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-di ol 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 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.
Rehse
K
K
Institut für Pharmazie der Freien Universität Berlin.
Wolf
S
S
Wenzel
M
M
D000818:Animals; D000925:Anticoagulants / Q000493:pharmacokinetics*; D002072:Butylene Glycols / Q000493:pharmacokinetics*; D005260:Female; D006207:Half-Life; D007408:Intestinal Absorption; D007457:Iodine Radioisotopes; D051379:Mice; D010975:Platelet Aggregation Inhibitors / Q000493:pharmacokinetics*; D014018:Tissue Distribution
C094625:1,4-bis-(4-(3-iodo-4-methoxyphenyl)butylamino)butane-2,3-diol; D000925:Anticoagulants; D002072:Butylene Glycols; D007457:Iodine Radioisotopes; D010975:Platelet Aggregation Inhibitors