BAKER J R
Br J Pharmacol Chemother. 1958 Dec;13(4):436-9. doi: 10.1111/j.1476-5381.1958.tb00234.x.
The toxicity to laboratory animals of 4-(2:6-diaminopyrimidin-4-ylamino)phenylarsine oxide (compound 12,065), and its ability to cure laboratory infections of Trypanosoma rhodesiense were investigated. The intramuscular LD50 to mice was 22 mg./kg.; rats were more susceptible. Monkeys tolerated two daily doses of 6 mg./kg., but not two daily doses of 10 mg./kg. The intramuscular CD50 to mice was about 6 mg./kg. with two strains of T. rhodesiense recently isolated from human patients, and 2 mg./kg. with a strain of T. rhodesiense which had been maintained by cyclical transmission through tsetse flies in the laboratory for about 17 months. These results are compared with those reported by Ainley and Davey (1958) for a strain of T. rhodesiense which had been maintained in the laboratory by cyclical transmission for about 12 years and then by syringe transmission for about 10 years. The syringe-transmitted strain was at least 20 times more susceptible to the drug than the recently isolated strains. The potencies of compound 12,065 and melarsen oxide/BAL in curing T. rhodesiense infections in mice were compared: the CD50 for compound 12,065 was 6.5 mg./kg. and for melarsen oxide/BAL was 3.7 mg./kg. The ratios LD50/CD50 for the drugs were about 4 and 6 respectively.
对4-(2:6-二氨基嘧啶-4-基氨基)苯胂氧化物（化合物12,065）对实验动物的毒性及其治愈罗德西亚锥虫实验性感染的能力进行了研究。对小鼠的肌肉注射半数致死量为22毫克/千克；大鼠更易受影响。猴子能耐受每日两次剂量为6毫克/千克，但不能耐受每日两次剂量为10毫克/千克。对于最近从人类患者分离出的两株罗德西亚锥虫，对小鼠的肌肉注射半数治愈量约为6毫克/千克，而对于在实验室通过采采蝇循环传播维持了约17个月的一株罗德西亚锥虫，半数治愈量为2毫克/千克。将这些结果与艾因利和戴维（1958年）报道的一株在实验室通过循环传播维持了约12年，然后通过注射器传播维持了约10年的罗德西亚锥虫的结果进行了比较。经注射器传播的菌株对该药物的敏感性至少是最近分离出的菌株的20倍。比较了化合物12,065和美拉胂醇氧化物/二巯丙醇治愈小鼠罗德西亚锥虫感染的效力：化合物12,065的半数治愈量为6.5毫克/千克，美拉胂醇氧化物/二巯丙醇的半数治愈量为3.7毫克/千克。这两种药物的半数致死量与半数治愈量之比分别约为4和6。
