Isolation and characterization of benzodiazepine receptor ligand from Scutellaria baicalensis Georgi

  • Hui, Kwok-Min
Publication date
January 2000

Abstract

Several naturally occuring monoflavonoids, isolated from Scutellaria baicalensis Georgi using silica gel and LH-20 chromatography, inhibited [3H] flunitrazepam binding to the central benzodiazepine receptors (BDZ-Rs) with high to moderately low binding affinity. The most potent one is 5,7,2’-trihydroxy-6,8-dimethoxyflavone (K36) with a Ki of 7.7 nM and the weakest one is baicalin with a Ki of 77.1 μM. The functional properties of wogonin (Ki=1.06 μM) and K36 were determined by electrophysiological studies, employing dorsal root ganglion (DRG) neurons and recombinant GABAA receptor functionally expressed in Xenopus laevis oocytes. Wogonin and K36 brought about an enhancement of the GABA-activated current, which could be reversed by the co-a...

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