Funder J W, Pearce P T, Smith R, Smith A I
Medical Research Centre, Prince Henry's Hospital, Melbourne, Australia.
Science. 1988 Oct 28;242(4878):583-5. doi: 10.1126/science.2845584.
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 beta-hydroxy-steroid dehydrogenase, which converts cortisol and corticosterone, but not aldosterone, to their 11-keto analogs. These analogs cannot bind to mineralocorticoid receptors.
盐皮质激素受体，无论是在组织提取物中还是重组衍生的，对生理性盐皮质激素醛固酮以及糖皮质激素皮质醇和皮质酮都具有同等亲和力，而皮质醇和皮质酮的循环浓度比醛固酮高得多。这种受体存在于生理性盐皮质激素靶组织（肾脏、腮腺和结肠）以及非靶组织如海马体和心脏中。在盐皮质激素靶组织中，由于存在11β-羟基类固醇脱氢酶，该酶将皮质醇和皮质酮而非醛固酮转化为它们的11-酮类似物，所以受体在体内对醛固酮具有选择性。这些类似物不能与盐皮质激素受体结合。
