Relative binding affinity of steroids for the corticosterone receptor system in rat hippocampus
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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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MRs have a much higher affinity for CORT (Kd = 0.5 nM) than GRs (Kd = 5.0 nM).
“Mineralocorticoid receptors have a much higher affinity (Kd = 0.5 nM) for CORT than do GRs (Kd =5.0 nM) (De Kloet, Veldhuis, Wagenaars, & Bergink, 1984; De Kloet, Vreugdenhil, Oitzl, & Joels, 1998)”
From Hypothalamic–pituitary–adrenal and hypothalamic–pituitary–gonadal axes: sex differences in regulation of stress responsivity (2017) · cites this paper as De Kloet, Veldhuis, Wagenaars, & Bergink, 1984
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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
- Open access
- Licence
- 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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