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題名 Long-lasting antinociceptive spinal effects in primates of the novel nociceptin/orphanin FQ receptor agonist UFP-112
作者 Hu, Eric;Calò, Girolamo;Guerrini, Remo;Ko, Mei-Chuan
柯美全
貢獻者 心智、大腦與學習研究中心
關鍵詞 Nociceptin/orphanin FQ;NOP receptors;UFP-112;Spinal cord;Capsaicin;Morphine
日期 2010-01
上傳時間 24-Aug-2015 11:25:40 (UTC+8)
摘要 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)Phe4Aib7Arg14Lys15]N/OFQ-NH2 (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 °C water) and capsaicin-induced thermal hyperalgesia. Intrathecal UFP-112-induced antinociception could be reversed by a NOP receptor antagonist, J-113397 (0.1 mg/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 4–5 h. 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 that intrathecal UFP-112 produced long-lasting morphine-comparable antinociceptive effects without potential itch side effect. This study is the first to provide functional evidence that selective NOP receptor agonists such as UFP-112 alone or in conjunction with morphine may improve the quality of spinal analgesia.
關聯 PAIN, 148(1), 107-113
資料類型 article
DOI http://dx.doi.org/10.1016/j.pain.2009.10.026
dc.contributor 心智、大腦與學習研究中心
dc.creator (作者) Hu, Eric;Calò, Girolamo;Guerrini, Remo;Ko, Mei-Chuan
dc.creator (作者) 柯美全zh_TW
dc.date (日期) 2010-01
dc.date.accessioned 24-Aug-2015 11:25:40 (UTC+8)-
dc.date.available 24-Aug-2015 11:25:40 (UTC+8)-
dc.date.issued (上傳時間) 24-Aug-2015 11:25:40 (UTC+8)-
dc.identifier.uri (URI) http://nccur.lib.nccu.edu.tw/handle/140.119/77944-
dc.description.abstract (摘要) 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)Phe4Aib7Arg14Lys15]N/OFQ-NH2 (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 °C water) and capsaicin-induced thermal hyperalgesia. Intrathecal UFP-112-induced antinociception could be reversed by a NOP receptor antagonist, J-113397 (0.1 mg/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 4–5 h. 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 that intrathecal UFP-112 produced long-lasting morphine-comparable antinociceptive effects without potential itch side effect. This study is the first to provide functional evidence that selective NOP receptor agonists such as UFP-112 alone or in conjunction with morphine may improve the quality of spinal analgesia.
dc.format.extent 130 bytes-
dc.format.mimetype text/html-
dc.relation (關聯) PAIN, 148(1), 107-113
dc.subject (關鍵詞) Nociceptin/orphanin FQ;NOP receptors;UFP-112;Spinal cord;Capsaicin;Morphine
dc.title (題名) Long-lasting antinociceptive spinal effects in primates of the novel nociceptin/orphanin FQ receptor agonist UFP-112
dc.type (資料類型) articleen
dc.identifier.doi (DOI) 10.1016/j.pain.2009.10.026
dc.doi.uri (DOI) http://dx.doi.org/10.1016/j.pain.2009.10.026