Flumazenil (Ro 15-1788) antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS), thereby preventing the chloride channel opening events and inhibiting neuronal hyperpolarization. As a result, flumazenil reverses benzodiazepine-induced effects including sedation, psychomotor deficits, amnesia, and hypoventilation in a dose-dependent manner. Flumazenil is an imidazobenzodiazepine derivative, effective in reversing benzodiazepine-induced activities.

在BALB / c小鼠的高架十字迷宫和光/暗测试测试中, Flumazenil（1 mg/kg）有很强的抗焦虑效果.在小鼠中,慢性乙醇撤回引起的变化会被Flumazenil（3 mg/kg）阻止,导致开放臂时间和开放臂入口百分比减少.在大鼠中Flumazenil（10 mg/kg）有效地防止四氢孕酮产生的还原作用.在小鼠中,Flumazenil（5-20 mg/kg）对地西泮有拮抗作用,但对GYKI52466的抗惊厥和不良反应没有效果.在MES模型而不是在PTZ测试中,Flumazenil可使NBQX抗惊厥的活性稍微降低.Flumazenil可与中央苯（并）二氮受体结合,从而拮抗或扭转苯（并）二氮反兴奋剂和激动剂对神经系统及电生理效应的作用.Flumazenil可逆转苯（并）二氮和其它药物联用引起的中毒镇静反应,但不适用于环状抗抑郁中毒.