Quantitative autoradiography of serotonin uptake sites in rat brain using [3H]cyanoimipramine

Brain Res. 1988 Jun 28;454(1-2):78-88. doi: 10.1016/0006-8993(88)90805-0.


The binding of [3H]cyanoimipramine to serotonin uptake sites in rat brain slices was studied using quantitative autoradiography. Binding was of high affinity and was to a single class of binding site. This is in contrast to results previously obtained by others with [3H]imipramine where two binding sites were observed. The sites labeled by [3H]cyanoimipramine had properties consistent with this ligand labeling serotonin uptake sites, as: (1) binding is displaced by drugs which are potent inhibitors of serotonin uptake but not by drugs which are weak inhibitors of uptake; (2) binding is dependent on the presence of sodium ions as is the uptake of serotonin; (3) binding is almost completely eliminated in the brains of rats lesioned by the serotonin neurotoxin 5,7-dihydroxytryptamine; (4) the distribution of binding sites throughout the rat brain is highly correlated with that found previously for [3H]indalpine, a potent serotonin uptake inhibitor, and for [3H]imipramine. The properties of binding of [3H]cyanoimipramine make it an ideal ligand for the quantitative autoradiography of serotonin uptake sites.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 1-Naphthylamine / analogs & derivatives
  • 1-Naphthylamine / metabolism
  • Animals
  • Autoradiography
  • Binding, Competitive
  • Brain / metabolism*
  • Fluoxetine / metabolism
  • Imipramine / analogs & derivatives*
  • Imipramine / metabolism
  • Kinetics
  • Male
  • Rats
  • Rats, Inbred Strains
  • Receptors, Serotonin / metabolism*
  • Sertraline
  • Zimeldine / analogs & derivatives
  • Zimeldine / metabolism


  • Receptors, Serotonin
  • Fluoxetine
  • cianopramine
  • Zimeldine
  • norzimelidine
  • 1-Naphthylamine
  • Imipramine
  • Sertraline