UFP-112 a potent and long lasting agonist selective for the nociceptin/orphanin FQ receptor

作者: Girolamo Calo' , Anna Rizzi , Carlo Cifani , Maria Vittoria Micioni Di Bonaventura , Domenico Regoli

DOI: 10.1111/J.1755-5949.2009.00107.X

关键词: In vitroPeptide sequenceNociceptin receptorAgonistChemistryPeptideIn vivoReceptorPharmacologyNOP

摘要: Nociceptin/orphanin FQ (N/OFQ) controls several biological functions via selective activation of the N/OFQ peptide receptor (NOP). [(pF)Phe4Aib7Arg14Lys15]N/OFQ-NH2 (UFP-112) is an NOP ligand designed using a combination chemical modifications in same sequence that increase affinity/potency and/or reduce susceptibility to enzymatic degradation. In present review article, we summarize data from literature and original findings on vitro vivo pharmacological features UFP-112. Moreover, important actions possible therapeutic indications agonists are discussed based results obtained with UFP-112 compared other nonpeptide ligands.

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