抑制性的影响地高辛和洋地黄毒苷在大鼠皮质甾酮生产带fasciculata-reticularis细胞。

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王SW、Pu高频,菅直人科幻小说,曾CI,王瞧MJ, PS

抑制性的影响地高辛和洋地黄毒苷在大鼠皮质甾酮生产带fasciculata-reticularis细胞。

Br J杂志。2004年8月,142 (7):1123 - 30。Epub 2004年7月12日。

PubMed ID

15249423 (在PubMed

]

文摘

本研究的目的是调查的直接影响和行动机制洋地黄生产皮质甾酮在大鼠肾上腺皮质细胞。雄性老鼠与地高辛的挑战(1 microg毫升(1)千克(1))的存在与否adrenocorticotropin (ACTH、5 microg毫升(1)千克(1))由静脉注射右颈静脉。收集血液样本在0,30岁,60岁,120分钟后的挑战。皮质甾酮的浓度大鼠血浆样品测定等。带fasciculata-reticularis (ZFR可以)在雄性老鼠细胞准备然后孵化有或没有地高辛或洋地黄毒苷的存在与否ACTH (10 (9) m), forskolin (10 (7) m), 8-bromo-cyclic 3”: 5 '一磷酸腺苷(10 (4)m), cyclopiazonic酸(CPA, 10 (5) m), trilostane (10 (6) m), 25-OH-cholesterol(10(5)米),孕烯醇酮(10(5)米)、孕酮(10(5)米),或去氧皮质酮(10 (5)m)在37摄氏度1 h之前媒体的集合。皮质甾酮或孕烯醇酮水平是衡量等。单一的地高辛注入不改变等离子体皮质甾酮的基础水平,但抑制血浆皮质酮水平应对ACTH体内释放。政府的地高辛或洋地黄毒苷降低自发和ACTH-stimulated释放肾上腺酮体外。地高辛(10 (7)-10 (5)m)和洋地黄毒苷(10(7)-10(5)米),但不是乌本苷(10(7)-10(5)米),剂量依赖性抑制皮质甾酮生产forskolin和8-Br-cyclic AMP在老鼠的ZFR可以细胞。地高辛(10(5)(6)-10米)和洋地黄毒苷(10(6)-10(5)米)减毒皮质甾酮生产应对注册会计师。 Digoxin (10(-5) m) or digitoxin (10(-5) m) inhibited cytochrome P450 side-chain cleavage enzyme (cytochrome P450scc) activity (catalyses conversion of cholesterol to pregnenolone in the presence of trilostane) in rat ZFR cells. The enzyme activity of 11 beta-hydroxylase (catalyses conversion of deoxycorticosterone to corticosterone) in ZFR cells was also inhibited by the administration of digoxin (10(-5) m) or digitoxin (10(-5) m).10 These results together suggest that digoxin and digitoxin decrease the release of corticosterone by acting directly on ZFR cells via a Na+, K+-ATPase-independent mechanism involving the inhibition of the activities of adenylyl cyclase, cytochrome P450scc and 11 beta-hydroxylase, as well as the functioning of cyclic AMP and intracellular calcium.

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药物酶

药物	酶	类	生物	药理作用	行动
地高辛	胆固醇侧链裂解酶、线粒体	蛋白质	人类	未知的	抑制剂	细节