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

Abstract

α 1 -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 α 1 -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 α 1 -ARs agonists in α 1 -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 α 1 -AR subtype-selective ligands.

Synthesis, biological evaluation, and molecular docking of novel hydroxyzine derivatives as potential AR antagonists

“…The antagonistic activity of these derivatives against AR was assessed using luciferase assays ( Xu et al, 2014 ; Xu et al, 2015 ; Zuo et al, 2017 ; Xu et al, 2018 ). As shown in Table 2 , the compounds 3–10 exhibited weak antagonistic potency against AR.…”

Synthesis, bioactivity, and molecular docking of novel arylpiperazine derivatives as potential AR antagonists

“…The AR antagonist effect of tested compounds was evaluated using the luciferase reporter gene assay ( Xu et al, 2014 ; Xu et al, 2015 ; Zuo et al, 2017 ; Xu et al, 2018 ). Briefly, RLUs were used to indicate firefly and Renilla luciferase activity, and the activities were evaluated using dual luciferase assay kits (Promega) in accordance with the manufacturer’s instructions.…”