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本文引用的文献

1
A Selective Nociceptin Receptor Antagonist to Treat Depression: Evidence from Preclinical and Clinical Studies.一种用于治疗抑郁症的选择性孤啡肽受体拮抗剂：来自临床前和临床研究的证据。
Neuropsychopharmacology. 2016 Jun;41(7):1803-12. doi: 10.1038/npp.2015.348. Epub 2015 Nov 20.
2
Small-molecule nociceptin receptor agonist ameliorates mast cell activation and pain in sickle mice.小分子孤啡肽受体激动剂可改善镰状小鼠的肥大细胞活化及疼痛。
Haematologica. 2015 Dec;100(12):1517-25. doi: 10.3324/haematol.2015.128736. Epub 2015 Aug 20.
3
Cebranopadol : a first-in-class potent analgesic agent with agonistic activity at nociceptin/orphanin FQ and opioid receptors.塞布瑞诺帕多：一种一流的强效镇痛药，对孤啡肽/孤啡肽FQ受体和阿片受体具有激动活性。
Expert Opin Investig Drugs. 2015 Jun;24(6):837-44. doi: 10.1517/13543784.2015.1036985. Epub 2015 Apr 12.
4
Supraspinal actions of nociceptin/orphanin FQ, morphine and substance P in regulating pain and itch in non-human primates.孤啡肽/痛敏肽、吗啡和P物质在调节非人灵长类动物疼痛和瘙痒中的脊髓上作用
Br J Pharmacol. 2015 Jul;172(13):3302-12. doi: 10.1111/bph.13124. Epub 2015 Apr 24.
5
Acute and subchronic antinociceptive effects of nociceptin/orphanin FQ receptor agonists infused by intrathecal route in rats.鞘内注射孤啡肽/强啡肽原受体激动剂对大鼠急性和亚慢性抗伤害作用。
Eur J Pharmacol. 2015 May 5;754:73-81. doi: 10.1016/j.ejphar.2015.02.020. Epub 2015 Feb 19.
6
Mechanical hyperalgesia in rats with diabetic polyneuropathy is selectively inhibited by local peripheral nociceptin/orphanin FQ receptor and µ-opioid receptor agonism.糖尿病多发性神经病大鼠的机械性痛觉过敏可被局部外周孤啡肽/强啡肽 FQ 受体和 μ 阿片受体激动剂选择性抑制。
Eur J Pharmacol. 2015 May 5;754:61-5. doi: 10.1016/j.ejphar.2015.01.049. Epub 2015 Feb 16.
7
Effects of the NOP agonist SCH221510 on producing and attenuating reinforcing effects as measured by drug self-administration in rats.阿片受体（NOP）激动剂SCH221510对大鼠药物自我给药所测产生和减弱强化作用的影响。
Eur J Pharmacol. 2014 Dec 15;745:182-9. doi: 10.1016/j.ejphar.2014.10.029. Epub 2014 Oct 29.
8
Design, synthesis and evaluation of [(3)H]PF-7191, a highly specific nociceptin opioid peptide (NOP) receptor radiotracer for in vivo receptor occupancy (RO) studies.[(3)H]PF-7191的设计、合成与评价，一种用于体内受体占有率（RO）研究的高特异性孤啡肽阿片肽（NOP）受体放射性示踪剂。
Bioorg Med Chem Lett. 2014 Nov 15;24(22):5219-23. doi: 10.1016/j.bmcl.2014.09.069. Epub 2014 Oct 2.
9
The endogenous nociceptin/orphanin FQ-NOP receptor system as a potential therapeutic target for intestinal disorders.内源性孤啡肽/孤啡肽FQ-阿片受体系统作为肠道疾病的潜在治疗靶点。
Neurogastroenterol Motil. 2014 Nov;26(11):1519-26. doi: 10.1111/nmo.12460.
10
Cebranopadol: a first in-class example of a nociceptin/orphanin FQ receptor and opioid receptor agonist.塞布瑞诺帕多：一种痛敏肽/孤啡肽FQ受体和阿片受体激动剂的首个同类药物实例。
Br J Anaesth. 2015 Mar;114(3):364-6. doi: 10.1093/bja/aeu332. Epub 2014 Sep 23.

孤啡肽阿片受体（NOP）作为治疗靶点：从临床前研究到临床应用的转化进展

Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.

作者信息

Zaveri Nurulain T

机构信息

Astraea Therapeutics , 320 Logue Avenue, Suite 142, Mountain View, California 94043, United States.

出版信息

J Med Chem. 2016 Aug 11;59(15):7011-28. doi: 10.1021/acs.jmedchem.5b01499. Epub 2016 Mar 14.

DOI:10.1021/acs.jmedchem.5b01499
PMID:26878436
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5001850/
Abstract

In the two decades since the discovery of the nociceptin opioid receptor (NOP) and its ligand, nociceptin/orphaninFQ (N/OFQ), steady progress has been achieved in understanding the pharmacology of this fourth opioid receptor/peptide system, aided by genetic and pharmacologic approaches. This research spawned an explosion of small-molecule NOP receptor ligands from discovery programs in major pharmaceutical companies. NOP agonists have been investigated for their efficacy in preclinical models of anxiety, cough, substance abuse, pain (spinal and peripheral), and urinary incontinence, whereas NOP antagonists have been investigated for treatment of pain, depression, and motor symptoms in Parkinson's disease. Translation of preclinical findings into the clinic is guided by PET and receptor occupancy studies, particularly for NOP antagonists. Recent progress in preclinical NOP research suggests that NOP agonists may have clinical utility for pain treatment and substance abuse pharmacotherapy. This review discusses the progress toward validating the NOP-N/OFQ system as a therapeutic target.

摘要

自发现孤啡肽阿片受体（NOP）及其配体孤啡肽/痛敏肽（N/OFQ）以来的二十年里，借助基因和药理学方法，在理解这个第四种阿片受体/肽系统的药理学方面取得了稳步进展。这项研究促使各大制药公司的发现计划催生了大量小分子NOP受体配体。NOP激动剂已在焦虑、咳嗽、药物滥用、疼痛（脊髓性和外周性）及尿失禁的临床前模型中研究其疗效，而NOP拮抗剂则已在帕金森病的疼痛、抑郁和运动症状治疗中进行了研究。临床前研究结果向临床的转化由PET和受体占有率研究指导，特别是对于NOP拮抗剂。临床前NOP研究的最新进展表明，NOP激动剂可能对疼痛治疗和药物滥用药物治疗具有临床效用。本综述讨论了将NOP-N/OFQ系统验证为治疗靶点方面的进展。