Flumazenil is a benzodiazepine receptor antagonist. It is currently us
ed mainly in the anaesthetic and emergency rooms to reverse the effect
of exogenous benzodiazepines. Its use in a variety of experimental an
imal models and in human neuropsychiatric disorders continues to gener
ate a wealth of information on the possible role of the benzodiazepine
-GABA(A) receptor complex in their pathogenesis. In addition, labelled
with carbon-11, flumazenil has proved to be one of the most successfu
l positron emission tomography ligands stimulating research on the rol
e of the benzodiazepine receptor in these disorders. This review focus
es on the current state of play of flumazenil as a therapeutic or inve
stigative agent in neuropsychiatry, citing also the relevant animal mo
dels.