Development of norepinephrine transporter reuptake inhibition assays using SK-N-BE(2)C cells. Issue 5 (May 2018)

• Record Type: Journal Article
• Authors: Decker, Ann M.; Blough, Bruce E.
• Is Part Of: Heliyon. Volume 4:Issue 5(2018)
• Publication Date: 2018-05
• Subjects: Neuroscience; Research -- Periodicals; Medical sciences -- Periodicals; Natural history -- Periodicals; Social sciences -- Periodicals; Earth sciences -- Periodicals; Physical sciences -- Periodicals; 507.2
• DOI: 10.1016/j.heliyon.2018.e00633
• Languages: English
• ISSNs: 2405-8440

Abstract

Abstract: This report describes efforts to develop and validate novel norepinephrine transporter reuptake inhibition assays using human neuroblastoma SK-N-BE(2)C cells in 24-well format. Before conducting the assays, the SK-N-BE(2)C cells were first evaluated for their ability to uptake [ 3 H]norepinephrine and were shown to have a saturable uptake with a KM value of 416 nM. Using this determined KM value, reuptake inhibition assays were then conducted with a variety of ligands including antidepressants, as well as piperazine and phenyltropane derivatives. The results obtained with the SK-N-BE(2)C cells indicate that this model system can detect a range of ligand potencies, which compare well with other established transporter assays. Our data suggest that SK-N-BE(2)C cells have potential utility to serve as another model system to detect norepinephrine reuptake inhibition activity.