Structure-activity relationships of flavonoids, isolated from Scutellaria baicalensis, binding to benzodiazepine site of GABA(A) receptor complex.
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.
Wang
Hongyan
H
Department of Natural Product Chemistry, Shenyang Pharmaceutical University, P.R.China. syliu@mail.sy.In.cn
Hui
Kwok-Min
KM
Chen
Yingjie
Y
Xu
Suixu
S
Wong
J Tze-Fei
JT
Xue
Hong
H
D000818:Animals; D047310:Apigenin; D001665:Binding Sites / Q000187:drug effects; D044950:Flavanones; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism*; D005445:Flunitrazepam / Q000494:pharmacology; D018757:GABA Modulators / Q000494:pharmacology; D005965:Glucuronates; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000378:metabolism; D021281:Quantitative Structure-Activity Relationship; D051381:Rats; D017207:Rats, Sprague-Dawley; D011963:Receptors, GABA-A / Q000187:drug effects / Q000378:metabolism*; D031364:Scutellaria baicalensis
D044950:Flavanones; D005419:Flavonoids; D018757:GABA Modulators; D005965:Glucuronates; D010936:Plant Extracts; D011963:Receptors, GABA-A; C484876:scutellarin; C043561:chrysin; C006680:baicalein; D005445:Flunitrazepam; D047310:Apigenin; C458179:scutellarein; C028610:flavanone