The gastric effects of UFP-112, a new nociceptin/orphanin receptor agonist, in physiological and pathological conditions.

摘要: Nociceptin/orphanin FQ (N/OFQ), the endogenous NOP receptor ligand, centrally modulates gastric motor and secretory functions prevents ethanol-induced lesions in rats. A recently synthesized N/OFQ analog, [(pF)Phe(4)Aib(7)Arg(14)Lys(15)]N/OFQ-NH(2) (UFP-112), acts as a highly potent selective peptide agonist for receptors produces longer-lasting vitro vivo effects mice than natural ligand N/OFQ. In this study, we evaluated of (intracerebroventricularly/icv) peripherally (intraperitoneally/ip) injected UFP-112 on emptying acid secretion, development mucosal induced by 50% ethanol rat. When icv, it dose-dependently delayed phenol red meal (by up to 70%), decreased secretion water-loaded rats after 90 pylorus ligature, reduced 87%). all three assays, was more effective The antagonist, UFP-101, efficacy UFP-112, thus confirming that central mediate inhibitory control these functional pathological conditions Ip non-dose-related hypersecretory antiulcer effects, which UFP-101 partially abolished. appeared equiactive but about 30-100 times less ip stimulating preventing lesion formation. injected, both left unchanged, suggesting peripheral have role mediating are not involved regulating motility. addition, novel lasted longer those conclusion, is promising new pharmacological tool studying roles system.