Neurosci. 2014 Jul 16;5(7):597-610.