Corpus ID: 12530156

A new inhibitor of norepinephrine uptake devoid of affinity for receptors in rat brain.

@article{Wong1982ANI,
  title={A new inhibitor of norepinephrine uptake devoid of affinity for receptors in rat brain.},
  author={D. Wong and P. Threlkeld and K. L. Best and F. Bymaster},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1982},
  volume={222 1},
  pages={
          61-5
        }
}
LY135252, (+/-)-N-methyl-gamma-(2-methylphenoxy) phenylpropylamine hydrochloride, is a competitive inhibitor of norepinephrine uptake in synaptosomes of rat hypothalamus. The resolved optical (-)-isomer, LY139603, is 2 and 9 times more effective than the racemate and the (+)-isomer, LY139602, with inhibitor constants (Ki) of 1.9, 3.4 and 16.8 nM, respectively. All three compounds are relatively weak in the inhibition of dopamine and serotonin uptake, with Ki values at least two orders of… Expand
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