HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

The beta3-adrenoceptor agonist SR58611A ameliorates experimental colitis in rats.

Abstract
Beta(3)-adrenoceptor agonists protect against experimental gastric ulcers. We investigated the effects of the beta(3)-adrenoceptor agonist SR58611A on 2,4-dinitrobenzene sulphonic acid-induced colitis in rats and analysed the expression of beta(3)-adrenoceptors in the colonic wall. SR58611A was administered orally (1-10 mg kg(-1)) for 7 days, starting the day before induction of colitis. Colitis was assessed by macroscopic and histological scores, tissue myeloperoxidase activity, interleukin-1beta (IL-1beta), interleukin-6 (IL-6) and tumour necrosis factor-alpha (TNF-alpha) levels. Reverse transcription-polymerase chain reaction and immunohistochemical analysis were used to examine the expression of beta(3)-adrenoceptors. SR58611A significantly reduced the severity of colitis as well as the tissue levels of TNF-alpha, IL-1beta and IL-6. Colitis was associated with a decreased expression of beta(3)-adrenoceptor mRNA in the mucosal/submucosal layer of distal colon and this reduction was not affected by SR58611A. Immunohistochemical analysis revealed beta(3)-adrenoceptors within the muscularis externa, in myenteric neurons and nerve fibres and in the submucosa. beta(3)-Adrenoceptor immunoreactivity was decreased in inflamed tissues compared to controls, particularly in the myenteric plexus; this reduction was counteracted by SR58611A. Amelioration of experimental colitis by the selective beta(3)-adrenoceptor agonist SR58611A suggests that beta(3)-adrenoceptors may represent a therapeutic target in gut inflammation.
AuthorsV Vasina, E Abu-Gharbieh, G Barbara, R de Giorgio, R Colucci, C Blandizzi, N Bernardini, T Croci, M Del Tacca, F de Ponti
JournalNeurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society (Neurogastroenterol Motil) Vol. 20 Issue 9 Pg. 1030-41 (Sep 2008) ISSN: 1365-2982 [Electronic] England
PMID18492028 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Adrenergic beta-3 Receptor Agonists
  • Adrenergic beta-Agonists
  • Cytokines
  • Receptors, Adrenergic, beta-3
  • Tetrahydronaphthalenes
  • 2,4-dinitrofluorobenzene sulfonic acid
  • Dinitrofluorobenzene
  • Proto-Oncogene Proteins c-kit
  • amibegron
Topics
  • Adrenergic beta-3 Receptor Agonists
  • Adrenergic beta-Agonists (therapeutic use)
  • Animals
  • Body Weight
  • Colitis (chemically induced, drug therapy, pathology)
  • Colon (cytology, metabolism, pathology)
  • Cytokines (immunology)
  • Dinitrofluorobenzene (analogs & derivatives, pharmacology)
  • Dose-Response Relationship, Drug
  • Humans
  • Inflammation (chemically induced, metabolism, pathology)
  • Male
  • Proto-Oncogene Proteins c-kit (metabolism)
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Adrenergic, beta-3 (genetics, metabolism)
  • Tetrahydronaphthalenes (therapeutic use)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: