Amitriptyline: Long-term treatment elevates α-adrenergic and muscarinic receptor binding in mouse brain

Moshe Rehavi, Orly Ramot, Bella Yavetz, Mordechai Sokolovsky

Research output: Contribution to journalArticlepeer-review

Abstract

The effects of long-term treatment of the tricyclic antidepressant drug, amitriptyline, on α-adrenergic, muscarinic and dopaminergic receptor binding were studied in mouse brain. No changes could be observed after 7 or 14 days of amitriptyline administration, but after 21 days a two-fold increase in α-adrenergic binding was detected in the medulla pons and in the hippocampus using [3H]WB-4101 as the binding ligand. In the same regions, a moderate increase in muscarinic receptor binding (25%) as measured by [3H]4NMPB was seen, while no change was detected in dopaminergic receptor binding measured by [3H]spiperone. Scatchard analysis reveals that the increases in receptor densities are not a result of changes in the dissociation constants of the tritiated drugs for their receptors. It is suggested that the increase in α-adrenergic as well as in muscarinic binding is a consequence of a chronic blockade of these two types of receptors by amitriptyline in vivo.

Original languageEnglish
Pages (from-to)443-453
Number of pages11
JournalBrain Research
Volume194
Issue number2
DOIs
StatePublished - 4 Aug 1980

Keywords

  • amitriptyline
  • chronic treatment
  • muscarinic
  • α-adrenoreceptor

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