Long-lasting antinociceptive spinal effects in primates of the novel nociceptin/orphanin FQ receptor agonist UFP-112.

Pain
Eric HuMei-Chuan Ko

Abstract

Chemical modifications of nociceptin/orphanin FQ (N/OFQ) peptide that result in increased potency and resistance to degradation have recently lead to the discovery of [(pF)Phe(4)Aib(7)Arg(14)Lys(15)]N/OFQ-NH(2) (UFP-112), a novel N/OFQ peptide (NOP) receptor agonist. The aim of this study was to investigate the pharmacological profile of intrathecally administered UFP-112 in monkeys under different behavioral assays. Intrathecal UFP-112 (1-10 nmol) dose-dependently produced antinociception against an acute noxious stimulus (50 degrees C water) and capsaicin-induced thermal hyperalgesia. Intrathecal UFP-112-induced antinociception could be reversed by a NOP receptor antagonist, J-113397 (0.1mg/kg), but not by a classic opioid receptor antagonist, naltrexone (0.03 mg/kg). Like intrathecal morphine, UFP-112 produced antinociception in two primate pain models with a similar magnitude of effectiveness and a similar duration of action that last for 4-5h. Unlike intrathecal morphine, UFP-112 did not produce itch/scratching responses. In addition, intrathecal inactive doses of UFP-112 and morphine produced significant antinociceptive effects when given in combination without increasing scratching responses. These results demonstrated t...Continue Reading

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Citations

Jan 15, 2021·Nature·Christopher R DonnellyRu-Rong Ji
Jan 17, 2021·Experimental Neurology·Huiping Ding, Mei-Chuan Ko
Jun 30, 2012·The Journal of Pharmacology and Experimental Therapeutics·Colette M CremeansMei-Chuan Ko
Feb 10, 2012·The Journal of Pharmacology and Experimental Therapeutics·Bruce R BianchiJun Chen
Jul 26, 2012·British Journal of Pharmacology·S MolinariR Guerrini
Apr 8, 2020·Journal of Neuroscience Research·Norikazu KiguchiMei-Chuan Ko
Feb 26, 2010·Expert Opinion on Therapeutic Patents·Tally M Largent-Milnes, Todd W Vanderah
Aug 31, 2016·Proceedings of the National Academy of Sciences of the United States of America·Huiping DingMei-Chuan Ko
Nov 28, 2020·Cellular and Molecular Neurobiology·Cherkaouia KibalyCatherine M Cahill
Feb 23, 2020·Science Translational Medicine·Zilong WangRu-Rong Ji
Dec 2, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Joanna Starnowska-Sokół, Barbara Przewłocka
May 7, 2021·Nihon yakurigaku zasshi. Folia pharmacologica Japonica·Norikazu KiguchiMei-Chuan Ko
May 10, 2020·Current Topics in Medicinal Chemistry·Norikazu KiguchiMei-Chuan Ko
Oct 11, 2011·Peptides·Richard J Bodnar
Nov 27, 2021·British Journal of Pharmacology·Balazs R VargaSusruta Majumdar

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