Antimuscarinic properties of antidepressants: Dibenzepin (Noveril®)

Moshe Rehavi*, Saul Maayani, Leon Goldstein, Marcel Assael, Mordechai Sokolovsky

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

The antimuscarinic potency of dibenzepin (Noveril®) was estimated by measuring (a) central in vivo effects in mice (antihypothermia and antitremor, both induced by oxotremorine), (b) peripheral in vivo activity (mydriasis caused by systemic administration of the drug), (c) the effects of dibenzepin on isolated smooth muscle from guinea pig ileum, and (d) in vitro determination of the affinity constant of dibenzepin toward the muscarinic binding sites in whole mouse-brain homogenate. The data allowed the construction of a normalized antimuscarinic potency scale for some of the common tricyclic antidepressants. With a value of 1 for scopolamine, the following relative anticholinergic potencies were calculated: dibenzepin-1/600, nortriptyline-1/300, imipramine-1/200, and amitriptyline-1/75. These values suggest an explanation for the absence of clinically detectable anticholinergic side effects during treatment of depression with high doses of dibenzepin. Structural and spatial interrelations among various tricyclic antidepressants and scopolamine are discussed.

Original languageEnglish
Pages (from-to)35-38
Number of pages4
JournalPsychopharmacology
Volume54
Issue number1
DOIs
StatePublished - Jan 1977

Keywords

  • Antidepressants
  • Antimuscarinic
  • Cholinersterases
  • Muscarinic receptor

Fingerprint

Dive into the research topics of 'Antimuscarinic properties of antidepressants: Dibenzepin (Noveril®)'. Together they form a unique fingerprint.

Cite this