In vitro and in silico analysis of the vascular effects of asymmetrical N,N-bis(alkanol)amine aryl esters, novel multidrug resistance-reverting agents

@article{Fusi2016InVA,
  title={In vitro and in silico analysis of the vascular effects of asymmetrical N,N-bis(alkanol)amine aryl esters, novel multidrug resistance-reverting agents},
  author={Fabio Fusi and Miriam Durante and Ottavia Spiga and Alfonso Trezza and Maria Frosini and Elisa M. Floriddia and Elisabetta Teodori and Silvia Dei and Simona Saponara},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={2016},
  volume={389},
  pages={1033 - 1043}
}
Asymmetrical N,N-bis(alkanol)amine aryl esters (FRA77, GDE6, and GDE19) are potent multidrug resistance (MDR) reversers. Their structures loosely remind that of the Ca2+ antagonist verapamil. Therefore, the aim of this study was to investigate their vascular activity in vitro. Their effects on the mechanical activity of fresh and cultured rat aorta rings on Cav1.2 channel current (ICa1.2) of A7r5 cells and their cytotoxicity on A7r5 and EA.hy926 cells were analyzed. Docking at the rat α1C… 

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