title: Effect of thienorphine on intestinal transit and isolated guinea-pig ileum contraction.
abstract: OBJECTIVE
  To evaluate the effect of thienorphine on small intestinal transit in vivo and on guinea-pig ileum (GPI) contraction in vitro.
  
  
  METHODS
  The effects of thienorphine on intestinal transit were examined in mice and in isolated GPI. Buprenorphine and morphine served as controls. The distance traveled by the head of the charchol and the total length of the intestine were measured in vivo. Gastrointestinal transit was expressed as a percentage of the distance traveled by the head of the marker relative to the total length of the small intestine. The isolated GPI preparations were connected to an isotonic force transducer and equilibrated for at least 1 h before exposure to drugs. Acetylcholine was used for muscle stimulation.
  
  
  RESULTS
  Thienorphine (0.005-1.0 mg/kg, ig) or buprenorphine (0.005-1.0 mg/kg, sc) dose-dependently significantly inhibited gut transit compared with saline. Thienorphine inhibited gut transit less than buprenorphine. The maximum inhibition by thienorphine on the intestinal transit was 50%-60%, whereas the maximum inhibition by morphine on gut transit was about 100%. Thienorphine also exhibited less inhibition on acetylcholine-induced contraction of GPI, with a maximum inhibition of 65%, compared with 93% inhibition by buprenorphine and 100% inhibition by morphine. Thienorphine induced a concentration-dependent decrease in the basal tonus of spontaneous movement of the GPI, the effect of which was weaker than that with buprenorphine. The duration of the effect of thienorphine on the GPI was longer than that with buprenorphine.
  
  
  CONCLUSIONS
  Thienorphine had less influence, but a longer duration of action on GPI contraction and moderately inhibited intestinal transit.
authors.affiliation: Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China.
authors.forename: Pei-Lan
authors.initials: PL
authors.lastname: Zhou
authors.forename: Yu-Lei
authors.initials: YL
authors.lastname: Li
authors.forename: Ling-Di
authors.initials: LD
authors.lastname: Yan
authors.forename: Zheng
authors.initials: Z
authors.lastname: Yong
authors.forename: Gang
authors.initials: G
authors.lastname: Yu
authors.forename: Hua-Jin
authors.initials: HJ
authors.lastname: Dong
authors.forename: Hui
authors.initials: H
authors.lastname: Yan
authors.forename: Rui-Bin
authors.initials: RB
authors.lastname: Su
authors.forename: Ze-Hui
authors.initials: ZH
authors.lastname: Gong
mesh_terms: D000701:Analgesics, Opioid / Q000494:pharmacology*; D000818:Animals; D002047:Buprenorphine / Q000031:analogs & derivatives* / Q000494:pharmacology; D018679:Cholinergic Agonists / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005772:Gastrointestinal Transit / Q000187:drug effects*; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects*; D008297:Male; D051379:Mice; D009020:Morphine / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects*; D009292:Narcotic Antagonists / Q000494:pharmacology; D013997:Time Factors
chemical_list: D000701:Analgesics, Opioid; D018679:Cholinergic Agonists; D009292:Narcotic Antagonists; C512397:thienorphine; D002047:Buprenorphine; D009020:Morphine
keywords: Buprenorphine; Contraction; Guinea-pig ileum; Gut transit; Thienorphine
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