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新型利尿药奥唑啉酮光学活性异构体的研究。I. 奥唑啉酮肾脏靶结构的立体选择性差异。

Studies with the optically active isomers of the new diuretic drug ozolinone. I. Differences in stereoselectivity of the renal target structures of ozolinone.

作者信息

Greven J, Defrain W, Glaser K, Meywald K, Heidenreich O

出版信息

Pflugers Arch. 1980 Mar;384(1):57-60. doi: 10.1007/BF00589514.

Abstract

The renal actions of the optically active isomers of the new diuretic drug ozolinone were studied by clearance, flowmeter and micropuncture techniques in rats. The levorotatory, but not the dextrorotatory isomer of ozolinone increased urine flow, urinary sodium and chloride excretion and enhanced sodium and chloride concentrations in early distal tubular fluid as checked by in situ microperfusion of Henle's loops. This indicates stereospecificity of the drug's diuretic action. However, both isomers of ozolinone equally inhibited maximal tubular secretion of paraaminohippurate and increased renal blood flow as measured by an electromagnetic flowmeter. Thus, the different renal target structures of ozolinone differ markedly with respect to stereoselectivity.

摘要

采用清除率、流量计和微穿刺技术,在大鼠身上研究了新型利尿药奥唑啉酮旋光异构体的肾脏作用。奥唑啉酮的左旋异构体而非右旋异构体可增加尿流量、尿钠和氯排泄,并通过对亨利袢进行原位微灌注检查发现,其可提高远端小管起始部液体中的钠和氯浓度。这表明该药物利尿作用具有立体特异性。然而,通过电磁流量计测量发现,奥唑啉酮的两种异构体均能同等程度地抑制对氨基马尿酸的最大肾小管分泌,并增加肾血流量。因此,奥唑啉酮不同的肾脏靶结构在立体选择性方面存在显著差异。

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