Radioimmunoassay and metabolism of the catechol estrogen 2-hydroxyestradiol

S. Kono, G. R. Merriam, D. D. Brandon, D. L. Loriaux, M. B. Lipsett

Research output: Contribution to journalArticlepeer-review

33 Scopus citations


Plasma levels of 2-hydroxyestradiol (2-OHE2) was 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 μg/h purified 2-OHE2 elevated its plasma concentration to 155 pg/ml, consistent with a plasma MCR (MCR[p]) of approximately 20,000 liters/day. The infusion of [3H]2-OHE2 to equilibrium and chromatographic separation of the extracted plasma metabolites yielded an MCR[p] of about 13,000 liters/day; the major plasma metabolite comigrated with 2-methoxyestradiol, and [3H]ξ-methoxyestrone was also formed. The MCR[p] of 2-OHE2 is approximately half that of 2-hydroxyestrone (2-OHE1), but much higher than those of other steroids. As is true for 2-OHE1, the clearance of 2-OHE2 must occur primarily in the blood compartment. Together, the measured MCR[p] values and estrogen receptor affinities of 2-OHE2 and 2-OHE1 predict a relative potency for effects upon gonadotropin secretion which is close to that observed in vivo.

Original languageEnglish (US)
Pages (from-to)150-154
Number of pages5
JournalUnknown Journal
Issue number1
StatePublished - 1982
Externally publishedYes

ASJC Scopus subject areas

  • Endocrinology, Diabetes and Metabolism
  • Biochemistry
  • Endocrinology
  • Clinical Biochemistry
  • Biochemistry, medical


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