Inhibition of transport function and desipramine binding at the human noradrenaline transporter by N-ethylmaleimide and protection by substrate analogs

  title={Inhibition of transport function and desipramine binding at the human noradrenaline transporter by N-ethylmaleimide and protection by substrate analogs},
  author={Kevin F. Foley and Nicholas V Cozzi},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  • K. Foley, N. Cozzi
  • Published 18 April 2002
  • Biology, Chemistry, Computer Science
  • Naunyn-Schmiedeberg's Archives of Pharmacology
Abstract.N-ethylmaleimide (NEM) inhibits [3H]desipramine binding and [3H]noradrenaline uptake at the rat noradrenaline transporter (rNET) by covalently modifying cysteine residues. We report here that NEM also inhibits [3H]desipramine binding and [3H]noradrenaline uptake at the cloned human noradrenaline transporter (hNET) stably expressed in C6 glial cells. The IC50 for NEM inhibition of [3H]noradrenaline uptake was 43.6±5.5 µM. We tested several compounds for their abilities to inhibit [3H… 
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Inhibition of neuronal noradrenaline uptake (uptake1) and desipramine binding by N-ethylmaleimide (NEM)
The inhibition by N-ethylmaleimide of uptake1 and desipramine binding was studied on clonal rat phaeochromocytoma cells and results are compatible with the hypothesis of a common binding site for substrates and inhibitors of the neuronal noradrenaline carrier.
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