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降钙素基因相关肽受体拮抗剂:超越偏头痛疼痛——骨关节炎的一种潜在镇痛策略?

Calcitonin gene-related peptide receptor antagonists: beyond migraine pain--a possible analgesic strategy for osteoarthritis?

机构信息

Arthritis Research UK Pain Centre, School of Biosciences, University of Nottingham, Sutton Bonington Campus, Leicestershire, LE12 5RD, UK,

出版信息

Curr Pain Headache Rep. 2013 Nov;17(11):375. doi: 10.1007/s11916-013-0375-2.

DOI:10.1007/s11916-013-0375-2
PMID:24068339
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3824306/
Abstract

Osteoarthritis (OA) pain is poorly understood and managed, as current analgesics have only limited efficacy and unwanted side effect profiles. A broader understanding of the pathological mechanisms driving OA joint pain is vital for the development of improved analgesics. Both clinical and preclinical data suggest an association between joint levels of the sensory neuropeptide calcitonin gene-related peptide (CGRP) and pain during OA. Whether a direct causative link exists remains an important unanswered question. Given the recent development of small molecule CGRP receptor antagonists with clinical efficacy against migraine pain, the interrogation of the role of CGRP in OA pain mechanisms is extremely timely. In this article, we provide the background to the importance of CGRP in pain mechanisms and review the emerging clinical and preclinical evidence implicating a role for CGRP in OA pain. We suggest that the CGRP receptor antagonists developed for migraine pain warrant further investigation in OA.

摘要

骨关节炎(OA)疼痛的发病机制尚不清楚,且难以治疗,因为目前的镇痛药疗效有限,且具有不良的副作用。深入了解导致 OA 关节疼痛的病理机制对于开发更好的镇痛药至关重要。临床和临床前数据均表明,关节中感觉神经肽降钙素基因相关肽(CGRP)的水平与 OA 期间的疼痛之间存在关联。是否存在直接的因果关系仍然是一个重要的未解决的问题。鉴于最近开发出了具有偏头痛疼痛临床疗效的小分子 CGRP 受体拮抗剂,因此及时研究 CGRP 在 OA 疼痛机制中的作用。在本文中,我们提供了 CGRP 在疼痛机制中的重要性的背景信息,并回顾了越来越多的临床和临床前证据表明 CGRP 在 OA 疼痛中的作用。我们建议,进一步研究偏头痛疼痛治疗中开发的 CGRP 受体拮抗剂在 OA 中的作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/13a5/3824306/36e10f0a580c/11916_2013_375_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/13a5/3824306/36e10f0a580c/11916_2013_375_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/13a5/3824306/36e10f0a580c/11916_2013_375_Fig1_HTML.jpg

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