Biological Activity
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.
In 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 receptors
In 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.
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.