PLATELET-AGGREGATION INHIBITING AND ANTIC OAGULANT EFFECTS OLIGOAMINES .30. ABSORPTION, ORGAN DISTRIBUTION, AND EXCRETION OF THE OLIGOAMINE-IODO-4-METHOXYPHENYL)-BUTYLAMINO]-BUTANE-2,3-DIOL AND ITS METABOLITES())
K. Rehse et al., PLATELET-AGGREGATION INHIBITING AND ANTIC OAGULANT EFFECTS OLIGOAMINES .30. ABSORPTION, ORGAN DISTRIBUTION, AND EXCRETION OF THE OLIGOAMINE-IODO-4-METHOXYPHENYL)-BUTYLAMINO]-BUTANE-2,3-DIOL AND ITS METABOLITES()), Archiv der pharmazie, 328(5), 1995, pp. 465-467
The pharmacokinetic behaviour of the 131-iodine-labelled title compoun
d 3 and its metabolites in mice was investigated. A two phase, 1st or
der elimination profile was observed. The second phase is very slow le
aving about 35 % of radioactivity in the mice even 100 h after iv. inj
ection, because of high affinity to liver and spleen, caused by strong
binding of oligoamines to phospholipids of liver and blood cell membr
anes. 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 mu mol/kg for a time
interval of 1-6 h after administration.