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In vitro study of the interaction of Tilia europeae L. aqueous extract with GABAA receptors in rat brain

The interaction of GABAA receptor‐complex in rat brain was investigated in vitro with aqueous extracts obtained from the inflorescences of Tilia europeae L., using the [3H]muscimol and [3H]flunitrazepam binding techniques to synaptic membranes and the uptake of 36Cl‐ to synaptoneurosomes from cortices. The extract inhibited [3H]muscimol binding, stimulated 36ClCl‐ uptake by synaptoneurosomes and displaced at high concentrations, the [3H]flunitrazepam bound to synaptic membranes. When analysed by HPLC, the aqueous extract of Tilia europeae L. contained several amino acids, including GABA (about 100 μM). This GABA content can justify the displacement of [3H]muscimol produced by the extract but it did not increase the binding of [3H]flunitrazepam, as expected. Probably the extract contains other benzodiazepine‐like substances which displace the [3H]flunitrazepam binding and counteract the expected GABA‐induced increase in [3H]flunitrazepam binding. © 1997 John Wiley & Sons, Ltd.