Bilobalide is a natural non-selective blocker of the 5-HT3A and GABA(A) channels. Balobalide is a sesquiterpene trilactone extracted from the leaves of the tree Ginkgo bilboa. Bilobalide has an effective concentration of 1-100 μM and an IC50 of 470 μM for the 5-HT3A receptor3 and an IC50 of 4.6±0.5 μM for the GABA(A) receptor. Bilobalide also binds to other anion Cys-loop receptors such as glycine receptors with a much higher affinity than to the 5-HT3A receptor. Bilobalide inhibits direct GABA mediated currents from recombinant human GABA(A) receptors thus suggesting it enhances neuronal excitability. Bilobalide is used in traditional Japanese medicine as a memory enhancer, treating symptoms associated with mild-moderate dementia and improving cognitive functions related to old age and senility
