@article{APS3817,
author = {Yi-lin Zhang and Hai-qing Zhang and Xiao-yu Liu and Shi-neng Hua and Lu-bing Zhou and Jun Yu and Xue-hai Tan},
title = {Identification of human dopamine receptors agonists from Chinese herbs},
journal = {Acta Pharmacologica Sinica},
volume = {28},
number = {1},
year = {2016},
keywords = {},
abstract = {Aim: To find human dopamine receptors, especially D1-like receptor specific agonists
from Chinese herbs as potential antihypertension drug leads. Methods: Two
D1-like receptor cell lines carrying a β-lactamase reporter gene, and a D2 receptor
cell line coexpressing a promiscuous G protein G15 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. Results: 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. Conclusion: We established cellbased
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.},
issn = {1745-7254}, url = {http://www.chinaphar.com/article/view/3817}
}