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  • Title: Identification of serotonin 5-HT1A receptor partial agonists in ginger.
    Author: Nievergelt A, Huonker P, Schoop R, Altmann KH, Gertsch J.
    Journal: Bioorg Med Chem; 2010 May 01; 18(9):3345-51. PubMed ID: 20363635.
    Abstract:
    Animal studies suggest that ginger (Zingiber officinale Roscoe) reduces anxiety. In this study, bioactivity-guided fractionation of a ginger extract identified nine compounds that interact with the human serotonin 5-HT(1A) receptor with significant to moderate binding affinities (K(i)=3-20 microM). [(35)S]-GTP gamma S assays indicated that 10-shogaol, 1-dehydro-6-gingerdione, and particularly the whole lipophilic ginger extract (K(i)=11.6 microg/ml) partially activate the 5-HT(1A) receptor (20-60% of maximal activation). In addition, the intestinal absorption of gingerols and shogaols was simulated and their interactions with P-glycoprotein were measured, suggesting a favourable pharmacokinetic profile for the 5-HT(1A) active compounds.
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