High‐Affinity Binding of [3H]Desipramine to Rat Brain: A Presynaptic Marker for Noradrenergic Uptake Sites

M. Rehavi, P. Skolnick, M. J. Brownstein, S. M. Paul*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


Abstract: High‐affinity binding sites (apparent KD= 1.5 nM) for [3H]desipramine have been demonstrated and characterized in membranes prepared from rat brain. The binding of [3H]desipramine was found to be saturable, reversible, heat‐sensitive, sodium‐dependent, and regionally distributed among various regions of the brain. High concentrations of [3H]desipramine binding sites were found in the septum, cerebral cortex, and hypothalamus, whereas lower concentrations were found in the medulla, cerebellum, and corpus striatum. A very good correlation (r= 0.81, P < 0.001) was observed between the potencies of a series of drugs in inhibiting high‐affinity [3H]desipramine binding and their capacity to block norepinephrine uptake into synaptosomes. In 6‐hydroxydopamine‐lesioned rats there was a marked decrease in [3H]norepinephrine uptake and [3H]desipramine binding with no significant alterations in either [3H]serotonin uptake or [3H]imipramine binding. These results suggest that the high‐affinity binding of [3HJdesipramine to rat brain membranes is pharmacologically and biochemically distinct from the high‐affinity binding of [3H]imipramine, and that there is a close relationship between the high‐affinity binding site for [3H]desipramine and the uptake site for norepinephrine.

Original languageEnglish
Pages (from-to)889-895
Number of pages7
JournalJournal of Neurochemistry
Issue number4
StatePublished - Apr 1982
Externally publishedYes


  • Norepinephrine uptake
  • Serotonin uptake
  • Tricyclic antidepressants
  • [H]Desipramine binding
  • [H]imipramine binding


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