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 language | English (US) |
|---|---|
| Pages (from-to) | 26-28 |
| Number of pages | 3 |
| Journal | Psychopharmacology |
| Volume | 76 |
| Issue number | 1 |
| DOIs | |
| State | Published - Jan 1982 |
Keywords
- Antimuscarinic activity
- Tricyclic antidepressants
ASJC Scopus subject areas
- Pharmacology