Novel halogenated analogs of tomoxetine that are potent and selective inhibitors of norepinephrine uptake in brain.

@article{Gehlert1995NovelHA,
  title={Novel halogenated analogs of tomoxetine that are potent and selective inhibitors of norepinephrine uptake in brain.},
  author={Donald R. Gehlert and Douglas A Schober and Susan K. Hemrick-Luecke and Joseph H. Krushinski and James Jeffry Howbert and David W. Robertson and Ray W. Fuller and David T. Wong},
  journal={Neurochemistry international},
  year={1995},
  volume={26 1},
  pages={47-52}
}
Halogenated analogs of the potent norepinephrine (NE) uptake inhibitor, tomoxetine, were synthesized and their affinities for the serotonin (5HT) and NE uptake sites evaluated. One of the most potent was the 2-iodo substituted analog (289306) that inhibited [3H]tomoxetine binding to rat cerebral cortex with a Ki of 0.37 nM. The compound also inhibited the uptake of [3H]NE into rat hypothalamic synaptosomes with a Ki of 3.5 nM. This analog was significantly less potent at the 5HT uptake site, as… CONTINUE READING

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