Identification of serotonin 5-HT1A receptor partial agonists in ginger.
作者： Andreas Nievergelt , Peter Huonker , Roland Schoop , Karl-Heinz Altmann , Jürg Gertsch
DOI: 10.1016/J.BMC.2010.02.062
关键词: Chemistry 、 Biochemistry 、 Ginger Extract 、 Intestinal absorption 、 Pharmacology 、 Zingiber officinale 、 Partial agonist 、 5-HT1A receptor 、 Gingerol 、 Shogaol 、 5-HT receptor
摘要: Animal studies suggest that ginger (Zingiber officinale Roscoe) reduces anxiety. In this study, bioactivity-guided fractionation of a extract identified nine compounds interact with the human serotonin 5-HT(1A) receptor significant to moderate binding affinities (K(i)=3-20 microM). [(35)S]-GTP gamma S assays indicated 10-shogaol, 1-dehydro-6-gingerdione, and particularly whole lipophilic (K(i)=11.6 microg/ml) partially activate (20-60% maximal activation). addition, intestinal absorption gingerols shogaols was simulated their interactions P-glycoprotein were measured, suggesting favourable pharmacokinetic profile for active compounds.
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