Novel potent agonist [(pF)Phe4,Aib7,Aib11,Arg14,Lys15]N/OFQ-NH2 and antagonist [Nphe1,(pF)Phe4,Aib7,Aib11,Arg14,Lys15]N/OFQ-NH2 of nociceptin/orphanin FQ receptor

Regulatory Peptides
Ya-Li PengRui Wang

Abstract

Two novel ligands for the nociceptin/orphanin FQ (N/OFQ) receptor (NOP), [(pF)Phe4,Aib7, Aib11,Arg14,Lys15]N/OFQ-NH2 (peptide-1) and [Nphe1,(pF)Phe4,Aib7,Aib11,Arg14,Lys15]N/OFQ-NH2 (peptide-2), have been generated by combining different modifications of N/OFQ sequence. In the present study, we investigated the actions of two analogues and compared them with those of N/OFQ in four assays. Peptide-1 mimicked N/OFQ effects in mouse vas deferens and mouse colon and showed similar maximal effects but higher potency relative to N/OFQ. The effects of peptide-1 were sensitive to NOP receptor selective antagonist ([Nphe1]N/OFQ(1-13)-NH2) but not to naloxone in vitro. Peptide-1 (25 pmol, i.c.v.) mimicked the pronociceptive action of N/OFQ (2.5 nmol, i.c.v.) in mouse tail withdrawal assay, displaying higher potency and longer lasting effects. In anesthetized rats, peptide-1 (1 nmol/kg, i.v.) produced a marked decrease in mean arterial pressure, which was comparable to that evoked by i.v. N/OFQ (100 nmol/kg). Peptide-2 did not produce any effect per se but antagonized N/OFQ actions in mouse vas deferens and mouse colon assays. Peptide-2 is active in vivo where it prevented the pronociceptive effect induced by 2.5 nmol N/OFQ i.c.v. in the ...Continue Reading

References

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Citations

Jun 29, 2007·Naunyn-Schmiedeberg's Archives of Pharmacology·M KitayamaD G Lambert
Jan 19, 2010·Pharmacological Reports : PR·Margarita KirkovaSimeon Todorov
Oct 24, 2007·Peptides·Richard J Bodnar
May 26, 2010·CNS Neuroscience & Therapeutics·Girolamo Calo'Remo Guerrini
Feb 3, 2011·Cell Biochemistry and Function·Elina TzvetanovaMargarita Kirkova
Jan 26, 2010·Medicinal Research Reviews·Carlo Mustazza, Giuditta Bastanzio
Feb 26, 2010·Expert Opinion on Therapeutic Patents·Tally M Largent-Milnes, Todd W Vanderah
Dec 23, 2020·Chemistry & Biodiversity·Karol Wtorek, Anna Janecka

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