The Antitumor Agent, 1,3-bis(2-chloroethyl)-1-nitrosourea
The Antitumor Agent, 1,3-bis(2-chloroethyl)-1-nitrosourea
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抗肿瘤剂，1,3-双(2-氯乙基)-1-亚硝基脲
DOI：
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发表时间：
1966
期刊：
影响因子：
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通讯作者：
D. Rall
中科院分区：
文献类型：
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作者：
T. L. Loo;R. L. Dion;R. Dixon;D. Rall
新型高效抗肿瘤剂1，3-双（2-氯乙基）-1-亚硝基脲（BCNU）在pH 4时最稳定。在酸和pH值高于7的溶液中，它迅速分解。在血浆中，BCNU的半衰期为20分钟。在体外，并且少于15分钟。in vivo .它的烷基化作用不是由氯的缓慢水解引起的。在0°时，BCNU与人血浆蛋白的结合率为80%。犬静脉给药时，其容易进入脑脊液（CSF），并迅速从血浆和CSF中消失。4小时内经尿液排泄的原型药物总量。低于剂量的0.1%。在43°下加热5小时。将BCNU部分转化为1，3-双（2-氯乙基）脲。
The new potent antitumor agent, 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU), is most stable at pH 4. In acid and in solutions above pH 7, it decomposes rapidly. In plasma, BCNU has a half-life of 20 min. in vitro , and less than 15 min. in vivo . Its alkylating action is not caused by the slow hydrolysis of the chlorine. BCNU is 80 per cent bound to human plasma protein at 0°. When administered intravenously to the dog, it enters the cerebrospinal fluid (CSF) readily and disappears speedily from the plasma and the CSF. The total amount of unchanged drug excreted in the urine in 4 hr. is less than 0.1 per cent of the dose. Heating at 43° for 5 hr. converts BCNU partly into 1,3-bis(2-chloroethyl)urea.