High affinity binding sites for [3H]imipramine in human brain and platelet: Clinical implications

S. M. Paul, M. Rehavi, P. Skolnick, F. K. Goodwin

Research output: Contribution to journalArticlepeer-review

4 Scopus citations


High affinity and saturable binding sites for [3H]imipramine have been demonstrated in membrane preparations from human brain and platelet. These binding sites appear to be specific for tricyclic antidepressants since specifically bound [3H]imipramine is displaced by pharmacologically-active tricyclic antidepressants at low concentrations. Tertiary amine antidepressants such as imipramine and amitriptyline are more potent inhibitors of [3H]imipramine binding than are the corresponding secondary amines nortriptyline and desipramine; suggesting a relationship between the high affinity binding sites and the serotonin reuptake site. In contrast other psychotropic drugs and neurotransmitter agonists and antagonists have little or no effect on specific [3H]imipramine binding. The characteristics of [3H]Imipramine binding in human brain membranes are very similar (if not identical) to that of human platelets suggesting that the latter may be a useful model in studying the pharmacological significance of these binding sites. Preliminary studies of [3H]imipramine binding in platelets from severely depressed patients reveal a significant (≥ 30%) decrease in binding site density (Bmax) when compared to platelets from healthy age-matched controls.

Original languageEnglish
Pages (from-to)187-193
Number of pages7
JournalAdvances in the Biosciences
Issue numberC
StatePublished - 1981


  • Tricyclic antidepressants
  • [H]imipramine binding
  • depression
  • human platelets human brain


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