Platelet Aggregation Inhibiting and Anticoagulant Effects of Oligoamines,XXX: Absorption,Organ Distribution,and Excretion of the Oligoamine (+)-(S,S)-1,4-Bis-[4-(3-iodo-4-methoxyphenyl)-butylamino]-butane-2,3-diol and its Metabolites

The pharmacokinetic behaviour of the 131-iodine-labelled title compound 3 * and its metabolites in mice was investigated. A two phase, 1st order elimination profile was observed. The second phase is very slow leaving about 35% of radioactivity in the mice even 100h after i.v. injection, because of high affinity to liver and spleen, caused by strong binding of oligoamines to phospholipids of liver and blood cell membranes. The blood-brain-barrier is not passed. No deep compartments were observed. The doses necessary for antithrombotic effects in vivo were calculated from the blood levels to be 20.5–39.7 μmol/kg for a time interval of 1–6 h after administration.