Corticosteroid receptor-gene variants: Modulators of the stress-response and implications for mental health

On the basis of Scatchard and Lineweaver-Burk analysis, it was demonstrated that a series of drugs either activated or inhibited the function of types II and III glucocorticoid receptors. Analgine (0.04-10.0 mM) and sodium salicylate (12.5-50.0 mM) suppress the type II glucocorticoid receptor function of rat liver cytosol. Maradol (5.0 mM) increases the type II glucocorticoid receptors density but decreases the measurable constant for the [3H]acetonide triamsinolone interaction with type II glucocorticoid receptors. Analgine (1.25-10.0 mM) and sodium salicylate (0.62-10.0 mM) increase the type III glucocorticoid receptor function of rat liver cytosol. Maradol (0.25-1.0 mM) suppresses the type III glucocorticoid receptor function. The mechanism of regulation of the glucocorticoid effect by nonsteroid drugs influencing upon the function of types II and III glucocorticoid receptors is discussed.

Sodium salicylate

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Expression of mineralocorticoid and glucocorticoid receptor mRNA in the human hippocampus

Neuroscience Letters (2000)

Matthias Watzka Stefan Beyenburg Ingmar Blümcke Christian E. Elger F. Bidlingmaier

Mineralocorticoid

10.1016/s0304-3940(00)01325-2

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Citations (54)

Isozymes of 11β-hydroxysteroid dehydrogenase: Which enzyme endows mineralocorticoid specificity?

Steroids (1994)

Zygmunt Krozowski P. Provencher Roy E. Smith Varuni Obeyesekere Wendy Mercer

Hydroxysteroid Dehydrogenases

Mineralocorticoid

Hydroxysteroid Dehydrogenases

10.1016/0039-128x(94)90087-6

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Citations (33)

Mineralocorticoid Action: Target Tissue Specificity Is Enzyme, Not Receptor, Mediated

Science (1988)

John W. Funder P. Pearce Roy E. Smith A. Ian Smith

Mineralocorticoid receptors, both when in tissue extracts and when recombinant-derived, have equal affinity for the physiological mineralocorticoid aldosterone and for the glucocorticoids cortisol and corticosterone, which circulate at much higher concentrations than aldosterone. Such receptors are found in physiological mineralocorticoid target tissues (kidney, parotid, and colon) and in nontarget tissues such as hippocampus and heart. In mineralocorticoid target tissues the receptors are selective for aldosterone in vivo because of the presence of the enzyme 11 β-hydroxy-steroid dehydrogenase, which converts cortisol and corticosterone, but not aldosterone, to their 11-keto analogs. These analogs cannot bind to mineralocorticoid receptors.

Mineralocorticoid

Corticosterone

10.1126/science.2845584

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Corticosteroid receptor-gene variants: Modulators of the stress-response and implications for mental health

European Journal of Pharmacology (2008)

Roel H. DeRijk Nienke van Leeuwen Melanie D. Klok Frans G. Zitman

Mineralocorticoid

10.1016/j.ejphar.2008.03.012

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Citations (115)