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[用(3H)-咯利普兰对哺乳动物眼中cAMP选择性磷酸二酯酶进行定位]

[Localization of cAMP-selective phosphodiesterase in the mammalian eye by (3H)-rolipram].

作者信息

Liekfeld A, Kaulen P, Kahle G, Wollensak J

机构信息

Augenklinik Virchow-Klinikum, Humboldt-Universität, Berlin.

出版信息

Ophthalmologe. 1996 Oct;93(5):581-5. doi: 10.1007/s003470050043.

Abstract

It has been shown that inhibition of phosphodiesterase (PDE) or an increase in intracellular cyclic adenosine monophosphate (cAMP) can lower the intraocular pressure in mammalian eyes. The PDE inhibitor rolipram binds with high affinity to a cAMP-dependent PDE. In the following study, receptors for rolipram in the mammalian eye are determined by autoradiography. About 1050 histological sections of rabbit (albino and pigmented), rat, monkey (baboon and marmoset) and human eyes were examined concerning rolipram-binding sites in different structures. The highest specific binding of rolipram to the ciliary body epithelium was seen in human, rabbit and baboon eyes. Marmoset eyes showed the highest specific binding in the ciliary body muscle, rat eyes in the retina. Specific binding was consistently high in the ciliary body epithelium and therefore at the site of aqueous humor formation. Because of these results and the known mode of action of rolipram, one can assume a close connection between rolipram-binding sites and the regulation of intraocular pressure.

摘要

已经表明,抑制磷酸二酯酶(PDE)或增加细胞内环磷酸腺苷(cAMP)可降低哺乳动物眼睛的眼压。PDE抑制剂咯利普兰与cAMP依赖性PDE具有高亲和力结合。在以下研究中,通过放射自显影法确定咯利普兰在哺乳动物眼中的受体。检查了约1050张兔(白化和有色)、大鼠、猴(狒狒和狨猴)和人眼的组织学切片,以了解不同结构中的咯利普兰结合位点。在人、兔和狒狒眼中,咯利普兰与睫状体上皮的特异性结合最高。狨猴眼在睫状体肌中显示出最高的特异性结合,大鼠眼在视网膜中显示出最高的特异性结合。在睫状体上皮中特异性结合一直很高,因此在房水形成部位也是如此。由于这些结果以及咯利普兰已知的作用方式,可以假设咯利普兰结合位点与眼压调节之间存在密切联系。

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