N-去烷基氟西泮

N-去烷基氟西泮
法律規範狀態
法律規範
  • 加：Schedule IV
  • 德：NpSG（仅限工业与科研使用）
  • 英：PSA
识别信息
  • 7-Chloro-5-(2-fluorophenyl)-1,3-dihydro-1,4-benzodiazepin-2-one
CAS号2886-65-9
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.018.863 編輯維基數據鏈接
化学信息
化学式C15H10ClFN2O
摩尔质量288.71 g·mol−1
3D模型（JSmol（英语：JSmol））
熔点205至206 °C（401至403 °F） [1]
  • Fc1ccccc1C2=NCC(=O)Nc3ccc(Cl)cc23

N-去烷基氟西泮（N-Desalkylflurazepam）又称去甲氟西泮（norflurazepam）是一种苯二氮卓类药物的类似物，亦是包括氟西泮[2]、氟托西泮[3]、氟地西泮[4]、咪达唑仑[5]、氟他唑仑[6]、夸西泮[7]与氯氟卓乙酯在内的若干其他苯二氮卓类药物的活性代谢产物[8][9]。其作用时间长，易于蓄积，且会与苯二氮卓受体的各种不同亚型进行非选择性结合[7]。从 2016 年起其便作为策划药出售[10]。

参考

[编辑]
  1. ^ SciFinder record for CAS#2886-65-9
  2. ^ Riva R, de Anna M, Albani F, Baruzzi A. Rapid quantitation of flurazepam and its major metabolite, N-desalkylflurazepam, in human plasma by gas-liquid chromatography with electron-capture detection. Journal of Chromatography. March 1981, 222 (3): 491–5. PMID 7228960. doi:10.1016/S0378-4347(00)84153-5. 
  3. ^ Barzaghi N, Leone L, Monteleone M, Tomasini G, Perucca E. Pharmacokinetics of flutoprazepam, a novel benzodiazepine drug, in normal subjects. European Journal of Drug Metabolism and Pharmacokinetics. 1989, 14 (4): 293–8. PMID 2633923. S2CID 20710732. doi:10.1007/bf03190114. 
  4. ^ Human Toxicology 1st. Elsevier Science. December 1996: 43. 
  5. ^ Vogt S, Kempf J, Buttler J, Auwärter V, Weinmann W. Desalkylflurazepam found in patients' samples after high-dose midazolam treatment. Drug Testing and Analysis. 2013, 5 (9–10): 745–7. PMID 23713025. doi:10.1002/dta.1484. 
  6. ^ Miyaguchi H, Kuwayama K, Tsujikawa K, Kanamori T, Iwata YT, Inoue H, Kishi T. A method for screening for various sedative-hypnotics in serum by liquid chromatography/single quadrupole mass spectrometry. Forensic Science International. February 2006, 157 (1): 57–70. PMID 15869852. doi:10.1016/j.forsciint.2005.03.011. 
  7. ^ 7.0 7.1 Nikaido AM, Ellinwood EH. Comparison of the effects of quazepam and triazolam on cognitive-neuromotor performance. Psychopharmacology. 1987, 92 (4): 459–64. PMID 2888152. S2CID 13162524. doi:10.1007/bf00176478. 
  8. ^ Ba BB, Iliadis A, Cano JP. Pharmacokinetic modeling of ethyl loflazepate (Victan) and its main active metabolites. Annals of Biomedical Engineering. 1989, 17 (6): 633–46. PMID 2574017. S2CID 31310535. doi:10.1007/bf02367467. 
  9. ^ Davi H, Guyonnet J, Necciari J, Cautreels W. Determination of circulating ethyl loflazepate metabolites in the baboon by radio-high-performance liquid chromatography with injection of crude plasma samples: comparison with solvent extraction and thin-layer chromatography. Journal of Chromatography. July 1985, 342 (1): 159–65. PMID 2864352. doi:10.1016/S0378-4347(00)84498-9. 
  10. ^ Manchester KR, Maskell PD, Waters L. a and plasma protein binding values for benzodiazepines appearing as new psychoactive substances. Drug Testing and Analysis. March 2018, 10 (8): 1258–1269. PMID 29582576. doi:10.1002/dta.2387.