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.
IC 50
mGluR1
References
[1] Eric D Hostetler, et al. Synthesis, Characterization, and Monkey PET Studies of [18F]MK-1312, a PET Tracer for Quantification of mGluR1 Receptor Occupancy by MK-5435. Synapse. 2011 Feb;65(2):125-35. DOI:10.1002/syn.20826
