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首页> 外文期刊>Biochemical Pharmacology >Efficacy of isatin analogues as antagonists of rat brain and heart atrial natriuretic peptide receptors coupled to particulate guanylyl cyclase.
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Efficacy of isatin analogues as antagonists of rat brain and heart atrial natriuretic peptide receptors coupled to particulate guanylyl cyclase.

机译:Isatin类似物作为大鼠脑和心脏房利钠肽受体与颗粒鸟苷环化酶偶联的拮抗剂的功效。

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摘要

Isatin is an endogenous indole and an inhibitor of atrial natriuretic peptide (ANP) receptors coupled with particulate guanylyl cyclase (GC). In this study, several isatin analogues were tested as inhibitors of ANP-stimulated GC in rat brain and heart membranes. None of these analogues affected activity in the absence of ANP, or stimulated ANP-induced activity. In both tissues, some 5-substituted isatins (5-hydroxyisatin, 5-methylisatin, and 5-aminoisatin) exhibited more effective inhibitory activity than isatin itself, with IC50 values in the range 1.3-20 microM. The efficacy of other analogues varied and was not consistent between the two tissues, raising the possibility of receptor heterogeneity and relative selectivity of inhibition. Some substituted isatins may have a role as pharmacological tools for investigating the physiological roles of natriuretic peptides and their receptors.
机译:Isatin是一种内源性吲哚,是与颗粒鸟苷酰环化酶(GC)偶联的心钠素(ANP)受体的抑制剂。在这项研究中,测试了几种isatin类似物作为大鼠脑和心脏膜中ANP刺激的GC的抑制剂。在没有ANP的情况下,这些类似物均不影响活性,或刺激ANP诱导的活性。在这两个组织中,一些5取代的isatins(5-hydroxyisatin,5-methylisatin和5-aminoisatin)显示出比isatin本身更有效的抑制活性,IC50值在1.3-20 microM之间。其他类似物的功效各不相同,并且在两个组织之间不一致,从而增加了受体异质性和抑制相对选择性的可能性。一些取代的isatin可能作为药理学工具,用于研究利钠肽及其受体的生理作用。

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