Unger C, Eibl H, Engel J, Nagel G A, Eisenbrand G
Department of Hematology and Oncology, University of Göttingen, FRG.
Invest New Drugs. 1987 Dec;5(4):361-4. doi: 10.1007/BF00169975.
The uptake of 14C-labeled 1-(2-chloroethyl)-1-nitroso-3-(2-hydroxyethyl)urea (HECNU) into the brain was investigated in the rat after intracarotid injection according to the method of OLDENDORF, as well as in cisternal cerebrospinal fluid obtained by suboccipital puncture after i.v. injection of the drug. The brain uptake index was 31.9 +/- 2.9%. Cerebrospinal fluid/blood quotients after i.v. injection were 0.82 at 10 min and 1.10 at 60 min. The results of both methods clearly show that HECNU, in spite of its hydrophilic property, easily penetrates the blood-brain barrier.
根据OLDENDORF的方法，在大鼠经颈动脉注射后，研究了14C标记的1-(2-氯乙基)-1-亚硝基-3-(2-羟乙基)脲（HECNU）在脑内的摄取情况，以及在静脉注射该药物后通过枕下穿刺获得的脑池脑脊液中的摄取情况。脑摄取指数为31.9±2.9%。静脉注射后的脑脊液/血液比值在10分钟时为0.82，在60分钟时为1.10。两种方法的结果都清楚地表明，尽管HECNU具有亲水性，但它很容易穿透血脑屏障。
