BioCentury
ARTICLE | Targets & Mechanisms

Losing sleep over flumazenil

December 20, 2012 8:00 AM UTC

Emory University researchers have identified excessive daytime sleepiness as a repurposing opportunity for flumazenil, a generic GABAA receptor antagonist.1 Although safety issues have stymied prior attempts to use GABAA receptor antagonists in this chronic indication, the group thinks a new formulation could make it possible.

Flumazenil is the only FDA-approved GABAA antagonist. It is a competitive antagonist that targets the benzodiazepine binding site on GABAA receptors and is marketed to treat sedative overdose and improve recovery from anesthesia...