Pharmacokinetics of free catecholestrogens and catecholestrogen benzoates.
To provide a definite basis for studies on the biological effects of exogenously administered catecholestrogens, the time courses of the concentrations of these estrogens in serum, pituitary and CNS-tissues were studied in male rats after s.c. injection of either 150 microgram of 4-hydroxyestradiol or 2-hydroxyestradiol (dissolved in 200 microliter sesame oil/ethanol/ascorbic acid; 97.5/2.5/0.1; vol/vol/wt) or equimolar amounts of 4-hydroxyestradiol 3, 4-dibenzoate or 2-hydroxyestradiol 2,3-dibenzoate (dissolved in 200 microliter sesame oil). The injection of free catecholestrogens resulted in bolus-like elevations of the serum and tissue concentrations of the respective compound (max. values up to 9 ng/ml, half-life below 1 h) whereas the injection of catecholestrogen benzoates gave lower (max. values about 1 ng/ml) but prolonged elevations (half-life approx. 24 h and 32 h for 4-OHE2 and 2-OHE2) of the respective free catecholestrogen.
D000818:Animals; D002393:Estrogens, Catechol / Q000097:blood / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D010902:Pituitary Gland / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D013997:Time Factors
D002393:Estrogens, Catechol