Overview
- Hanrahan, J.R. et al. (2003) Bioorg. Med. Chem. Lett. 13, 2281.
- Nielsen, M. et al. (1988) Biochem. Pharmacol. 37, 3285.
- Butterweck, V. et al. (2002) Psychopharmacology (Berl.) 162, 193.
Alomone Labs Amentoflavone inhibits specific binding of Flunitrazepam to rat brain GABA(A) receptors.Percent inhibition of specific binding of 1 nM [3H]Flunitrazepam to membranes from whole rat brain (except cerebellum) was plotted against concentrations of Amentoflavone (#A-165), (green circles) and of Diazepam (assay standard, black squares) and used to calculate IC50 and Ki values for Amentoflavone (IC50 ≈ 4.95 nM, and Ki ≈ 4.03nM).
Amentoflavone is a natural compound derived from the plant Selaginella tamariscina. It is a negative allosteric modulator of GABA(A) receptors. Amentoflavone can be found in a number of plants with medicinal properties including Ginkgo biloba and Hypercium perforatum. Amentoflavone is the first high affinity ligand known for the benzodiazepine receptor devoid of nitrogen in its structure. It has been hypothesized recently that amentoflavone can cross the blood brain barrier in vivo by passive diffusion. In addition to its effect on GABA receptors, amentoflavone inhibits binding at 5-HT, D3-dopamine and δ-opioid receptors. The action of amentoflavone on the GABA(A) receptor is independent of high affinity benzodiazepine modulatory sites on the receptor. Amentoflavone and other substances of the flavone class have been found to exert anxiolytic activity in mice without the side effect associated with the use of benzodiazepines1.
