title: High-throughput screening for norepinephrine transporter inhibitors using the FLIPRTetra.
abstract: 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(+)).
authors: Department of Pharmacology & Lead Discovery, Neurocrine Bisciences, Inc., San Diego, California 92130, USA.
authors: Ryan
authors: R
authors: Wagstaff
authors: Michael
authors: M
authors: Hedrick
authors: Jun
authors: J
authors: Fan
authors: Paul D
authors: PD
authors: Crowe
authors: Daniel
authors: D
authors: DiSepio
mesh_terms: D018759:Adrenergic Uptake Inhibitors / Q000032:analysis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D050484:Norepinephrine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011726:Pyridinium Compounds
chemical_list: C032315:4-(4-dimethylaminostyryl)-1-methylpyridinium; D018759:Adrenergic Uptake Inhibitors; D050484:Norepinephrine Plasma Membrane Transport Proteins; D011726:Pyridinium Compounds