Rivara Mirko, Zuliani Valentina
a Dipartimento di Farmacia , Università degli Studi di Parma , Via Area delle Scienze 27/A, I-43124 Parma , Italy.
Expert Opin Investig Drugs. 2016;25(2):215-26. doi: 10.1517/13543784.2016.1121992. Epub 2015 Dec 14.
Effective and safe drugs for the treatment of neuropathic pain are still an unmet clinical need. Neuropathic pain, caused by a lesion or disease that affects the somatosensory system, is a debilitating and hampering condition that has a great economic cost and, above all, a tremendous impact on the quality of life. Sodium channels are one of the major players in generating and propagating action potentials. They represent an appealing target for researchers involved in the development of new and safer drugs useful in the treatment of neuropathic pain. The actual goal for researchers is to target sodium channels selectively to stop the abnormal signaling that characterizes neuropathic pain while leaving normal somatosensory functions intact.
This review covers the most recent publications regarding sodium channel blockers and their development as new treatments for neuropathic pain. The main areas discussed are the natural sources of new blockers, such as venom extracts and the recent efforts from many pharmaceutical companies in the field.
There have been serious efforts by both the pharmaceutical industry and academia to develop new and safer therapeutic options for neuropathic pain. A number of different strategies have been undertaken; the main efforts directed towards the identification of selective blockers starting from both natural products or screening chemical libraries. At this time, researchers have identified and characterized selective compounds against NaV1.7 or NaV1.8 voltage-gated sodium channels but only time will tell if they reach the market.
治疗神经性疼痛的有效且安全的药物仍是未满足的临床需求。神经性疼痛由影响躯体感觉系统的损伤或疾病引起,是一种使人衰弱且造成阻碍的病症,具有巨大的经济成本,最重要的是,对生活质量有极大影响。钠通道是产生和传导动作电位的主要参与者之一。它们是参与开发用于治疗神经性疼痛的新型更安全药物的研究人员感兴趣的靶点。研究人员的实际目标是选择性地作用于钠通道,以阻止表征神经性疼痛的异常信号传导,同时保持正常的躯体感觉功能完整。
本综述涵盖了关于钠通道阻滞剂及其作为神经性疼痛新疗法的发展的最新出版物。讨论的主要领域是新阻滞剂的天然来源,如毒液提取物,以及该领域许多制药公司最近的努力。
制药行业和学术界都在认真努力开发用于神经性疼痛的新型更安全的治疗选择。已经采取了许多不同的策略;主要努力方向是从天然产物或筛选化学文库中鉴定选择性阻滞剂。此时,研究人员已经鉴定并表征了针对NaV1.7或NaV1.8电压门控钠通道的选择性化合物,但只有时间能告诉我们它们是否能进入市场。