Disposition and anticoagulant activity of biologically active heparin fragments in the rat
The disposition of biologically active (/sup 35/S)heparin fragments was studied in both normal and uremic rats after an i.v. dose of 1 mg/kg. In normal animals, the amount of radioactivity in the blood rapidly decreased with a half-life of less than 2 min whereas the anticoagulant activity showed a half-life of 30 min. By 5 hr, only 0.4% of the initial radioactivity was present in the blood whereas no anticoagulant activity could be detected. The heparin fragments were rapidly excreted: by 5 hr, 85% of the initial dose was excreted into the urine, whereas only 1% of the radioactivity was present in the feces. In contrast, 55% of the initial dose of the same amount of radioactive heparin was excreted into the urine after 5 hr. By 5 hr, 5.2% of the heparin fragments was organ-associated and 3.1% was present in the skin, muscle and bone. One week after injection, 3.9% of the radioactivity was still present in the body. In uremic animals, the radioactivity in the blood decreased to 12% of the initial dose by 5 hr whereas 13.5% was organ-associated and 64% was present in the skin, muscle and bone. Comparison of heparin with di- or hexasac-charide fragments indicated that both the clearance in the blood and the excretion into the urine are size-dependent. By 5 hr, the body burden of heparin is approximately five times higher than it is after the same dose of heparin fragments.
- Research Organization:
- Massachusetts Inst. of Tech., Cambridge
- OSTI ID:
- 5886252
- Journal Information:
- J. Pharmacol. Exp. Ther.; (United States), Journal Name: J. Pharmacol. Exp. Ther.; (United States) Vol. 231:2; ISSN JPETA
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
AMINES
ANIMALS
ANTICOAGULANTS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
CARBOHYDRATES
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
DRUGS
EVEN-ODD NUCLEI
HEMATOLOGIC AGENTS
HEPARIN
INJECTION
INTAKE
INTRAVENOUS INJECTION
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LIGHT NUCLEI
MAMMALS
MUCOPOLYSACCHARIDES
NUCLEI
ORGANIC COMPOUNDS
ORGANIC SULFUR COMPOUNDS
POLYSACCHARIDES
RADIOISOTOPES
RATS
REACTION KINETICS
RETENTION
RODENTS
SACCHARIDES
SULFUR 35
SULFUR ISOTOPES
SYMPTOMS
TISSUE DISTRIBUTION
TRACER TECHNIQUES
UREMIA
VERTEBRATES