title: Isolation and identification of 6-methylapigenin, a competitive ligand for the brain GABA(A) receptors, from Valeriana wallichii.
abstract: Using the guidance by a competitive assay for the benzodiazepine binding site in the GABA(A) receptor, active compounds were isolated from the rhizomes and roots of Valeriana wallichii DC. The UV, NMR and mass spectral data permitted the identification of 6-methylapigenin. This flavonoid has a Ki = 495 nM for the BDZ-bs and a GABA ratio of 1.6-2.0, which suggests possible agonistic properties. The calculated percentage of 6-methylapigenin in the crude drug is in the range: 0.013% to 0.0013%.
authors.affiliation: Instituto de Química y Fisicoquímica Biológicas, Facultad de Farmacia y Bioquímica, Juín, Buenos Aires, Argentina.
authors.forename: Cristina
authors.initials: C
authors.lastname: Wasowski
authors.forename: Mariel
authors.initials: M
authors.lastname: Marder
authors.forename: Haydeé
authors.initials: H
authors.lastname: Viola
authors.forename: Jorge Horacio
authors.initials: JH
authors.lastname: Medina
authors.forename: Alejandro Constantino
authors.initials: AC
authors.lastname: Paladini
mesh_terms: D000818:Animals; D003975:Diazepam / Q000378:metabolism; D005419:Flavonoids / Q000737:chemistry / Q000378:metabolism*; D018757:GABA Modulators / Q000737:chemistry / Q000378:metabolism*; D009682:Magnetic Resonance Spectroscopy; D008517:Phytotherapy; D018517:Plant Roots; D011485:Protein Binding; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism*; D013056:Spectrophotometry, Ultraviolet; D013687:Telencephalon / Q000378:metabolism*; D014632:Valerian
chemical_list: C469106:6-methylapigenin; D005419:Flavonoids; D018757:GABA Modulators; D011963:Receptors, GABA-A; D003975:Diazepam