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• W2028326787 abstract "To find human dopamine receptors, especially D1-like receptor specific agonists from Chinese herbs as potential antihypertension drug leads. Two D1-like receptor cell lines carrying a β-lactamase reporter gene, and a D2 receptor cell line coexpressing a promiscuous G protein G1 5 were constructed using HEK293 cells. A natural compound library made from fractionated samples of herbal extracts was used for high-throughput screening (HTS) against one of the cell lines, HEK/D5R/CRE-blax. The interested hits were evaluated for their activities against various dopamine receptors. Fourteen hits were identified from primary screening, of which 2 of the better hit samples, HD0522 and HD0059, were selected for further material and activity analysis, and to obtain 2 compounds that appeared as 2 single peaks in HPLC, HD0522H01 and HD0059H01. HD0059H01 could activate D1, D2, and D5 receptors, with EC50 values of 2.28 μg/mL, 0.85 μg/mL, and 1.41 μg/mL, respectively. HD0522H01 could only activate D1R and D5R with EC50 values of 2.95 μg/mL and 8.38 μg/mL. We established cell-based assays for 3 different human dopamine receptors and identified specific agonists HD0522H01 and HD0059H01 through HTS. The specific agonist to D1-like receptors, HD0522H01, may become a new natural product-based drug lead for antihypertension treatment." @default.
• W2028326787 created "2016-06-24" @default.
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• W2028326787 date "2007-01-01" @default.
• W2028326787 modified "2023-10-06" @default.
• W2028326787 title "Identification of human dopamine receptors agonists from Chinese herbs" @default.
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• W2028326787 doi "https://doi.org/10.1111/j.1745-7254.2007.00460.x" @default.
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