丙双吗啉的抗肿瘤作用和吸收分布排泄研究

STUDIES ON ANTITUMOR ACTION AND ADSORPTION,DISTRIBUTION AND EXCRETION OF PROBIMANE

丙双吗啉(AT-2153)是丙亚胺(ICRF 159)的衍生物,ip 80～100mg/kg ×5d,对裸小鼠肾包膜下接种的人肺癌LAK-83移植瘤有显著的抑制作用。接种Lewis肺癌的小鼠,ig [^(14)C]AT-2153后,胃、肠和胆囊的放射性最高,其次为肺的肿瘤转移灶。给药后24和48h的尿和粪中,放射性总排出量分别为给药量的35.2和65.9％。

Probimane (AT-2153) is a derivative of ICRF 159.At the dosagesof 80~100 mg/kg it could significantly inhibit the growth of human pulmonaryadenocarcinoma transpianted into subrenal capsule of nude mice. In mice bearingLewis lung carcinoma after oral administration with [^(14)C]-probimane, the highestradioactivities were found in stomach, intestine and bile, less in the lung metas-tatic foci. After 24 and 48 hours, the total radioactivities excreted both from urineand feces were found to be 35.2% and 65.9%, respectively.