The preclinical pharmacology of flumazenil.

Flumazenil (Ro 15-1788) is a ligand of the benzodiazepine receptor (BZR) with high affinity, great specificity and minimal positive intrinsic efficacy, which reaches its sites of action within the CNS very rapidly after i.v. and oral administration and which prevents and reverses dose-dependently all effects that BZR agonists and inverse agonists produce via the BZR. General aspects of the competitive interaction between flumazenil and BZR agonists are illustrated here. Flumazenil has slight partial agonistic properties that can be seen as a built-in safety mechanism when used in reversing agonist effects and that may be of use in the treatment of epilepsies.