Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Rivière, P.J. et al.

Fedotozine reverses ileus induced by surgery or peritonitis: action at peripheral kappa-opioid receptors.

BACKGROUND: Fedotozine is a peripheral opioid agonist. Its effects were assessed in experimental ileus in rats. METHODS: Ileus was induced by abdominal surgery (laparotomy and cecum palpation) or peritonitis (acetic acid, intraperitoneally). Digestive motility was recorded by electromyography and gastrointestinal transit estimated using a 51Cr-labeled test meal. RESULTS: Surgery or peritonitis inhibited motility and migrating myoelectrical complexes for 2-3 hours. In both models, fedotozine (3 mg/kg, intravenously; 10 mg/kg, subcutaneously) restored a normal motility pattern. This action was reproduced by the kappa-agonist, U-50, and 488H and was blocked by subcutaneous naloxone, naloxone-methiodide, or nor-binaltorphimine, a selective kappa-antagonist. Peritonitis induced a 57% inhibition of gastric emptying and intestinal transit that was reversed by fedotozine (1-10 mg/kg, subcutaneously) or kappa-agonists (U-50, 488H, bremazocine) but not delta-agonists (DPDPE, [D-Ala2]-deltorphin-II), whereas mu-agonists (morphine, fentanyl) potentiated ileus. Fedotozine restoration of transit was blocked by subcutaneous naloxone, naloxone-methiodide, or norbinaltorphimine but not by intracerebroventricular naloxone. Fedotozine was inactive up to 300 micrograms/rat when given intracerebroventrically or intrathecally. CONCLUSION: Fedotozine reverses experimental ileus via an action at peripheral kappa-opioid receptors.[1]

References

Fedotozine reverses ileus induced by surgery or peritonitis: action at peripheral kappa-opioid receptors. Rivière, P.J., Pascaud, X., Chevalier, E., Le Gallou, B., Junien, J.L. Gastroenterology (1993) [Pubmed]

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