Uptake and metabolism of estramustine in the Dunning R3327H tumour.
A time-dependent plasma, tumour cell and nuclear uptake was found after intraperitoneal 3H-estramustine administration, in rats bearing the Dunning H tumour. Uptake of the drug into tumour cells had not reached a maximum after 4 h, whereas no real change was seen in the nuclear fraction after 2 h. Binding to the nuclear protein matrix of Dunning H tumour cells of 3H-estramustine was also found (2.46 pmol/g protein). High performance liquid chromatography demonstrated the existence of estramustine, its oxidized metabolite estromustine, estradiol and estrone in the plasma and the tumour after intravenous administration of 100 microCi 3H-estramustine.
Kruse
E
E
Department of Biochemistry, University of Lund, Sweden.
Hartley-Asp
B
B
D000818:Animals; D001692:Biological Transport; D002460:Cell Line; D002467:Cell Nucleus / Q000378:metabolism; D004961:Estramustine / Q000097:blood / Q000378:metabolism* / Q000493:pharmacokinetics; D008297:Male; D011471:Prostatic Neoplasms / Q000097:blood / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D014316:Tritium
D014316:Tritium; D004961:Estramustine