Wagstaff Ryan, Hedrick Michael, Fan Jun, Crowe Paul D, DiSepio Daniel
Department of Pharmacology & Lead Discovery, Neurocrine Bisciences, Inc., San Diego, California 92130, USA.
J Biomol Screen. 2007 Apr;12(3):436-41. doi: 10.1177/1087057106297994.
Monoamine transporters regulate the concentration of neurotransmitters in the synapse following neurotransmission and are very important drug targets in the pharmaceutical industry. Because of the labor-intensive nature of functional uptake assays using radioactive substrates, high-throughput screening for monoamine transporter inhibitors has been limited to radioligand binding assays. In this article, the authors describe the development of a 384-well, high-throughput functional screening assay for norepinephrine transporter inhibitors using the FLIPR(Tetra) and a recently identified fluorescent substrate, 4-(4-dimethylaminostyryl)- N-methyl-pyridinium (ASP(+)).
