Sorivudine 是口服有效的,嘧啶核苷抗代谢药物。它的抗病毒活性来自某些 DNA 病毒中存在的特定胸苷激酶选择性转化为核苷酸,从而反过来会干扰病毒 DNA 合成。
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Sorivudine has antiviral activity against several viruses including varicella zoster virus, herpes simplex type 1 virus, and Epstein-Barr virus by interfering with viral DNA synthesis.
体外活性
Sorivudine inhibits strains of HSV-1 and HSV-2 (ID50s (50% inhibitory dose): 0.39 and 0.67 μM, respectively). Sorivudine has antiviral activity against several viruses including varicella-zoster virus, herpes simplex type 1 virus, and Epstein-Barr virus. Sorivudine has in vitro inhibitory activity against the varicella-zoster virus at concentrations of 00001-0.004 mg/ml. These concentrations are over 1000-fold lower than those which are required for the inhibition of VZV replication by acyclovir 3 Sorivudine also inhibits HSV-I replication at concentrations ranging from 0.03-0.1 mg/ml [1][2].
体内活性
Sorivudine has been evaluated in the treatment of HSV-l encephalitis when administered orally to mice. The survival of treated mice is prolonged at dosages in excess of 12.5 mg/kg. A significant decrease in mortality was achieved as well with doses in excess of 50 mg/kg. Sorivudine therapy at dosages as low as 20 mg/kg per day given intramuscularly or 100 mg/kg per day administered orally completely protected against viremia and mortality. There was no evidence of neurotoxicity or abnormalities in hematology or clinical chemistries. Doses as low as 0.2 mg/kg per day were effective; however, breakthrough viremia was noted at lower dosages [2].
Cas No.
77181-69-2
分子式
C11H13BrN2O6
分子量
349.14
别名
BV-araU;索立夫定
储存和溶解度
DMSO:125 mg/mL (358.03 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years