High affinity of the naturally-occurring biflavonoid, amentoflavon, to brain benzodiazepine receptors in vitro.

In a search for pharmacologically-active ingredients in the plant extract Karmelitter Geist, we have isolated and identified a high-affinity benzodiazepine receptor ligand, amentoflavon. Amentoflavon binds in a mix-type competitive and non-competitive manner to brain benzodiazepine receptors with an IC50-value of 6 nM in vitro, comparable to the affinity of diazepam. Amentoflavon shows a GABA ratio of 1.4 at 0 degrees and increases 35S-TBPS binding by 12% (60 min incubation at 25 degrees), which indicates a partial agonistic effect on benzodiazepine receptors. The substance does not influence the binding of a variety of other brain receptor ligands. Amentoflavon does not inhibit 3H-flunitrazepam-binding to brain benzodiazepine receptors following i.v. administration in the mouse in vivo, and it is therefore not likely that amentoflavon is responsible for any pharmacological effect of Karmelitter Geist.