Corticosterone/cortisol

Die selektive Reduktion der 20-Oxo-prcgnene fiihrt zu pharmazeutisch wichtigen Cor-ticostcroiden (Progesteron, Corticosteron, Cortisol, Cortison u. a.) z. B. ... 

Data of animal experiments discussed in this chapter suggest a variety of potential pharmacological targets for the treatment of pathological anxiety (Fig. 1). As the occurrence of traumatic events is usually unpredictable, it seems more promising to interfere with consolidation than with acquisition processes. In this context, the sympatho-adrenergic and the hypothalamic-pituitary-adrenal system are of particular interest. Both noradrenaline and corticosterone/cortisol are known to facilitate memory consolidation, in par-... 

Further radiolabeled ligand-binding assays have been reported for a wide variety of analytes, namely morphine and leu-enkephaline [30], (S )-propanolol [33], atra-zine [47], 17-jS-estradiol [59], 2,4-dichlorophenoxyacetic acid (2,4-D) [32], yohimbine and corynanthine [60], and corticosterone/cortisol [29]. Other assays are summarized in Table 3. 

Uhr, M., Holshoer, F., and Muller, M.B. (2002) Penetration of endogenous steroid hormones corticosterone, cortisol, aldosterone and progesterone into fhe brain is enhanced in mice deficient for both mdrla and mdrlb P-glycoproteins. Journal of Neuroendocrinology, 14, 753-759. 

Simultaneous androstenedione, corticosterone, cortisol, cortisone, ll-deo g corticosterone, 11-deoxycortisol, dexamethasone acetate, estradiol, estriol, estrone, 17a-hydro roges-terone, progesterone, testosterone... 

The four corticosteroids, corticosterone, cortisol, cortisone and aldosterone, are structurally and biosynthetically related (see Fig. 10.1, p. 161). The principal ones are corticosterone and aldosterone. The former is present in the highest concentrations in plasma. The ratio corticosteronealdosterone in plasma is approximately 14 1 in domestic fowl, and 63 1 in the duck (Harvey, Scanes Brown, 1986). The enzymes together with P-450 cytochrome, which catalyse the biosynthesis of corticosteroids, are present on the endoplasmic reticulum. 

Reichstain s sub nces R H. M, Q and S see Cortisone, Corticosterone, Cortisol, Cortexone, Cor-texolone. 

In contrast to most it-Cw, A5-C2i or estrogen conjugates, comparative studies with corticosterone and corticosterone-21-sulfate injected into the umbilical vein establish that this ester sulfate is transferred to the mother slightly more quickly than the free hormone (see Section III, D, 3 and Table IV). These studies also demonstrate that the transfer rates of the free corticosteroids from the fetus to the mother are very different after perfusion of corticosterone, cortisol, cortisone, and deoxycortisosterone into the umbilical vein at midgestation, these steroids were transferred very slowly (2-8% of the administered radioactivity is collected in the maternal urine) on the other hand, after tritiated aldosterone was perfused through the umbilical vein, 20 to 30% of the radioactivity was recovered in the maternal urine (Pasqualini, 1970). 

Cortisol-Cortisone Conversion. Under normal conditions, this equilibrium slightly favors the oxidized compound. Similarly, the conversion of corticosterone to 11-deoxycorticosterone is also mediated by the liP-hydroxysteroid dehydrogenase enzyme system and requites NAD(P) /NAD(P)H. This conversion is especially important both in the protection of the human fetus from excessive glucocorticoid exposure, and in the protection of distal nephron mineral ocorticoid receptors from glucocorticoid exposure (14). The impairment of this conversion is thought to result in hypertension associated with renal insufficiency (15). 

C-20 deduction. Two stereoisomers can result from this transformation, although cortisol is thought to act primarily with (R)20P-hydroxysteroid dehydrogenase. This is a first step in the metabohsm of corticosterone. 

The natural compounds cortisol [50-23-7], cortisone [53-06-5], and corticosterone [50-22-6] vary only slightly in stmctures and pharmacologic properties (see Steroids). The synthetic analogues inmore modem practice, prednisolone [52438-85-4], dexamethasone [50-02-2], triamcinolone [124-94-7], and betamethasone have greater antiinflammatory potency, and their effects on sodium retention tend to be less severe. 

Cortisol, corticosterone, cortisone and cortisone-21-acetate see entries in Chapter 6. 

The main mineralocorticoid agonist in humans is aldosterone. Additionally, cortisol, corticosterone, and DOC have also mineralocorticoid agonistic activity. The synthetic steroid fludrocortisone (9a-fluorocorti-sol) is extremely potent and usually chosen for replacement mineralocorticoid therapy. In contrast, aldosterone and DOC are not useful in oral therapy due to rapid degradation in liver after absorption. 

The steroids aldosterone, cortisone, cortisol, 11-P-hydroxyandrostenedione, corticosterone, and rostenedione, 11-desoxycorticosterone, 17-hydroxy-progesterone, and progesterone have been performed on Ultrasphere ODS using methanokwater.19 Ranitidine N-[2-[[[5-[(dimethylamino)methyl]-2-furanyl]-methyl]thio]ethyl]-N1-methyl-2-nitro-l,l-ethenediamine has been separated using a p-Bondapak C18 column operated with acetoni-trile methanol water buffered with triethylamine phosphate.117 Pyridoxal-5 -phosphate and other B6 vitamers, including pyridoxamine phosphate, pyri-doxal, pyridoxine, and 4-pyridoxic acid, were separated as bisulfite adducts... 

High doses of caffeine produce a stresslike neuroendocrine response (Spindel 1984 Spindel et al. 1984). This includes increased levels of corticosterone, jS-endorphin, and decreased serum growth hormone and thyrotropin-stimulating hormone in the rat. However, similar effects are not observed in humans until approximately 500 mg is consumed, the equivalent of 5 cups of coffee. At this dose in humans, elevations are seen in adrenocorticotrophic hormone, jS-endorphin, and cortisol. 

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