Corticotropin-releasing hormone receptor 1 antagonist blocks brain-gut activation induced by colonic distention in rats

Gastroenterology. 2005 Nov;129(5):1533-43. doi: 10.1053/j.gastro.2005.07.053.

Abstract

Background & aims: The corticotropin-releasing hormone receptor 1 mediates stress-induced changes in colonic motor activity and emotion. We tested the hypothesis that pretreatment with JTC-017, a specific corticotropin-releasing hormone receptor 1 antagonist, blocks colorectal distention-induced hippocampal noradrenaline release and visceral perception in rats. We also investigated whether pretreatment with JTC-017 blocks acute or chronic colorectal distention-induced adrenocorticotropic hormone release, anxiety, and stress-induced changes in colonic motility.

Methods: Rats were pretreated intrahippocampally with alpha-helical corticotropin-releasing hormone (1.25 microg/kg; vehicle), a nonspecific corticotropin-releasing hormone receptor antagonist, or intraperitoneally with JTC-017 (10 mg/kg). Hippocampal noradrenaline release after microdialysis and the frequency of abdominal contractions were measured in response to acute colorectal distention. Plasma adrenocorticotropic hormone levels, anxiety-related behavior, and stress-induced changes in colonic motility were evaluated after acute or chronic colorectal distention followed by exposure to an elevated plus maze.

Results: Administration of alpha-helical corticotropin-releasing hormone or JTC-017 significantly attenuated hippocampal noradrenaline release and reduced the frequency of abdominal contractions induced by acute distention. In addition, JTC-017 significantly reduced plasma adrenocorticotropic hormone and anxiety after acute distention. After chronic distention, changes in plasma adrenocorticotropic hormone and anxiety were not significant because of habituation. In contrast, a significant increase in fecal pellet output during the elevated plus maze was observed after chronic distention. This increase in fecal pellet output was blocked by pretreatment with JTC-017.

Conclusions: Our results suggest that JTC-017, a specific corticotropin-releasing hormone receptor 1 antagonist, attenuates hippocampal noradrenaline release, visceral perception, adrenocorticotropic hormone release, and anxiety after acute colorectal distention in rats. In addition, JTC-017 blocks stress-induced changes in colonic motility after chronic colorectal distention in rats.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Abdominal Muscles / physiology
  • Acute Disease
  • Adrenocorticotropic Hormone / metabolism
  • Animals
  • Anxiety / physiopathology
  • Behavior, Animal
  • Benzamides / chemistry
  • Benzamides / metabolism
  • Benzamides / pharmacology*
  • Binding, Competitive
  • Catheterization
  • Chronic Disease
  • Colon / innervation
  • Colon / physiology*
  • Corticotropin-Releasing Hormone / metabolism
  • Corticotropin-Releasing Hormone / pharmacology
  • Gastrointestinal Motility / drug effects*
  • Gastrointestinal Motility / physiology
  • Hippocampus / metabolism*
  • Hormone Antagonists / metabolism
  • Hormone Antagonists / pharmacology
  • Male
  • Muscle Contraction / drug effects
  • Muscle Contraction / physiology
  • Norepinephrine / metabolism
  • Rats
  • Rats, Wistar
  • Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
  • Receptors, Corticotropin-Releasing Hormone / metabolism
  • Stress, Physiological / physiopathology

Substances

  • Benzamides
  • Hormone Antagonists
  • JTC-017
  • Receptors, Corticotropin-Releasing Hormone
  • alpha helical corticotropin-releasing hormone
  • CRF receptor type 1
  • Adrenocorticotropic Hormone
  • Corticotropin-Releasing Hormone
  • Norepinephrine