Pharmacology and clinical experience with fedotozine

Expert Opin Investig Drugs. 2001 Jan;10(1):97-110. doi: 10.1517/13543784.10.1.97.


Fedotozine [(1R)-1-phenyl-1-[(3,4,5-trimethoxy)benzyloxymethyl]-N,N- dimethyl-n-propylamine, (2S,3S-tartrate] is derived from the arylacetamide series. As with other compounds of this series, fedotozine is more or less selective of kappa(1)-opioid receptors and particularly for the kappa(1a)-receptor subtype, where it acts as an agonist. Pharmacological studies have shown that fedotozine exerts a peripheral antinociceptive action, comparable with that of other kappa-agonists. Its main effects have been demonstrated at the level of the afferent nerve pathways originating from the gut. Fedotozine alters the processing of visceral sensations along these pathways and hence, the perception of gut stimuli at the brain level. It modifies reflexes induced in various pathological conditions, like experimental inflammation of the gut, chemically-induced peritonitis or post-operative ileus. Fedotozine also decreases the nociceptive reflexes triggered by noxious gut distension in animals. In humans, fedotozine decreases the perception of gut distension, both in physiological and pathological conditions. Clinical trials undertaken in patients with functional digestive disorders, non-ulcer dyspepsia and irritable bowel syndrome, have shown that fedotozine relieves abdominal pain in these patients in 6-week treatments. kappa-Opioid receptors remain an interesting area for future development of new treatments for abdominal pain in patients with functional digestive disorders.

Publication types

  • Review

MeSH terms

  • Animals
  • Benzyl Compounds / pharmacokinetics
  • Benzyl Compounds / pharmacology*
  • Benzyl Compounds / therapeutic use
  • Colonic Diseases, Functional / drug therapy
  • Dyspepsia / drug therapy
  • Gastrointestinal Motility / drug effects
  • Humans
  • Pain / physiopathology
  • Propylamines / pharmacokinetics
  • Propylamines / pharmacology*
  • Propylamines / therapeutic use
  • Receptors, Opioid, kappa / agonists*
  • Receptors, Opioid, kappa / drug effects
  • Receptors, Opioid, kappa / physiology


  • Benzyl Compounds
  • Propylamines
  • Receptors, Opioid, kappa
  • fedotozine