Novel Mixed NOP/Opioid Receptor Peptide Agonists.

ABSTRACT: The nociceptin/orphanin FQ (N/OFQ)/N/OFQ receptor (NOP) system controls different biological functions including pain and cough reflex. Mixed NOP/opioid receptor agonists elicit similar effects to strong opioids but with reduced side effects. In this work, 31 peptides with the general sequence [Tyr/Dmt¹,Xaa⁵]N/OFQ(1-13)-NH₂ were synthesized and pharmacologically characterized for their action at human recombinant NOP/opioid receptors. The best results in terms of NOP versus mu opioid receptor potency were obtained by substituting both Tyr¹ and Thr⁵ at the N-terminal portion of N/OFQ(1-13)-NH₂ with the noncanonical amino acid Dmt. [Dmt^1,5]N/OFQ(1-13)-NH₂ has been identified as the most potent dual NOP/mu

SUBMITTER: Pacifico S 

PROVIDER: S-EPMC8279409 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature