- Inhibition of fatty acid amide hydrolase by BIA 10-2474 in rat brain.
Inhibition of fatty acid amide hydrolase by BIA 10-2474 in rat brain.
Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism (2016-09-22)
Junchao Tong, Romina Mizrahi, Sylvain Houle, Stephen J Kish, Isabelle Boileau, Jose Nobrega, Pablo M Rusjan, Alan A Wilson
PMID27650910
ABSTRACT
In a recent clinical trial, the drug BIA 10-2474, a putative fatty acid amide hydrolase(FAAH) inhibitor, 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. We synthesised BIA 10-2474 and determined its ability to inhibit FAAH ex vivo in rat brain using a FAAH selective radiotracer. BIA 10-2474 proved to be a potent FAAH inhibitor with IC