通过μ-阿片受体途径设计更安全的镇痛药
Designing Safer Analgesics via μ-Opioid Receptor Pathways.
作者信息
Chan H C Stephen, McCarthy Dillon, Li Jianing, Palczewski Krzysztof, Yuan Shuguang
机构信息
Laboratory of Physical Chemistry of Polymers and Membranes, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH B3 495 (Bâtiment CH) Station 6, Lausanne 1015, Switzerland; Faculty of Life Sciences, University of Bradford, Bradford BD7 1DP, UK.
Department of Chemistry, University of Vermont, Burlington, VT 05405, USA.
出版信息
Trends Pharmacol Sci. 2017 Nov;38(11):1016-1037. doi: 10.1016/j.tips.2017.08.004. Epub 2017 Sep 19.
Abstract
Pain is both a major clinical and economic problem, affecting more people than diabetes, heart disease, and cancer combined. While a variety of prescribed or over-the-counter (OTC) medications are available for pain management, opioid medications, especially those acting on the μ-opioid receptor (μOR) and related pathways, have proven to be the most effective, despite some serious side effects including respiration depression, pruritus, dependence, and constipation. It is therefore imperative that both academia and industry develop novel μOR analgesics which retain their opioid analgesic properties but with fewer or no adverse effects. In this review we outline recent progress towards the discovery of safer opioid analgesics.
摘要
疼痛既是一个重大的临床问题，也是一个经济问题，受其影响的人数超过糖尿病、心脏病和癌症患者人数的总和。虽然有多种处方药或非处方药可用于疼痛管理，但阿片类药物，尤其是那些作用于μ-阿片受体（μOR）及其相关途径的药物，已被证明是最有效的，尽管存在一些严重的副作用，包括呼吸抑制、瘙痒、成瘾和便秘。因此，学术界和工业界都必须开发新型的μOR镇痛药，这些药物保留其阿片类镇痛特性，但副作用更少或没有副作用。在这篇综述中，我们概述了在发现更安全的阿片类镇痛药方面的最新进展。
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