Journal article
Identification of serotonin 5-HT1A receptor partial agonists in ginger.
- Nievergelt A Department of Chemistry and Applied Biosciences, ETH 8093 Zurich, Switzerland.
- Huonker P
- Schoop R
- Altmann KH
- Gertsch J
- 2010-04-06
Published in:
- Bioorganic & medicinal chemistry. - 2010
Anti-Anxiety Agents
Caco-2 Cells
Catechols
Cell Line
Fatty Alcohols
Ginger
Humans
Molecular Structure
Serotonin 5-HT1 Receptor Agonists
English
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.
- Language
-
- English
- Open access status
- closed
- Identifiers
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- DOI 10.1016/j.bmc.2010.02.062
- PMID 20363635
- Persistent URL
- https://sonar.ch/global/documents/265376
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