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胍硫醇——一种具有降压和抗聚集特性的可溶性鸟苷酸环化酶新激活剂。

Guanidine thiol--a new activator of soluble guanylate cyclase with antihypertensive and antiaggregatory properties.

作者信息

Severina I S, Bussygina O G, Belushkina N N, Grigoryev N B

机构信息

Institute of Biomedical Chemistry, Russian Academy of Medical Sciences, Moscow, Russia.

出版信息

Biochem Mol Biol Int. 1995 Jul;36(4):913-25.

PMID:8528155
Abstract

Effects of aminoethylisothiuronium bromide (AET), known as radioprotector, on human platelet soluble guanylate cyclase and on ADP-induced human platelets aggregation were studied. It was shown that AET - in Tris buffer and at certain pH values - is converted, via transguanidine rearrangement, to mercaptoethylguanidine. The latter contains in its molecule both the guanidine and SH groups which act as donor and acceptor of nitric oxide (NO), respectively. It was demonstrated that AET, after its rearrangement to mercaptoethylguanidine, is able to activate human platelet soluble guanylate cyclase, as well as to inhibit ADP-induced human stimulatory effect of AET is dependent on the effectiveness of its transguanidine rearrangement to mercaptoethylguanidine. The molecular mechanism of the hypotensive by - effect of AET is proposed.

摘要

研究了作为辐射防护剂的溴化氨乙基异硫脲(AET)对人血小板可溶性鸟苷酸环化酶以及对ADP诱导的人血小板聚集的影响。结果表明,在Tris缓冲液和特定pH值条件下,AET通过转胍基重排转化为巯基乙胍。后者分子中同时含有胍基和SH基团,它们分别作为一氧化氮(NO)的供体和受体。已证明,AET重排为巯基乙胍后,能够激活人血小板可溶性鸟苷酸环化酶,以及抑制ADP诱导的人血小板聚集。AET刺激作用的有效性取决于其转胍基重排为巯基乙胍的效率。提出了AET降压副作用的分子机制。

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