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.

疼痛既是主要的临床问题，也是经济问题，其影响的人数超过糖尿病，心脏病和癌症的总和。尽管可以使用多种处方药或非处方药（OTC）来治疗疼痛，但阿片类药物尤其是作用于μ阿片受体（μOR）和相关途径的阿片类药物已被证明是最有效的，尽管有些严重的副作用包括呼吸抑制，瘙痒，依赖性和便秘。因此，当务之急是学术界和工业界都必须开发出新型的μOR镇痛药，这些镇痛药必须保持其阿片样物质的镇痛特性，但副作用很少或没有副作用。在这篇综述中，我们概述了发现更安全的阿片类镇痛药的最新进展。