Effect of vanilloid drugs on gastrointestinal transit in mice

Br J Pharmacol. 2001 Apr;132(7):1411-6. doi: 10.1038/sj.bjp.0703975.

Abstract

1. We have studied the effect of capsaicin, piperine and anandamide, drugs which activate vanilloid receptors and capsazepine, a vanilloid receptor antagonist, on upper gastrointestinal motility in mice. 2. Piperine (0.5 - 20 mg kg(-1) i.p.) and anandamide (0.5 - 20 mg kg(-1) i.p.), dose-dependently delayed gastrointestinal motility, while capsaicin (up to 3 mg kg(-1) i.p.) was without effect. Capsazepine (15 mg kg(-1) i.p.) neither per se affected gastrointestinal motility nor did it counteract the inhibitory effect of both piperine (10 mg kg(-1)) and anandamide (10 mg kg(-1)). 3. A per se non effective dose of SR141716A (0.3 mg kg(-1) i.p.), a cannabinoid CB(1) receptor antagonist, counteracted the inhibitory effect of anandamide (10 mg kg(-1)) but not of piperine (10 mg kg(-1)). By contrast, the inhibitory effect of piperine (10 mg kg(-1)) but not of anandamide (10 mg kg(-1)) was strongly attenuated in capsaicin (75 mg kg(-1) in total, s.c.)-treated mice. 4. Pretreatment of mice with N(G)-nitro-L-arginine methyl ester (25 mg kg(-1) i.p.), yohimbine (1 mg kg(-1), i.p.), naloxone (2 mg kg(-1) i.p.), or hexamethonium (1 mg kg(-1) i.p.) did not modify the inhibitory effect of both piperine (10 mg kg(-1)) and anandamide (10 mg kg(-1)). 5. The present study indicates that the vanilloid ligands anandamide and piperine, but not capsaicin, can reduce upper gastrointestinal motility. The effect of piperine involves capsaicin-sensitive neurones, but not vanilloid receptors, while the effect of anandamide involves cannabinoid CB(1), but not vanilloid receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids*
  • Animals
  • Arachidonic Acids / pharmacology*
  • Benzodioxoles
  • Capsaicin / pharmacology*
  • Dose-Response Relationship, Drug
  • Endocannabinoids
  • Gastrointestinal Transit / drug effects*
  • Hexamethonium / pharmacology
  • Male
  • Mice
  • Mice, Inbred ICR
  • NG-Nitroarginine Methyl Ester / pharmacology
  • Naloxone / pharmacology
  • Piperidines / pharmacology*
  • Polyunsaturated Alkamides
  • Pyrazoles / pharmacology
  • Receptors, Drug / antagonists & inhibitors
  • Rimonabant
  • Yohimbine / pharmacology

Substances

  • Alkaloids
  • Arachidonic Acids
  • Benzodioxoles
  • Endocannabinoids
  • Piperidines
  • Polyunsaturated Alkamides
  • Pyrazoles
  • Receptors, Drug
  • Yohimbine
  • Naloxone
  • Hexamethonium
  • Rimonabant
  • Capsaicin
  • piperine
  • anandamide
  • NG-Nitroarginine Methyl Ester