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RU38486生物活性与[3H]地塞米松在大鼠中枢神经系统中受体竞争的相关性研究。

A correlative study of RU38486 biopotency and competition with [3H]dexamethasone for receptors in the rat central nervous system.

作者信息

Allen B D, Sutanto W, Jones M T

机构信息

Human Physiology Department, Royal Holloway and Bedford New College (University of London), Egham, Surrey, England.

出版信息

J Steroid Biochem. 1988;30(1-6):411-5. doi: 10.1016/0022-4731(88)90133-1.

DOI:10.1016/0022-4731(88)90133-1
PMID:3386269
Abstract

Dexamethasone inhibitory action on the release of adrenocorticotrophin has been studied using in vitro anterior pituitary preparations. This inhibition is reversed when the animal is given the antiglucocorticoid compound RU38486 simultaneously with dexamethasone. RU38486 acts at the receptor level and in the cytosolic binding study, it competes with [3H]dexamethasone for the binding sites in pituitary. Such competition is even more pronounced in hypothalamus and hippocampus, indicating that RU38486 also exert its antagonistic action at these sites.

摘要

已使用体外垂体前叶制剂研究了地塞米松对促肾上腺皮质激素释放的抑制作用。当给动物同时给予抗糖皮质激素化合物RU38486和地塞米松时,这种抑制作用会被逆转。RU38486在受体水平起作用,在细胞溶质结合研究中,它与[3H]地塞米松竞争垂体中的结合位点。这种竞争在丘脑下部和海马体中更为明显,表明RU38486在这些部位也发挥其拮抗作用。

相似文献

1
A correlative study of RU38486 biopotency and competition with [3H]dexamethasone for receptors in the rat central nervous system.RU38486生物活性与[3H]地塞米松在大鼠中枢神经系统中受体竞争的相关性研究。
J Steroid Biochem. 1988;30(1-6):411-5. doi: 10.1016/0022-4731(88)90133-1.
2
Activation of rat liver glucocorticoid receptor bound to the antiglucocorticoid RU38486.与抗糖皮质激素RU38486结合的大鼠肝脏糖皮质激素受体的激活。
Biochem Biophys Res Commun. 1985 Dec 17;133(2):745-52. doi: 10.1016/0006-291x(85)90967-2.
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Differences in the interaction of RU 486 and ketoconazole with the second binding site of the glucocorticoid receptor.米非司酮和酮康唑与糖皮质激素受体第二结合位点相互作用的差异。
Endocrinology. 1988 Oct;123(4):1902-6. doi: 10.1210/endo-123-4-1902.
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Autoradiographic study of the nuclear transfer of the antiglucocorticoid compound RU38486 in mouse tissues.抗糖皮质激素化合物RU38486在小鼠组织中核转运的放射自显影研究。
J Steroid Biochem. 1985 Sep;23(3):291-7. doi: 10.1016/0022-4731(85)90407-8.
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RU 38486: a potent antiglucocorticoid in vitro and in vivo.RU 38486:一种在体外和体内均有效的抗糖皮质激素。
J Steroid Biochem. 1985 Sep;23(3):247-51. doi: 10.1016/0022-4731(85)90401-7.
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Blockade of glucocorticoid receptor binding and inhibition of dexamethasone-induced muscle atrophy in the rat by RU38486, a potent glucocorticoid antagonist.强效糖皮质激素拮抗剂RU38486对大鼠糖皮质激素受体结合的阻断作用及对地塞米松诱导的肌肉萎缩的抑制作用。
Endocrinology. 1986 Jul;119(1):375-80. doi: 10.1210/endo-119-1-375.
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Binding studies of the antiglucocorticoid RU38486 in Daudi and Raji lymphoma cells.抗糖皮质激素RU38486在Daudi和Raji淋巴瘤细胞中的结合研究。
J Steroid Biochem. 1989;34(1-6):461-5. doi: 10.1016/0022-4731(89)90128-3.
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Physicochemical characteristics of the interaction of the glucocorticoid antagonist RU38486 with glucocorticoid receptors in vitro, and the role of molybdate.
J Steroid Biochem. 1986 Oct;25(4):473-81. doi: 10.1016/0022-4731(86)90390-0.
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RU 38486: potent antiglucocorticoid activity correlated with strong binding to the cytosolic glucocorticoid receptor followed by an impaired activation.RU 38486:强效抗糖皮质激素活性,与对胞质糖皮质激素受体的强结合相关,随后是激活受损。
J Steroid Biochem. 1984 Jan;20(1):271-6. doi: 10.1016/0022-4731(84)90216-4.
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High affinity binding and regulatory actions of dexamethasone-type I receptor complexes in mouse brain.地塞米松 - I型受体复合物在小鼠大脑中的高亲和力结合及调节作用。
Endocrinology. 1989 Sep;125(3):1194-203. doi: 10.1210/endo-125-3-1194.

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