Activators of soluble guanylate cyclase for the treatment of male erectile dysfunction

被引：43

作者：

Brioni, JD ^{[1
]}

Nakane, M ^{[1
]}

Hsieh, GC ^{[1
]}

Moreland, RB ^{[1
]}

Kolasa, T ^{[1
]}

Sullivan, JP ^{[1
]}

机构：

[1] Abbott Labs, Global Pharmaceut Res & Dev, Neurosci Res, Abbott Pk, IL 60064 USA

来源：

INTERNATIONAL JOURNAL OF IMPOTENCE RESEARCH | 2002年 / 14卷 / 01期

关键词：

guanylate cyclase; YC-1; penile erection; erectile dysfunction; corpus cavernosum; sildenafil; cGMP;

D O I：

10.1038/sj.ijir.3900801

中图分类号：

R5 [内科学]; R69 [泌尿科学（泌尿生殖系疾病）];

学科分类号：

1002 ; 100201 ;

摘要：

Soluble guanylate cyclase (sGC) is an important enzyme in corpus cavernosum smooth muscle cells as it is one of the regulators of the synthesis of cGMP. The efficacy of sildenafil (Viagra(TM)) in the treatment of male erectile dysfunction indicates the importance of the cGMP system in the erectile response as the increased levels of cGMP induce relaxation of the corpus cavernosum. sGC is physiologically activated by nitric oxide (NO) during sexual stimulation, and its activity can be pharmacologically enhanced by several NO-donors. Agents like YC-1 can also activate sGC after binding to a novel allosteric site in the enzyme, a site different from the NO binding site. YC-1 can relax rabbit cavernosal tissue and it facilitates penile erection in vivo. This review summarizes the enzymology, biochemistry and pharmacology of this novel allosteric site and its relevance for the regulation of penile function. This type of sGC activators represent a new class of compounds with a different pharmacological profile in comparison to the classical NO-donors and they could be beneficial for the treatment of male erectile dysfunction.

引用

页码：8 / 14

页数：7

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