Uptake and metabolism of estramustine in the Dunning R3327H tumour
Kruse, E.; Hartley-Asp, B.
In Vivo 2(6): 371-375
1988
ISSN/ISBN: 0258-851X PMID: 2979955 Document Number: 311211
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, is oxidized metabolite estromustine, estradiol and estrone in the plasma and the tumour after intravenous administration of 100 .mu.Ci 3H-estramustine.