National Research Institute of Police Science.
Biol Pharm Bull. 2021;44(2):159-161. doi: 10.1248/bpb.b20-00780.
The agonistic activity of fluorinated and nonfluorinated fentanyl analogs on µ-opioid receptor was investigated using a cell-based assay system. Based on the activity, fentanyl analogs were ranked as follows: fentanyl > isobutyrylfentanyl ≈ butyrylfentanyl ≈ methoxyacetylfentanyl > acetylfentanyl. However, among the fentanyl analogs fluorinated on the N-phenyl ring, 2-fluoro analogs and 3-fluoro analogs showed the strongest and weakest activities, respectively. These results suggest that the 2-fluorinated isomers of fentanyl analogs are more likely to cause poisoning.
采用基于细胞的检测系统，研究了氟化和非氟化芬太尼类似物对μ-阿片受体的激动活性。根据活性，芬太尼类似物的排列顺序如下：芬太尼>异丁酰芬太尼≈丁酰芬太尼≈甲氧基乙酰芬太尼>乙酰芬太尼。然而，在 N-苯环上氟化的芬太尼类似物中，2-氟类似物和 3-氟类似物分别表现出最强和最弱的活性。这些结果表明，芬太尼类似物的 2-氟化异构体更有可能引起中毒。
