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大鼠心脏中的高亲和力醛固酮结合位点(I型受体)。

High affinity aldosterone binding sites (type I receptors) in rat heart.

作者信息

Pearce P, Funder J W

机构信息

Medical Research Centre, Prince Henry's Hospital, Melbourne, Victoria, Australia.

出版信息

Clin Exp Pharmacol Physiol. 1987 Nov-Dec;14(11-12):859-66. doi: 10.1111/j.1440-1681.1987.tb02422.x.

Abstract
  1. The use of the receptor stabilizing agent sodium molybdate, and of RU26988 to exclude [3H]-aldosterone binding from Type II glucocorticoid receptors, has enabled the characterization of high affinity Type I aldosterone binding sites in rat atrial and ventricular cytosols. 2. In adult male and female rats the affinity of binding (Kd 4 degrees C) is approximately 1-2 nmol/l for both atria and ventricles; specificity of binding is similar to that for Type I sites in classical aldosterone target tissues (aldosterone = corticosterone much greater than dexamethasone). 3. Levels of atrial Type I sites are higher than the corresponding levels in ventricle in both males and females, whereas for Type II (classical glucocorticoid) receptors the reverse is the case; levels of both Type I and Type II sites fall over the age range examined (40 days-6 months). 4. The physiological function(s) of cardiac Type I sites, and their in vivo mineralocorticoid or glucocorticoid selectivity, remain to be explored.
摘要
  1. 使用受体稳定剂钼酸钠以及RU26988来排除II型糖皮质激素受体对[3H]-醛固酮的结合,从而能够对大鼠心房和心室胞质溶胶中的高亲和力I型醛固酮结合位点进行表征。2. 在成年雄性和雌性大鼠中,心房和心室的结合亲和力(4℃时的解离常数)约为1-2 nmol/l;结合特异性与经典醛固酮靶组织中I型位点的特异性相似(醛固酮=皮质酮远大于地塞米松)。3. 雄性和雌性大鼠心房I型位点的水平均高于心室中的相应水平,而对于II型(经典糖皮质激素)受体则相反;在研究的年龄范围内(40天至6个月),I型和II型位点的水平均下降。4. 心脏I型位点的生理功能及其体内盐皮质激素或糖皮质激素的选择性仍有待探索。

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