RESUMO
Probimane was first synthesized and developed in Shanghai Institute of Materia Medica, Chinese Academy of Science as a novel antit umor agent. Male mice were injected iv 〔14C〕 probimane 3.7?105Bq/20g( 5.62? 107Bq/g ) . At 0.5h,higher radioactivities were found in S87 tumor, kidney, bladder, and vertebra, moderate in skim, lung, liver, blood vessel and gut. The radioactivities tended to decre-aseafter 3h except in the tumor, kidney, and gut in which radioactivities persisted. After 12h, only a trace of radioactivity was detected n intestine. The distribution of probimane correlated with its therepeutic efficacy and toxicity.
RESUMO
AIM To compare the effects of probimane( Pro), bimolane ( Bim) and razoxane( Raz) on animal tumor metastasis in vivo . METHODS A biological inoculation method for assessment of pulmonary metastasis of Lewis lung carcinoma(3LL) was employed. RESULTS Pro and Bim inhibited the pulmonary metastasis of 3LL both from d 2 and from d 8 injections, but Raz only inhibited the pulmonary metastasis of 3LL from d 2 injections. Pro inhibited the pulmonary metastasis of 3LL more potently than Bim did at equitoxic dosage. CONCLUSION Pro is better in the treatment of pulmonary metastasis of 3LL than Raz for its possible novel molecular mechanisms.
RESUMO
Pharmaco kinetics of probimane in rabbits was studied by using high-performance liguid chromatography. After the oral adiminis-tration of probimane 75mg/kg to rabbits,the phatmacokinetic characteristics are found to fit a two compartment open model. The pharmacokinetic parameters are: tl/2? = 0.1933h, tl/2? = 4.9568h, K21 =2.9410h-1, K10=0.6492h-1 K12=3.75l2h-1 AUC = 98.9l01h ? mg/L, Cls=0.7583L? kg-1 ? h-1, V/f(c) = 1.0924L ? kg-1, VSS=1.5114L. kg-1.