维基百科

去甲基氟硝西泮

化合物

去甲基氟硝西泮（英语：Desmethylflunitrazepam或Norflunitrazepam、开发代号：Ro05-4435），也叫Fonazepam，误译作去甲基氟西泮，是一种苯二氮䓬类药物，是氟硝西泮的代谢产物，[1][2][3]已作为设计师药物在网上销售。[4][5]它对GABAA受体的IC50值为1.499 nM。[6][7]

去甲基氟硝西泮
法律规范状态
法律规范
识别信息
  • 5-(2-Fluorophenyl)-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one
CAS号2558-30-7
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.018.072 编辑维基数据链接
化学信息
化学式C15H10FN3O3
摩尔质量299.26 g·mol−1
3D模型（JSmol（英语：JSmol））
  • FC1=C(C=CC=C1)C2=NCC(NC3=C2C=C(C=C3)[N+](=O)[O-])=O
  • InChI=1S/C15H10FN3O3/c16-12-4-2-1-3-10(12)15-11-7-9(19(21)22)5-6-13(11)18-14(20)8-17-15/h1-7H,8H2,(H,18,20)
  • Key:KNGIGRDYBQPXKQ-UHFFFAOYSA-N

参见

编辑

参考资料

编辑
  1. ^ Busker RW, van Henegouwen GM, Kwee BM, Winkens JH. Photobinding of flunitrazepam and its major photo-decomposition product N-desmethylflunitrazepam. International Journal of Pharmaceutics. May 1987, 36 (2–3): 113–120. doi:10.1016/0378-5173(87)90145-1. 
  2. ^ Coller JK, Somogyi AA, Bochner F. Quantification of flunitrazepam's oxidative metabolites, 3-hydroxyflunitrazepam and desmethylflunitrazepam, in hepatic microsomal incubations by high-performance liquid chromatography. Journal of Chromatography. B, Biomedical Sciences and Applications. November 1998, 719 (1–2): 87–92. PMID 9869368. doi:10.1016/S0378-4347(98)00383-1. 
  3. ^ Kilicarslan T, Haining RL, Rettie AE, Busto U, Tyndale RF, Sellers EM. Flunitrazepam metabolism by cytochrome P450S 2C19 and 3A4. Drug Metabolism and Disposition. April 2001, 29 (4 Pt 1): 460–5 [2024-01-17]. PMID 11259331. （原始内容存档于2024-05-05）. 
  4. ^ Moosmann B, Bisel P, Franz F, Huppertz LM, Auwärter V. Characterization and in vitro phase I microsomal metabolism of designer benzodiazepines - an update comprising adinazolam, cloniprazepam, fonazepam, 3-hydroxyphenazepam, metizolam and nitrazolam. Journal of Mass Spectrometry. November 2016, 51 (11): 1080–1089. Bibcode:2016JMSp...51.1080M. PMID 27535017. doi:10.1002/jms.3840. 
  5. ^ Katselou M, Papoutsis I, Nikolaou P, Spiliopoulou C, Athanaselis S. Metabolites replace the parent drug in the drug arena. The cases of fonazepam and nifoxipam. Forensic Toxicology. 2016, 35 (1): 1–10. PMC 5214877  . PMID 28127407. doi:10.1007/s11419-016-0338-5. 
  6. ^ Maddalena DJ, Johnston GA. Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks. Journal of Medicinal Chemistry. February 1995, 38 (4): 715–24. PMID 7861419. doi:10.1021/jm00004a017. 
  7. ^ So SS, Karplus M. Genetic neural networks for quantitative structure-activity relationships: improvements and application of benzodiazepine affinity for benzodiazepine/GABAA receptors. Journal of Medicinal Chemistry. December 1996, 39 (26): 5246–56. PMID 8978853. doi:10.1021/jm960536o. 
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