Activators of soluble guanylate cyclase for the treatment of male erectile dysfunction
| Autor: | J D Brioni, J P Sullivan, M Nakane, G C Hsieh, T Kolasa, Robert B. Moreland |
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| Rok vydání: | 2001 |
| Předmět: |
Male
medicine.medical_specialty Indazoles Sildenafil Urology Allosteric regulation Enzyme Activators Stimulation Nitric oxide chemistry.chemical_compound Erectile Dysfunction In vivo Internal medicine medicine Animals Humans chemistry.chemical_classification business.industry Male erectile dysfunction PDE5 drug design Enzyme Endocrinology chemistry Solubility Guanylate Cyclase business Allosteric Site |
| Zdroj: | International journal of impotence research. 14(1) |
| ISSN: | 0955-9930 |
| Popis: | 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) 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. |
| Databáze: | OpenAIRE |
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