Anti-inflammatory and antinociceptive action of an orally available nociceptin receptor agonist SCH 221510 in a mouse model of inflammatory bowel diseases

The Journal of Pharmacology and Experimental Therapeutics
Marta SobczakJakub Fichna

Abstract

The nociceptin receptors (NOPs) are expressed in the gastrointestinal (GI) tract on muscle cell membranes and neurons, as well as the immune cells that infiltrate the mucosa. The involvement of NOPs in the pathophysiology of GI inflammation has been suggested, but due to the lack of selective NOP agonists, it never fully elucidated. Our aim was to characterize the anti-inflammatory and antinociceptive effect of the NOP agonist, SCH 221510 [3-endo-8-[bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo [3.2.1]octan-3-ol], as a potential therapeutic strategy in the treatment of inflammatory bowel diseases (IBD). The anti-inflammatory action of SCH 221510 was determined after intraperitoneal, oral, and intracolonic administration of SCH 221510 (0.1-3.0 mg/kg once or twice daily) in mice treated with 2,4,6-trinitrobenzenesulfonic acid (TNBS). Antinociceptive action of SCH 221510 was evaluated in the mouse model of mustard oil (MO)-induced abdominal pain. Relative NOP mRNA expression was assessed in patients with IBD using real-time reverse transcriptase-polymerase chain reaction. We found that the expression of NOP mRNA was significantly decreased in patients with IBD. The administration (0.1 and 1.0 mg/kg i.p. twice daily and 3 mg/kg ...Continue Reading

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Citations

Feb 24, 2016·Naunyn-Schmiedeberg's Archives of Pharmacology·Marta ZielińskaJakub Fichna
Oct 2, 2015·Current Opinion in Pharmacology·Peter HolzerAitak Farzi
Oct 14, 2014·Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society·S Agostini, C Petrella
Jul 22, 2014·Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society·J FichnaM Storr
Sep 26, 2015·European Journal of Pharmacology·Marta ZielińskaJakub Fichna
Aug 4, 2018·Journal of Molecular Neuroscience : MN·Qiang Wu, Li Liu
Sep 4, 2015·Pediatric Pulmonology·David P Nichols, James F Chmiel
Dec 20, 2018·International Journal of Colorectal Disease·Anna ZielińskaJakub Fichna
Sep 19, 2021·Pharmacological Reports : PR·Hubert ZatorskiJakub Fichna

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