Radioimmunoassay and metabolism of the catechol estrogen 2-hydroxyestradiol

Shinzo Kono, George R. Merriam, David D. Brandon, Donald (Lynn) Loriaux, Mortimer B. Lipsett

Research output: Contribution to journalArticlepeer-review

33 Scopus citations


Plasma levels of 2-hydroxyestradiol (2-OHE2)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 μg/h purified 2-OHE2 elevated its plasma concentration to 155 pg/ml, consistent with a plasma MCR (MCRp) of approximately 20, 000 liters/day. The infusion of [3H] 2-OHE2 to equilibrium and chromatographic separation of the extracted plasma metabolites yielded an MCRp of about 13, 000 liters/day; the major plasma metabolite comigrated with 2-methoxyestradiol, and [3H]/-methoxyestrone was also formed. The MCRp of 2-OHE2 is approximately half that of 2-hydroxyestrone (2-0HE), 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 MCRP values and estrogen receptor affinities of 2-OHE2 and 2-OHE 1 predict a relative potency for effects upon gonadotropin secretion which i close to that observed in vivo.

Original languageEnglish (US)
Pages (from-to)173-176
Number of pages4
JournalJournal of Clinical Endocrinology and Metabolism
Issue number1
StatePublished - 1982
Externally publishedYes

ASJC Scopus subject areas

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


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