Xanthoparmelia Scabrosa,X-Scabrosa:Natural Pyrazolo Pyrimidinone.Super PDE-5 Inhibitor and leader material in over-the-counter (OTC) sexual stimulants!

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X-Scabrosa and Pyrazolopyrimidinone derivatives more prominent efficacy on the treatment of impotence than sildenafil.

Xanthoparmelia Scabrosa Extract X-Scabrosa Natural Pyrazolo Pyrimidinone Xanthoparmelia Lichens Sexual Booster Super Phosphodiesterase-V PDE-5 Inhibitor Viagra Substitutor Epidithiopiperazinodione,4-Methylpiperazines Parmelia lichens sexual booster photo picture image Male erectile dysfunction is one of the most common sexual dysfunctions in men. Although erectile dysfunction can be primarily psychogenic in origin, it often accompanies chronic illnesses, such as diabetes mellitus, heart disease, hypertension, and a variety of neurological diseases. Its prevalence is strongly related to age, with a estimated prevalence of 2% at age 40 years rising to 25-30% by age of 65. Although no data are available on the prevalence of erectile dysfunction in men aged over 75, it is probably over 50%.

 Various treatment options for erectile dysfunction are available, such as counseling, hormonal therapy, self-injection or transurethral application of vasodilator agents, vacuum devices, prosthesis implantation, and venous/arterial surgery. However, these therapeutic options have several limitations such as side effects, high-cost and low efficacy. Therefore it has called for research efforts to develop new, high effective and simple to use treatment methods, potentially oral medication.

 Recently, sildenafil has been developed as a therapeutic agent for male erectile dysfunction by oral administration. Sildenafil is the first in a new class of drugs known as inhibiting phosphodiesterase-5 enzyme distributed specifically in corpus cavernosal tissues and induces relaxation of the corpus cavernosal smooth muscle cells, so that blood flow to the penis is enhanced, leading to an erection. Sildenafil has shown a response rate of around 80% in men with erectile dysfunction of organic cause.

 On the other hand, U.S. Pat. No. 3,939,161 discloses that 1,3-dimethyl-1H-pyrazolopyrimidinone derivatives exhibit anticonvulsant and sedative activiity, and also exhibit anti-inflammatory activity and gastric antisecretory activity; EP 201,188 discloses that 5-substituted pyrazolopyrimidinone derivatives have effects of antagonizing adenosine receptor and of inhibiting phosphodiesterase enzymes and can be used for the treatment of cardiovascular disorders such as heart failure or cardiac insufficiency; EP 463,756, EP 526,004, WO 93/6,104 and WO 93/7,149 disclose that pyrazolopyrimidinone derivatives which inhibit c-GMP phosphodiesterase more selectively than c-AMP phosphodiesterase have efficacy on cardiovascular disorders such as angina pectoris, hypertension, heart failure, atherosclerosis, chronic asthma, etc.; and WO 94/28,902, WO 96/16,644, WO 94/16,657 and WO 98/49,166 disclose that the known inhibitors of c-GMP phosphodiesterase including the pyrazolopyrimidinone derivatives of the above mentioned patents can be used for the treatment of male erectile dysfunction.

 The acid additive salts of pyrazolopyrimidinone derivatives according to the present invention have more prominent efficacy on the treatment of impotence than sildenafil, an already established therapeutic agent for impotence, based on the mechanism of inhibiting phosphodiesterase-5 enzyme. The selectivities for phosphodiesterase-6 and phosphodiesterase-3, of the compounds according to the present invention, are much better than those of sildenafil, reducing the side effects such as visual disorders or cardiovascular disorders. Furthermore, the solubility in water at pH=2 and 5 is much more improved and the metabolism in rat liver is noticeably decreased in some of the pyrazolopyrimidinone derivatives of the present invention. Therefore the probability of better absorption and better in vivo effect can be expected when administered orally compared with sildenafil and the dose of the compound may be reduced.

 The identifier scientists of acid additive salts of pyrazolopyrimidinone derivatives have investigated to develop the improved therapeutic agent for impotence and synthesized new pyrazolo pyrimidinone derivatives which have better potency for the treatment of impotence than that of sildenafil, based on the mechanism of inhibiting phosphodiesterase-5 enzyme. The selectivity over phosphodiesterase-6 distributed in retina and phosphodiesterase-3 distributed in heart, of the compounds of the present invention, is much more improved, to reduce the side effects. The solubility and the metabolism in the liver, which are very important factor affecting the rate of the absorption when administered orally, of the compounds of the present invention is much more improved.

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citations1.Xanthoparmelia Scabrosa,X-Scabrosa:Natural Pyrazolo Pyrimidinone.Super PDE-5 Inhibitor and leader material in over-the-counter (OTC) sexual stimulants!

last edit date:31th,May.2009.