5-Hydroxytryptamine2A receptor binding activity of compounds from Litsea sessilis.

Autor: Chung, Lip Yong, Lo, Mee Wah, Mustafa, Muhammad Rais, Goh, Swee Hock, Imiyabir, Zamrie
Zdroj: Phytotherapy Research; Mar2009, Vol. 23 Issue 3, p330-334, 5p
Abstrakt: A 96-well microplate filtration based 5-HT2A receptor-radioligand binding assay was optimized and adopted to carry out a bioassay-guided fractionation of the methanol extract of the leaves of Litsea sessilis. This purification led to the isolation of two compounds identified as (+)-boldine (1) and (+)-dehydrovomifoliol (2). (+)-Boldine binds to 5-HT2A receptors at high concentrations with a Ki value of 2.16 µ m. However, (+)-dehydrovomifoliol showed minimal competitive inhibition on the binding of [3H]ketanserin to the same receptor with a Ki value of 2.06 m m. These results suggest that (+)-boldine influences the activity of 5-HT2A receptors through competitive binding as an agonist or antagonist. Copyright © 2008 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index