[Pharmacokinetics of the antineoplastic agent 14C-prospidin in rats according to distribution data of the radioactive label].
Prospidin--N,N3-di(beta-chloroethyl)-N1,N2-dispirotripiperazinium - is a broad-spectrum antineoplastic drug with low toxicity. Experiments on albino rats with transplanted sarcoma M-1 were made to study the distribution and kinetics of 14C-prospidin labeled in the dispirotripiperazinium part of the molecule. On being given intravenously the drug accumulated for 15 minutes. The maximum value of the differential accumulation ratio (CAR) amounted to 3.34 (kidneys) and 0.16 (thymus). The content of the label in organs and tissues was related both to its presence in the blood and to the penetration into the cell structures. The magnitude of the integral indicator in the kidneys, liver, small intestine, bone marrow, lungs and tumor was considerably higher than in other organs. The accumulation of 14C-prospidin mainly by the lung tissue, bronchi, throat and bone marrow enables a correlation to be elucidated between the accumulation and antineoplastic action in the organs under consideration. The presence of the label in different fragments of the 14C-prospidin molecule (14C-dispirotripiperazinium and 14C-hydroxypropyl grouping) made it possible to establish that the DAR for the former label in organs and tissues 3--6 hours after the drug administration was 2--6 times greater than for the latter. As judged from the integral content of the label, prospidin had begun metabolizing and its biological activity decreased by the time indicated.
D000818:Animals; D007700:Kinetics; D010879:Piperazines / Q000378:metabolism*; D011447:Prospidium / Q000097:blood / Q000378:metabolism*; D051381:Rats; D012513:Sarcoma, Experimental / Q000378:metabolism*; D014018:Tissue Distribution
D010879:Piperazines; D011447:Prospidium
Farmakokinetika protivoopukholevogo preparata 14C-prospidina u krys po dannym raspredeleniia radioaktivnoĭ metki.