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[一种由一氧化氮生成的具有降压和抗聚集特性的可溶性鸟苷酸环化酶新激活剂]

[A new activator of soluble guanylate cyclase generated by nitric oxide and having antihypertensive and anti-aggregation properties].

作者信息

Busygina O G, Belushkina N N, Grigor'ev N B, Severina I S

出版信息

Biokhimiia. 1995 Sep;60(9):1460-7.

PMID:8562654
Abstract

The effects of aminoethylisothiuronium bromide known as a radioprotector on the activity of human platelet soluble guanylate cyclase and on ADP-induced aggregation of human platelets have been studied. It has been shown that in Tris-buffer and at definite pH values aminoethylisothiuronium bromide is converted into mercaptoethylguanidine as a result of a transguanidine rearrangement. The latter contains in its molecule both guanidine and SH-groups which appear to be the donor and acceptor of nitric oxide, respectively. It was found that after its rearrangement into mercaptoethylguanidine, aminoethylisothiuronium bromide activates human platelet soluble guanylate cyclase, inhibits ADP-induced aggregation of human platelets and accelerates their spontaneous disaggregation. The stimulating effect of aminoethylisothiuronium bromide depends on the effectiveness of its transguanidine rearrangement into mercaptoethylguanidine. A molecular mechanism of the hypotensive side effect of aminoethylisothiuronium bromide is proposed.

摘要

已对作为辐射防护剂的溴化氨乙基异硫脲对人血小板可溶性鸟苷酸环化酶活性及对二磷酸腺苷(ADP)诱导的人血小板聚集的影响进行了研究。结果表明,在Tris缓冲液及特定pH值条件下,溴化氨乙基异硫脲通过转胍基重排转化为巯基乙脒。后者分子中同时含有胍基和巯基,它们似乎分别是一氧化氮的供体和受体。研究发现,溴化氨乙基异硫脲重排为巯基乙脒后,可激活人血小板可溶性鸟苷酸环化酶,抑制ADP诱导的人血小板聚集,并加速其自发解聚。溴化氨乙基异硫脲的刺激作用取决于其转胍基重排为巯基乙脒的有效性。本文提出了溴化氨乙基异硫脲降压副作用的分子机制。

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