Nearly all of the roughly 64,000 Americans who died from opioid overdoses in 2016 succumbed because their breathing shut down, triggered by the effects of the drugs on important receptors in the brain stem. When they are activated, μ-opioid receptors potently relieve pain. They also control respiration. Now, for the first time, a drug that in binding these receptors causes powerful pain relief with less respiratory suppression is being evaluated for marketing approval by the Food and Drug Administration. Biotech company Trevana’s drug, oliceridine, acts as a μ-opioid receptor to activate a pain-relieving signaling pathway with less triggering of a separate path that leads to depressed breathing. Oliceridine is the first so-called “biased opioid” to emerge from human clinical trials. There will certainly be more: In a paper published in Cell this week, scientists at the Scripps Research Institute in Jupiter, Florida, have rigorously demonstrated for the first time in mice that the more biased a compound is toward activating the pain-relieving pathway, the less it suppresses breathing.

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“有偏见”的阿片类药物可以更安全地缓解疼痛

2016 年死于阿片类药物过量的大约 64,000 名美国人中，几乎所有的人都死于呼吸停止，这是由药物对脑干中重要受体的影响引发的。当它们被激活时，μ-阿片受体可以有效地缓解疼痛。它们还控制呼吸。现在，美国食品和药物管理局正在评估一种与这些受体结合可有效缓解疼痛并减少呼吸抑制的药物，以寻求上市许可。生物技术公司 Trevana 的药物 oliceridine 可作为 μ-阿片受体激活止痛信号通路，较少触发导致呼吸抑制的单独通路。Oliceridine 是第一个从人体临床试验中出现的所谓“有偏见的阿片类药物”。肯定会有更多：