Identification of serotonin 5-HT1A receptor partial agonists in ginger

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

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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:

06 Dec 2013 13:22

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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