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

Abstract

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 100 h 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 mumol/kg for a time interval of 1-6 h after administration.