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In vitro pharmacology of fentanyl analogs at the human mu opioid receptor and their spectroscopic analysis.
Drug Testing and Analysis ( IF 2.9 ) Pub Date : 2020-06-11 , DOI: 10.1002/dta.2822
Sherif H Hassanien 1 , Jonathon R Bassman 1 , Carmelita M Perrien Naccarato 2 , Jack J Twarozynski 2 , John R Traynor 2, 3 , Donna M Iula 1 , Jessica P Anand 2, 3
Affiliation  

Opioids are widely misused and account for almost half of overdose deaths in the United States. The cost in terms of lives, health care, and lost productivity is significant and has been declared a national crisis. Fentanyl is a highly potent mu opioid receptor (MOR) agonist and plays a significant role in the current opioid epidemic; fentanyl and its analogs (fentalogs) are increasingly becoming one of the biggest dangers in the opioid crisis. The availability of fentalogs in the illicit market is thought to play a significant role in the recent increase in opioid‐related deaths. Although there is both rodent homolog in vivo and in vitro data for some fentalogs, prior to this publication very little was known about the pharmacology of many of these illicit compounds at the human MOR (hMOR). Using gas chromatography–mass spectrometry, nuclear magnetic resonance spectroscopy, and in vitro assays, this study describes the spectral and pharmacological properties of 34 fentalogs. The reported spectra and chemical data will allow for easy identification of novel fentalogs in unknown or mixed samples. Taken together these data are useful for law enforcement and clinical workers as they will aid in the identification of fentalogs in unknown samples and can potentially be used to predict physiological effects after exposure.

中文翻译:

芬太尼类似物在人mu阿片样物质受体上的体外药理作用及其光谱分析。

阿片类药物被广泛滥用,占美国过量用药死亡人数的近一半。在生命,医疗保健和生产力损失方面的代价是巨大的,已被宣布为全国性危机。芬太尼是一种高效的μ阿片受体激动剂,在当前的阿片类药物流行中起着重要作用。芬太尼及其类似物(fentalogs)正日益成为阿片类药物危机中的最大危险之一。据认为,非法市场上存在大量的通缉令在最近与阿片类药物相关的死亡增加中起着重要作用。尽管体内体外都有啮齿动物的同系物某些通俗文献的数据,在该出版物发表之前,人们对人类MOR(hMOR)上许多这类非法化合物的药理学知之甚少。使用气相色谱-质谱法,核磁共振波谱法和体外测定法,本研究描述了34种五味子的光谱和药理特性。报告的光谱和化学数据将使您可以轻松识别未知或混合样品中的新型五味子。这些数据加在一起对执法人员和临床工作者很有用,因为它们将有助于鉴定未知样品中的五味子,并有可能被用于预测暴露后的生理效应。
更新日期:2020-06-11
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