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Pertussis toxin modifies the effect of central morphine on rat intestinal motility

D Parolaro1, G Patrini, P Massi

  • 1Institute of Pharmacology, Faculty of Sciences, University of Milan, Italy.

Insights

Central morphine

Area of Science:

  • Neuropharmacology
  • Gastroenterology
  • Molecular Biology

Background:

  • Opioid receptors are known to influence gastrointestinal motility.
  • The role of G-protein signaling in central opioid effects on the gut is not fully understood.

Purpose of the Study:

  • To investigate if the G-protein-mediated mechanism is involved in the antipropulsive effect of intracerebroventricularly administered morphine.
  • To elucidate the involvement of pertussis toxin-sensitive G-proteins in morphine's action on intestinal motility.

Main Methods:

  • Intracerebroventricular (i.c.v.) administration of pertussis toxin (PTX) in rats.
  • Assessment of intestinal transit using a charcoal meal test.
  • Monitoring of intestinal myoelectrical activity, specifically the myoelectric migrating complex (MMC).
  • Evaluation of PTX-catalyzed ADP ribosylation of specific substrates in rat brain membranes.

Main Results:

  • PTX pretreatment significantly antagonized morphine's antitransit effect and its abolition of MMC.
  • These effects were observed between 3 and 12 days post-PTX, with partial recovery after 25 days.
  • PTX reduced ADP ribosylation of a 39-41 kDa substrate, indicating G-protein involvement, which diminished by day 25.

Conclusions:

  • The antipropulsive effect of central morphine is initiated at receptor sites coupled to G-protein substrates sensitive to pertussis toxin.
  • G-protein-mediated signaling pathways are crucial for morphine's inhibitory action on intestinal motility.

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