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Radioimmunoassay and metabolism of the catechol estrogen 2-hydroxyestradiol

Journal Article · · J. Clin. Endocrinol. Metab.; (United States)
OSTI ID:5800531

Plasma levels of 2-hydroxyestradiol (2-OHE/sub 2/) were measured using a new RIA procedure. Values were below the detection limit of the assay (<10 pg/ml), except in the third trimester of pregnancy, when they rose to approximately 15 pg/ml. The infusion of 130 ..mu..g/h purified 2-OHE/sub 2/ elevated its plasma concentration to 155 pg/ml, consistent with a plasma MCR (MCR/sub p) of approximately 20,000 liters/day. The infusion of (/sup 3/H)2-OHE/sub 2/ to equilibrium and chromatographic separation of the extracted plasma metabolites yielded an MCR/sub p/ of about 13,000 liters/day; the major plasma metabolite comigrated with 2-methoxyestradiol, and (/sup 3/H)delta-methoxyestrone was also formed. The MCR/sub p/ of 2-OHE/sub 2/ is approximately half that of 2-hydroxyestrone (2-OHE)/sub 1/), but much higher than those of other steroids. As is true for 2-OHE/sub 1/ the clearance of 2-OHE/sub 2/ must occur primarily in the blood compartment. Together, the measured MCR/sub p/ values and estrogen receptor affinities of 2-OHE/sub 2/ and 2-OHE/sub 1/ predict a relative potency for effects upon gonadotropin secretion which is close to that observed in vivo.

Research Organization:
National Institutes of Health, Bethesda, MD
OSTI ID:
5800531
Journal Information:
J. Clin. Endocrinol. Metab.; (United States), Journal Name: J. Clin. Endocrinol. Metab.; (United States) Vol. 54:1; ISSN JCEMA
Country of Publication:
United States
Language:
English