Goffinet D R, Brown J M
Radiology. 1977 Sep;124(3):819-22. doi: 10.1148/124.3.819.
The halogenated pyrimidine analogue 5-bromo-2-deoxycytidine (BCdR) was infused into BALB/C mice bearing EMT-6 tumors via either the intravenous or intra-arterial route. Hepatic dehalogenation of the drug was blocked by 5-diazouracil (DAZU) in order to ascertain its relative importance in the degradation of intravenously administered analogues. Increased radiosensitization was noted with higher intravenous pyrimidine concentrations, but DAZU blockage of dehalogenation had little effect. These studies show that following intravenous infusion, enough BCdR apparently bypasses the hepatic vessels to permit tumor radiosensitization despite dilution of the drug by the systemic circulation.
将卤代嘧啶类似物5-溴-2-脱氧胞苷（BCdR）通过静脉内或动脉内途径注入患有EMT-6肿瘤的BALB/C小鼠体内。为了确定其在静脉注射类似物降解中的相对重要性，用5-重氮尿嘧啶（DAZU）阻断药物的肝脏脱卤作用。静脉内嘧啶浓度较高时，放射增敏作用增强，但DAZU对脱卤作用的阻断影响不大。这些研究表明，静脉内输注后，尽管药物被体循环稀释，但足够的BCdR显然绕过了肝血管，从而实现肿瘤放射增敏。
