Structure-activity relationships of flavonoids, isolated from Scutellaria baicalensis, binding to benzodiazepine site of GABA(A) receptor complex

Planta Med. 2002 Dec;68(12):1059-62. doi: 10.1055/s-2002-36357.

Abstract

Twenty-six flavonoids were isolated from Scutellaria baicalensis. Their affinities for the benzodiazepine (BDZ) binding site of GABA A receptor have been studied using [ 3H]flunitrazepam binding to rat cortical membranes in vitro. The structure-activity relationships suggested that 2'-OH flavones exhibited the most potent binding affinity, which could lead to the design and discovery of new BDZ receptor ligands.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apigenin*
  • Binding Sites / drug effects
  • Flavanones*
  • Flavonoids / chemistry
  • Flavonoids / isolation & purification
  • Flavonoids / metabolism*
  • Flunitrazepam / pharmacology
  • GABA Modulators / pharmacology
  • Glucuronates*
  • Molecular Structure
  • Plant Extracts / chemistry
  • Plant Extracts / metabolism
  • Quantitative Structure-Activity Relationship*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, GABA-A / drug effects
  • Receptors, GABA-A / metabolism*
  • Scutellaria baicalensis*

Substances

  • Flavanones
  • Flavonoids
  • GABA Modulators
  • Glucuronates
  • Plant Extracts
  • Receptors, GABA-A
  • scutellarin
  • chrysin
  • baicalein
  • Flunitrazepam
  • Apigenin
  • scutellarein
  • flavanone