New psychoactive substances continue to appear on the drug market. Until recently, new synthetic opioids, which are among the most dangerous new psychoactive substances, primarily encompassed analogs of the potent analgesic fentanyl. Lately, also other new synthetic opioids have increasingly started to surface. This is the first report on the identification and full chemical characterization of brorphine, a novel potent synthetic opioid with a piperidine benzimidazolone structure. A powder, identified as brorphine, was obtained from a patient seeking medical help for detoxification. Brorphine was also found in a serum sample of the patient. Liquid chromatography–high-resolution mass spectrometry (LC–HRMS) identified an exact mass of m/z 400.1020 and 402.1005 for the compound, corresponding to both bromine isotopes. Further chemical characterization was performed by gas chromatography–mass spectrometry, liquid chromatography–diode array detection and Fourier-transform infrared spectroscopy analyses. Finally, the structure was confirmed by performing ¹H-NMR and ¹³C-NMR spectroscopy. In vitro biological activity of brorphine was determined by a cell-based µ-opioid receptor activation assay, resulting in an EC₅₀ of 30.9 nM (13.5 ng/mL) and an E_max of 209% relative to hydromorphone, confirming the high potency and efficacy of this compound. In a serum sample of the patient, brorphine and a hydroxy-metabolite were found using the LC–HRMS screening method. The presence of opioid activity in the serum was also confirmed via the activity-based opioid screening assay. The occurrence of brorphine is yet another example of how the illicit drug market is continuously evolving in an attempt to escape international legislation. Its high potency poses a serious and imminent health threat for any user.

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关于溴吗啡的首次报道：致命的新型精神活性物质的前景是否会出现下一个阿片类药物？

新的精神活性物质继续出现在毒品市场上。直到最近，作为最危险的新型精神活性物质之一的新型合成阿片类药物主要包括强效镇痛药芬太尼的类似物。最近，其他新的合成阿片类药物也越来越多地浮出水面。这是关于鉴定和完全化学表征溴化吗啡的第一份报告，溴化吗啡是具有哌啶苯并咪唑酮结构的新型有效的合成阿片样物质。从一名寻求排毒医疗帮助的患者那里获得了一种名为溴啡的粉末。在患者的血清样本中也发现了Brorphine。液相色谱-高分辨率质谱法（LC-HRMS）鉴定出精确的m / z质量分别对应于两种溴同位素的化合物400.1020和402.1005。通过气相色谱-质谱，液相色谱-二极管阵列检测和傅立叶变换红外光谱分析进行了进一步的化学表征。最后，通过进行¹ H-NMR和¹³ C-NMR光谱来确认结构。通过基于细胞的μ阿片受体激活测定法确定了brorphine的体外生物学活性，得出EC ₅₀为30.9 nM（13.5 ng / mL），E _max为相对于氢吗啡酮为209％，证实了该化合物的高功效和功效。使用LC-HRMS筛查方法在患者的血清样本中发现了brorphine和羟基代谢物。还通过基于活性的阿片样物质筛选测定法确认了血清中阿片样物质活性的存在。溴吗啡的出现是非法药物市场如何不断发展以逃避国际立法的又一个例子。它的高功效对任何使用者都构成了严重且迫在眉睫的健康威胁。