Background:

CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist with IC50 of 2.6 nM. The selectivity of CFMTI to mGluR1 over mGluR5 was >2000-fold.target : mGluRIC 50: 2.6 nMIn vitro: The IC50 values of CFMTI against human mGluR5 were 5400 ± 1200 nM, showing that the activity of CFMTI is more than 2000-fold weaker against human mGluR5 than against human mGluR1. CFMTI up to 10 μM exhibited no agonistic activity toward any group I mGluR subtypes (data not shown). The IC50 values of CFMTI were higher than 10 μM against all targets, such as NMDA receptorsIn vivo: CFMTI can dissolve in ethanol, polyethylene glycol 400, and distilled water (1:4:5, v/v/v) for intravenous administration. Oral administration of CFMTI inhibited DHPG-induced face-washing behavior in a dose-dependent manner. CFMTI produced dose-dependent inhibition of specific ex vivo binding of [3H]FTIDC to striatal and cerebellar slices in mice. CFMTI significantly inhibit hyperlocomotion induced by MAP at a dose of 2 mg/kg.

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