阿维扎封

化合物

阿维扎封(英语:Avizafone[1]或Pro-Diazepam)是苯二氮䓬衍生物地西泮的水溶性前药。它可以用于肌肉内给药

阿维扎封
臨床資料
给药途径肌肉注射
ATC碼
  • 未分配
识别信息
  • (2S)-2,6-diamino-N-{[(2-benzoyl-4-chlorophenyl)methylcarbamoyl]methyl}hexanamide
CAS号65617-86-9  checkY
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C22H27ClN4O3
摩尔质量430.93 g·mol−1
3D模型(JSmol英语JSmol
  • Clc1cc(c(N(C(=O)CNC(=O)[C@@H](N)CCCCN)C)cc1)C(=O)c2ccccc2
  • InChI=1S/C22H27ClN4O3/c1-27(20(28)14-26-22(30)18(25)9-5-6-12-24)19-11-10-16(23)13-17(19)21(29)15-7-3-2-4-8-15/h2-4,7-8,10-11,13,18H,5-6,9,12,14,24-25H2,1H3,(H,26,30)/t18-/m0/s1 checkY
  • Key:LTKOVYBBGBGKTA-SFHVURJKSA-N checkY

阿维扎封被血液中的酶代谢形成活性药物地西泮。主要用作有机磷神经毒剂中毒的解毒剂[2][3][4]

参见

参考资料

  1. ^ GB 1517164 
  2. ^ Karlsson B, Lindgren B, Millquist E, Sandberg M, Sellström A. On the use of diazepam and pro-diazepam (2-benzoyl-4-chloro-N-methyl-N-lysylglycin anilide), as adjunct antidotes in the treatment of organophosphorus intoxication in the guinea-pig. The Journal of Pharmacy and Pharmacology. April 1990, 42 (4): 247–51. PMID 1974291. S2CID 32369013. doi:10.1111/j.2042-7158.1990.tb05401.x. 
  3. ^ Lallement G, Renault F, Baubichon D, Peoc'h M, Burckhart MF, Galonnier M, et al. Compared efficacy of diazepam or avizafone to prevent soman-induced electroencephalographic disturbances and neuropathology in primates: relationship to plasmatic benzodiazepine pharmacokinetics. Archives of Toxicology. October 2000, 74 (8): 480–6. PMID 11097386. S2CID 22292597. doi:10.1007/s002040000146. 
  4. ^ Taysse L, Calvet JH, Buée J, Christin D, Delamanche S, Breton P. Comparative efficacy of diazepam and avizafone against sarin-induced neuropathology and respiratory failure in guinea pigs: influence of atropine dose. Toxicology. June 2003, 188 (2–3): 197–209. PMID 12767691. doi:10.1016/s0300-483x(03)00086-6.