Cited by 47Estrogen and related hormone effectsStress Responses and CortisolAdrenal Hormones and Disorders

Relative binding affinity of steroids for the corticosterone receptor system in rat hippocampus

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De Kloet, E.R., Veldhuis, H.D., Wagenaars, J.L., Bergink, E.W.·1984·Journal of Steroid Biochemistry

Abstract

In cytosol of the hippocampus corticosterone displays highest affinity for the sites that remain available for binding in the presence of excess RU 26988, which is shown to be a "pure" glucocorticoid. A rather high affinity (greater than or equal to 25%) was found for 11 beta-hydroxyprogesterone, 21-hydroxyprogesterone, 5 alpha-corticosterone, 19-nor-deoxycorticosterone, 11-deoxycorticosterone and cortisol. A moderate affinity (greater than 5% and less than 25%) was displayed by about 14 steroids among which progesterone, aldosterone, 9 alpha-fluorocortisol and dexamethasone. Corticosterone also shows highest affinity to plasma transcortin and thymus cytosol in the presence of RU 26988. However, the rank-order in affinity by the competing steroids was distinctly different from that observed in the hippocampus; cf. aldosterone and dexamethasone displaced [3H]corticosterone from sites unoccupied by RU 26988 in the hippocampus but not from transcortin or sites in thymus cytosol. In thymus cytosol some potent glucocorticoids have higher affinity for the [3H]dexamethasone labeled sites than dexamethasone. The binding of [3H]dexamethasone in thymus cytosol is completely abolished in the presence of a 100-fold excess of RU 26988. We conclude that our data support the evidence for RU 26988 as a selective ligand for glucocorticoid receptors. RU 26988 leaves binding sites available with highest affinity for corticosterone in hippocampus cytosol that are distinct from transcortin-like s…

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Crossref · 10.1016/0022-4731(84)90380-7

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Authors
De Kloet, E. R., Veldhuis, H. D., Wagenaars, J. L., & Bergink, E. W.
Affiliations
  • Utrecht University (NL)
  • Organon (Netherlands) (NL)
Venue
Journal of Steroid Biochemistry
Publisher
Elsevier BV
Published
1984-08
Volume
21
Issue
2
Pages
173-178
ISSN
0022-4731 (ISSN-L)
OpenAlex
W2163562190
Cited by
47
References
44
Citations by year
2024: 1 · 2023: 2 · 2022: 1 · 2021: 1 · 2020: 1 · 2019: 1 · 2018: 1 · 2017: 1 · 2013: 2 · 2012: 3
FWCI
1.70
Type
journal article
Language
en
Locations
  • Journal of Steroid Biochemistry (publishedVersion)
  • PubMed (publishedVersion)
  • Utrecht University Repository (Utrecht University) (submittedVersion, other-oa)
  • University of Groningen research database (University of Groningen / Centre for Information Technology) (submittedVersion)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
  • Life Sciences › Neuroscience › Behavioral Neuroscience › Stress Responses and Cortisol
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Adrenal Hormones and Disorders
Keywords
glucocorticoid receptor, corticosterone, relative binding affinity, hippocampus, corticosteroid-binding globulin, dexamethasone, aldosterone, progesterone, cortisol, deoxycorticosterone, 11β-hydroxyprogesterone, receptor selectivity
MeSH terms
Androstanols, Animals, Binding, Competitive, Corticosterone, Dexamethasone, Hippocampus, Ligands, Male, Rats, Inbred Strains, Receptors, Glucocorticoid, Receptors, Steroid, Thymus Gland, Rats

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