GABA(A)-receptor ligands of flavonoid structure.
This review describes the new research developments that have established the CNS-activity of some natural flavonoids. The properties of flavone, chrysin, apigenin and cirsiliol are described and a survey of the occurrence of ligands for the benzodiazepine binding site in the flavonoid field is attempted. Natural compounds, structurally related to flavonoids and with similar CNS-activities, are also included. A medicinal chemistry approach to improve the biochemical and pharmacological properties of the flavone nucleus is described alongside with the enumeration of the principal achievements obtained to date. Quantitative structure-activity relationships studies leading to the formulation of pharmacophore models presumably describing the characteristics of the flavone-binding site in the GABA(A)-receptor are summarized.
Marder
Mariel
M
Instituto de Quimica y Fisicoquimica Biologicas, Facultad de Farmacia y Bioquimica, Junin 956, Buenos Aires, 1113, Argentina.
Paladini
Alejandro C
AC
D000818:Animals; D047310:Apigenin; D001569:Benzodiazepines / Q000378:metabolism; D001665:Binding Sites; D047309:Flavones; D005419:Flavonoids / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D018682:GABA Agents / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D008024:Ligands; D008958:Models, Molecular; D021281:Quantitative Structure-Activity Relationship; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism
D047309:Flavones; D005419:Flavonoids; D018682:GABA Agents; D008024:Ligands; D011963:Receptors, GABA-A; D001569:Benzodiazepines; C039824:cirsiliol; C043561:chrysin; D047310:Apigenin; C043562:flavone