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Molecules 2014, 19(8), 12699-12709; https://doi.org/10.3390/molecules190812699

Identification of Two Novel α1-AR Agonists Using a High-Throughput Screening Model

Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, China
These authors contributed equally to this work.
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Author to whom correspondence should be addressed.
Received: 17 June 2014 / Revised: 1 August 2014 / Accepted: 12 August 2014 / Published: 20 August 2014
(This article belongs to the Section Medicinal Chemistry)
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Abstract

α1-Adrenoceptors (ARs; 1A, 1B, and 1D) have been determined to perform different prominent functions in the physiological responses of the sympathetic nervous system. A high-throughput screening assay (HTS) was set up to detect α1-AR subtype-selective agonists by a dual-luciferase reporter assay in HEK293 cells. Using the HTS assay, two novel compounds, CHE3 and CHK3, were discovered as α1-ARs agonists in α1-ARs expressed in HEK293 cells. These compounds also showed moderate/weak anti-proliferative activities against tested cancer cell lines. The HTS assay proposed in this study represents a potential method for discovering more α1-AR subtype-selective ligands. View Full-Text
Keywords: agonist; α1-ARs; HTS model; anti-proliferative activities; subtype-selectivity agonist; α1-ARs; HTS model; anti-proliferative activities; subtype-selectivity
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Xu, F.; Chen, H.; He, X.; Xu, J.; Xu, B.; Huang, B.; Liang, X.; Yuan, M. Identification of Two Novel α1-AR Agonists Using a High-Throughput Screening Model. Molecules 2014, 19, 12699-12709.

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