Anticholinergic activity of imipramine and some analogs at muscarinic receptors of cultured mouse neuroblastoma cells

Ronald C. Petersen, Elliott Richelson

Research output: Contribution to journalArticle

16 Scopus citations

Abstract

Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic guanosine monophosphate (GMP) formation by cultured mouse neuroblastoma cells. Equilibrium dissociation constants for these compounds yielded the following rank order of potency at the muscarinic receptor: imipramine > trimipramine > 3-chlorimipramine > desipramine > 3-chloro-2-hydroxyimipramine > 2-hydroxyimipramine > didesmethylimipramine. These results indicate that didesmethylation of the side chain nitrogen or hydroxylation of the ring at the 2-position lead to marked reductions (30-fold and 12-fold, respectively) in antimuscarinic activity of imipramine.

Original languageEnglish (US)
Pages (from-to)26-28
Number of pages3
JournalPsychopharmacology
Volume76
Issue number1
DOIs
StatePublished - Jan 1 1982

Keywords

  • Antimuscarinic activity
  • Tricyclic antidepressants

ASJC Scopus subject areas

  • Pharmacology

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