The effects of bilobalide, a sesquiterpene isolated from the leaves of Ginkgo biloba L., were investigated in a rat hippocampal slice preparation. Bilobalide (10-500 microM) significantly increased the amplitude of population spikes evoked by electrical stimulation of Schaffer collateral/commissural fibers in a concentration-dependent manner. Paired-pulse inhibition at interpulse intervals of 10-50 ms was significantly reduced in the presence of bilobalide (50 microM). The inhibitory action of muscimol (1 microM) was attenuated by bilobalide (100 microM). These results suggest that bilobalide induces an enhancement of excitability of CA1 pyramidal neurons, which involves, at least in part, a reduction in GABAergic inhibition in rat hippocampus.