Platelet activating factor (PAF) is ubiquitous in mammals, and may have multiple functions in the central nervous system. Triazolobenzodiazepine compounds are active both at the GABAA receptor and as PAF antagonists. To investigate whether PAF antagonist activity is involved in the actions of triazolobenzodiazepines, we examined effects of two non-benzodiazepine PAF antagonists on binding and function at the GABAA receptor. The gingkolide terpene, BN 52021 and the dioxolane-based compound BN 52115 had no effect on benzodiazepine binding or chloride channel binding in cortical membrane preparations. However, chloride uptake into cortical synaptoneurosomes was enhanced with 1 microM BN 52021 but not 1 microM BN 52115. The effect of BN 52021 was prevented by 1 microM flumazenil. PAF antagonists appear to augment GABAA receptor function without affecting binding.