GENERAL PHARMACOLOGY OF IS(AMINOMETHYL)-2-ISOPROPYL-1,3-DIOXOLANE]PLATINUM (II)

The general pharmacological properties of inomethyl)-2-isopropyl-1,3-d ioxo-lane]platinum(II) (SKI 2053 R, CAS 146665-77-2), a new potential anticancer agent, were investigated in mice, rats, guinea pigs, rabbit s, cats and dogs. Intravenous administration of SKI 2053 R had no effe ct on the central nervous system. SKI 2053 R had no effect on the auto nomic nervous system and smooth muscles except that it slightly inhibi ted the spontaneous motility of isolated rabbit ileum at a concentrati on of 5 x 10(-5) g/ml. SKI 2053 R did not adversely affect the respira tory-cardiovascular junction, or renal function. SKI 2053 R did not si gnificantly alter the levels of serum glucose, serum free fatty acid a nd plasma lactate, and did not induce hemolysis. SKI 2053 R did not af fect blood coagulation mechanism and liver function. SKI 2053 R did no t exhibit anti-inflammatory activity. It was observed that SKI 2053 R increased the formation of hemolytic plaque by spleen cells of sensiti zed mice at high doses (10 mg/kg and 35 mg/kg). Therefore, it is concl uded from these general pharmacological studies that SKI 2053 R at the doses showing antitumor activity does not induce severe adverse effec ts on the central nervous, autonomic nervous, respiratory-cardiovascul ar, gastrointestinal, peripheral nervous, and other systems in experim ental animals.