Cannabinoid 1 receptors modulate intestinal sensory and motor function in rat

Neurogastroenterol Motil. 2010 Jun;22(6):672-e205. doi: 10.1111/j.1365-2982.2010.01473.x. Epub 2010 Feb 18.

Abstract

Background: Cannabinoid receptors are involved in visceral pain perception and control of intestinal motility in vivo. The underlying mechanisms are not well characterized. We aimed to determine whether the cannabinoid-1 (CB(1)) receptor modulates intestinal afferent nerve discharge and the peristaltic reflex.

Methods: Rats were anesthetized and intestinal segments were removed. Afferent nerve discharge from a mesenteric nerve was investigated in vitro in the presence of the CB(1) antagonist SR 141716A or the CB(1) agonist WIN 55212-2. The myenteric peristaltic reflex was induced by electrical field stimulation and influence of SR 141716A or WIN 55212-2 was recorded.

Key results: Afferent nerve discharge to the algesic mediator bradykinin was reduced to 11 +/- 5.1 imp s(-1) following pretreatment with SR 141716A and unchanged after WIN 55212-2 compared to 63 +/- 15.4 imp s(-1) in controls. At maximum distension pressure (80 cmH(2)O) during ramp distension, 92 +/- 12.4 imp s(-1) were reached following SR 141716A compared to 260 +/- 13.2 in vehicle controls and 227 +/- 15.4 in WIN 55212-2 pretreated animals. In contrast, afferent discharge to 5-HT (500 micromol L(-1)) was increased to 75 +/- 24.6 imp s(-1) following WIN 55212-2 compared to 18 +/- 5.9 imp s(-1) in controls, whereas SR 141716A had no effect. Ascending neuronal contractions were dose-dependently attenuated in the presence of SR 141716A and latency of these contractions was reduced. WIN 55212-2 had opposite effects that were abolished by SR 141716A.

Conclusions & inferences: Activation of the CB(1) receptor differentially alters afferent intestinal nerve sensitivity to bradykinin, 5-HT, and noxious mechanical distension, while it strengthens ascending neuronal contractions. Further studies are needed to determine the physiological relevance of these observations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzoxazines / pharmacology
  • Bradykinin / pharmacology
  • Dose-Response Relationship, Drug
  • Electrophysiology
  • Enteric Nervous System / drug effects
  • Enteric Nervous System / physiology
  • Gastrointestinal Motility / drug effects
  • Gastrointestinal Motility / physiology
  • Intestines / drug effects
  • Intestines / innervation*
  • Intestines / physiology*
  • Male
  • Morpholines / pharmacology
  • Motor Neurons / drug effects
  • Motor Neurons / physiology*
  • Muscle Contraction / physiology
  • Myenteric Plexus / drug effects
  • Naphthalenes / pharmacology
  • Piperidines / pharmacology
  • Pyrazoles / pharmacology
  • Rats
  • Rats, Wistar
  • Receptor, Cannabinoid, CB1 / agonists
  • Receptor, Cannabinoid, CB1 / antagonists & inhibitors
  • Receptor, Cannabinoid, CB1 / physiology*
  • Rimonabant
  • Sensory Receptor Cells / drug effects
  • Sensory Receptor Cells / physiology*
  • Serotonin / pharmacology

Substances

  • Benzoxazines
  • Morpholines
  • Naphthalenes
  • Piperidines
  • Pyrazoles
  • Receptor, Cannabinoid, CB1
  • Serotonin
  • (3R)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone
  • Rimonabant
  • Bradykinin