Effect of thyroid hormone analogues on the displacement of 125I-L-triiodothyronine from hepatic and heart nuclei in vivo: Possible relationship to hormonal activity

J. H. Oppenheimer, H. L. Schwartz, W. Dillman, Martin I. Surks

Research output: Contribution to journalArticle

73 Citations (Scopus)

Abstract

The capacity of iodotyrosines and iodothyronine analogues to displace tracer[125I] L-3,5,3′ triiodothyronine from specific nuclear binding sites in rat liver and heart was related to the displacement capacity of nonradioactive triiodothyronine. Iodotyrosines and L-3,3′,5′ triiodothyronine ("reverse T3") were devoid of displacement activity. Analogues with 3,5 substitution in the "inner" ring and single "bulk" substitution in the 3′ position in the phenolic ring exhibited the strongest displacement activity. When the distribution, fractional removal rates and metabolic conversion of the analogues were taken into account, displacement activity appeared to correlate well with the reported thyromimetic activity. These results support the biologic relevance of the nuclear sites.

Original languageEnglish (US)
Pages (from-to)544-550
Number of pages7
JournalBiochemical and Biophysical Research Communications
Volume55
Issue number3
DOIs
StatePublished - Dec 10 1973

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Monoiodotyrosine
Triiodothyronine
Thyroid Hormones
Substitution reactions
Reverse Triiodothyronine
Liver
Rats
Binding Sites

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

Cite this

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T2 - Possible relationship to hormonal activity

AU - Oppenheimer, J. H.

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AU - Dillman, W.

AU - Surks, Martin I.

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AB - The capacity of iodotyrosines and iodothyronine analogues to displace tracer[125I] L-3,5,3′ triiodothyronine from specific nuclear binding sites in rat liver and heart was related to the displacement capacity of nonradioactive triiodothyronine. Iodotyrosines and L-3,3′,5′ triiodothyronine ("reverse T3") were devoid of displacement activity. Analogues with 3,5 substitution in the "inner" ring and single "bulk" substitution in the 3′ position in the phenolic ring exhibited the strongest displacement activity. When the distribution, fractional removal rates and metabolic conversion of the analogues were taken into account, displacement activity appeared to correlate well with the reported thyromimetic activity. These results support the biologic relevance of the nuclear sites.

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