BIA10-2474

Description: BIA 10-2474 is a novel, potent, long-acting and reversible inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions. In a recent clinical trial, the drug BIA 10-2474 was responsible for severe adverse events (SAEs), including one death. To date, there has been little reliable information divulged about the potency of BIA 10-2474 at FAAH in the central nervous system. BIA 10-2474 proved to be a potent FAAH inhibitor with IC50s of 50-70?ug/kg (i.p.) in various brain regions. This information may be useful for determining the cause of the SAEs.

References: J Pharmacol Pharmacother. 2016 Jul-Sep; 7(3):120-6; J Cereb Blood Flow Metab. 2017 Nov; 37(11):3635-3639.