Nociceptin/orphanin FQ receptor and pain: Feasibility of the fourth opioid family member

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• 作者：Lorenzo Di Cesare Mannelli ; ^{lorenzo.mannelli@unifi.it" class="auth_mail" title="E-mail the corresponding author} ; Laura Micheli ; Carla Ghelardini
• 关键词：NOP ; MOP ; Morphine ; Chronic pain ; Neuropathic pain
• 刊名：European Journal of Pharmacology
• 出版年：2015
• 出版时间：5 November 2015
• 年：2015
• 卷：766
• 期：Complete
• 页码：151-154
• 全文大小：261 K

文摘

The pharmacological management of chronic pain is a major therapeutic problem. The need of repeated treatments reduces the usefulness of classical analgesic drugs, like 渭 opioid receptor (MOP) agonists, characterized by tolerance development, side effects and abuse. Moreover, the pathological persistence of pain modifies nociceptive signals and pain-devoted structure activity weakening MOP agonists and making difficult the research of new active molecules. Nociceptine/orphanin FQ (N/OFQ) and its receptor (NOP) offers a peculiar opioid system able to interact with MOP receptors and made more sensitive by chronic pain conditions. The pain reliever efficacy of NOP agonists against persistent pain, mainly neuropathic pain, has been highlighted after intrathecal infusions in rats and non human primates (NHPs). The differences emerged between the effects of NOP stimulation in rodents and NHPs allow to hypothesize the relevance of NOP modulators in higher organisms strongly encouraging the development of compounds active by a systemic route. Possible applicative perspectives are (i) selective NOP agonists as such, (ii) NOP modulation as adjuvant of MOP-based treatments, or (iii) mixed non-selective agonists vs NOP and classical opioid receptors.