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Comparison of the effects of T-1815, yohimbine and naloxone on mouse colonic propulsion.

Abstract
The colonic prokinetic activity of a newly synthesized compound, T-1815, administered orally, was compared with that of yohimbine and naloxone in mice. The time required to evacuate a glass bead inserted into the distal colon was taken as an index of prokinetic activity. Clonidine (3-30 micrograms/kg s.c.), and loperamide (0.3-3.0 mg/kg s.c.) delayed bead expulsion in a dose-dependent manner. Yohimbine (0.3-10 mg/kg) and T-1815 (0.1-10 mg/kg) showed a dose-dependent reduction of the delay in evacuation induced by clonidine, but naloxone had no effect. The loperamide-induced retardation of colonic propulsion was reduced by naloxone (0.3-10 mg/kg) and T-1815 (0.1-10 mg/kg) in a dose-dependent manner, but yohimbine had no effect. In normal animals, yohimbine and naloxone had no significant effect on evacuation, while a slight acceleration was observed with T-1815 at 10 mg/kg. No soft feces and/or diarrhea were observed with any of the three test drugs. These results indicate that T-1815 appears to be a unique colonic prokinetic compound, the action of which may be mediated through mechanisms other than antagonism for alpha 2-adrenoceptors or opioid receptors.
AuthorsK Yamada, Y Onoda
JournalJournal of smooth muscle research = Nihon Heikatsukin Gakkai kikanshi (J Smooth Muscle Res) Vol. 29 Issue 2 Pg. 47-53 (Apr 1993) ISSN: 0916-8737 [Print] Japan
PMID8318729 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Propylamines
  • Thiophenes
  • T 1815
  • Yohimbine
  • Naloxone
  • Loperamide
  • Clonidine
Topics
  • Administration, Oral
  • Animals
  • Clonidine (antagonists & inhibitors)
  • Colon (drug effects)
  • Dose-Response Relationship, Drug
  • Gastrointestinal Motility (drug effects)
  • Loperamide (antagonists & inhibitors)
  • Male
  • Mice
  • Naloxone (administration & dosage, pharmacology)
  • Propylamines (administration & dosage, pharmacology)
  • Thiophenes (administration & dosage, pharmacology)
  • Yohimbine (administration & dosage, pharmacology)

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