受损的肾11 9 alpha-fluorocortisol的机会:一个解释其盐皮质激素效力。

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Oelkers W布臣年代,Diederich年代,Krain J, Muhme年代,Schoneshofer M

受损的肾11 9 alpha-fluorocortisol的机会:一个解释其盐皮质激素效力。

中国性金属底座。1994年4月,78 (4):928 - 32。

PubMed ID

8157723 (在PubMed

]

文摘

9 alpha-Fluorocortisol(9αFF)是关于作为一个强200倍的盐皮质激素皮质醇(F)的人,尽管它结合的亲和力F和醛固酮这种人类的盐皮质激素受体。F的低盐皮质激素活性已被证明是由于其快速转换的肾脏可的松(E),不绑定到受体。因此,我们比较F E的转换与9αFF 9 alpha-fluorocortisone 11-hydroxysteroid(9α铁)的脱氢酶在人体内和体外。单一口服剂量的9αFF, 9α铁,和F是正常男性,和免费的排泄9αFF, 9α铁、F和E测定尿液中。人类肾脏和肝脏切片与无标号类固醇,孵化和自由11-hydroxy——11-oxosteroids量化后高效液相色谱分离,紫外吸收。口服F(5毫克)排出70%免费E和30%免费F(比例的免费类固醇)。口服9αFF(5毫克)排出90%免费9αFF和10%免费9α铁。免费9αFF排泄是14倍的F后摄取同样的剂量。口服9α铁(4毫克)也排出90% 9αFF和10% 9α铁。肾脏切片转化为F E更快比9αFF 9α铁。 The conversion of 9 alpha FE to 9 alpha FF is, on the contrary, much faster than that of E to F. Thus, the equilibrium of the reaction is on the 11-oxo side for F/E and on the 11-hydroxy side for 9 alpha FF/9 alpha FE. The interconversion of both pairs of steroids is inhibited by glycyrrhetinic acid in a dose-dependent manner. Liver slices do not measurably convert 9 alpha FF to 9 alpha FE, but do rapidly convert 9 alpha FE into 9 alpha FF. Reflecting this negligible conversion of 9 alpha FF to 9 alpha FE and the low plasma-protein binding of 9 alpha FF, free urinary 9 alpha FF excretion is much higher than that of F after the same oral dose.(ABSTRACT TRUNCATED AT 400 WORDS)

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氟氢可的松