AbstractLy81067, a diaryltriazine, represents a new class of compounds to enhance [3H]flunitrazepam binding to membranes of rat cerebral cortex. The enhancement induced by LY81067 exceeds that induced by γ‐aminobutyric acid (GABA) and is partially abolished by the GABA antagonists bicuculline and picrotoxin. Scatchard analysis on the saturable binding of [3H]flunitrazepam reveals that LY81067 at 10 μM increases mainly the affinity for the [3H]ligand, due to a reduced rate of dissociation of the receptor‐bound [3H]flunitrazepam. A dependence on chloride anions was demonstrated in the enhancement of [3H]flunitrazepam binding by LY81067. These findings suggest that the diaryltriazine LY81067 enhances [3H]flunitrazepam binding by exerting its effect at or near the picrotoxinsensitive anion recognition sites of the GABA/benzodiazepine receptor co