Nievergelt, Andreas; Huonker, Peter; Schoop, Roland; Altmann, Karl-Heinz; Gertsch, Jürg (2010). Identification of serotonin 5-HT1A receptor partial agonists in ginger. Bioorganic & medicinal chemistry, 18(9), pp. 3345-51. Amsterdam: Elsevier 10.1016/j.bmc.2010.02.062
Full text not available from this repository.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.
Item Type: |
Journal Article (Original Article) |
|---|---|
Division/Institute: |
04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Biochemistry and Molecular Medicine |
UniBE Contributor: |
Gertsch, Jürg |
ISSN: |
0968-0896 |
Publisher: |
Elsevier |
Language: |
English |
Submitter: |
Factscience Import |
Date Deposited: |
04 Oct 2013 14:12 |
Last Modified: |
05 Dec 2022 14:01 |
Publisher DOI: |
10.1016/j.bmc.2010.02.062 |
PubMed ID: |
20363635 |
Web of Science ID: |
000277083400036 |
URI: |
https://boris.unibe.ch/id/eprint/2440 (FactScience: 204939) |
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