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  • Authors: Dinh, Doan Long; Simmen, Urs; Berger Bueter, Karin; Beuter, Bernd; Lundstrom, Kenneth; Schaffner, Willi (2001)

  • Methanolic leaf and root extracts of the Hawaiian kava (Piper methysticum Forst.) cultivars, Mahakea, Nene, Purple Moi and PNG, were tested on binding affinities to CNS receptors including GABAA (GABA and benzodiazepine binding site), dopamine D2, opioid (μ and δ), serotonin (5-HT6 and 5-HT7) and histamine (H1 and H2). HPLC analysis was carried out in order to determine the amount of the main kavalactones kavain, 7,8-dihydrokavain, methysticin, 7,8-dihydromethysticin, yangonin and 5,6-demethoxyyangonin. The most potent binding inhibition was observed for leaf extracts to GABAA receptors (GABA binding site) with IC50 values of approximately 3 μg/ml, whereas root extracts were less active with IC50 values ranging from 5 μg/ml (Nene) to 87 μg/ml (Mahakea). Since the leaf extracts gener...