In vitro pharmacology of fentanyl analogs at the human mu opioid receptor and their spectroscopic analysis.
In vitro pharmacology of fentanyl analogs at the human mu opioid receptor and their spectroscopic analysis.
复制标题
DOI：
10.1002/dta.2822
复制
发表时间：
2020-08
影响因子：
2.9
通讯作者：
Anand JP
中科院分区：
文献类型：
--
作者：
Hassanien SH;Bassman JR;Perrien Naccarato CM;Twarozynski JJ;Traynor JR;Iula DM;Anand JP
阿片类药物被广泛滥用，占美国过量死亡人数的近一半。在生命、保健和生产力损失方面的代价是巨大的，已被宣布为国家危机。芬太尼是一种高效的μ阿片受体（莫尔）激动剂，在当前阿片类药物流行中发挥着重要作用;芬太尼及其类似物（芬太尼）正日益成为阿片类药物危机中最大的危险之一。非法市场上的芬太尼被认为在最近阿片类药物相关死亡增加中发挥了重要作用。虽然有啮齿类动物同系物在体内和体外数据的一些芬太尼，在此之前，很少有人知道这些非法化合物在人体莫尔（h莫尔）的药理学。利用气相色谱-质谱，核磁共振光谱，并在体外测定，本研究描述了34 fentalogs的光谱和药理学特性。报告的光谱和化学数据将允许在未知或混合样品中容易地识别新型芬太尼。总之，这些数据对执法和临床工作者是有用的，因为它们将有助于识别未知样品中的芬太尼，并可能用于预测暴露后的生理效应。
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.
登录
查看更多内容
影响因子：
2.5
作者：
Marinetti, Laureen J.;Ehlers, Brooke J.
通讯作者：
Ehlers, Brooke J.
影响因子：
6.1
作者：
Astrand, Anna;Toreskog, Amanda;Vikingsson, Svante
通讯作者：
Vikingsson, Svante
影响因子：
6.1
作者：
MIGNAT, C;WILLE, U;ZIEGLER, A
通讯作者：
ZIEGLER, A
影响因子：
2.5
作者：
Ohta, H;Suzuki, S;Ogasawara, K
通讯作者：
Ogasawara, K
影响因子：
3
作者：
Florence CS;Zhou C;Luo F;Xu L
通讯作者：
Xu L