Erectogenic effect of the selective phosphodiesterase type 5 inhibitor, DA-8159
Erectogenic effect of the selective phosphodiesterase type 5 inhibitor, DA-8159
复制标题
DOI：
10.1007/bf02976575
复制
发表时间：
2000-10
影响因子：
6.7
通讯作者：
T. Oh;K. Kang;B. Ahn;M. Yoo;W. Kim
中科院分区：
文献类型：
--
作者：
T. Oh;K. Kang;B. Ahn;M. Yoo;W. Kim
用大鼠阴茎勃起试验、离体家兔阴茎海绵体舒张试验和麻醉犬阴茎海绵体内压测定法，评价了新型磷酸二酯酶5抑制剂DA-8159的勃起作用。DA-8159（0.3 - 1 mg/kg）经口给药后，大鼠勃起次数随剂量增加而增加，10 mg/kg时阴茎勃起指数最高。DA-8159可使苯肾上腺素（PHE）引起的兔CC收缩舒张，并以剂量依赖方式降低一氧化氮供体硝普钠（SNP）的IC 50。在戊巴比妥麻醉的狗中，静脉给予DA-8159（1 × 300 μg/kg）以剂量相关的方式加强海绵体内SNP诱导的ICP升高。这些发现表明，DA-8159在治疗勃起功能障碍方面具有显著的治疗潜力。
DA-8159, a new phosphodiesterase 5 inhibitor, was assessed for its erectogenic potential by a penile erection test in rats, the relaxation of isolated rabbit corpus cavernosum (CC), and estimation of the intracavernous pressure (ICP) in the anesthetized dog. Oral administration of DA-8159 (0.3 to 1 mg/kg) increased the number of erections in rats with increasing dosage, with the highest penile erection index at 10 mg/kg. DA-8159 induced the relaxation of phenylephrine (PHE)-induced contractions in the rabbit CC and decreased the IC50of the nitric oxide donor sodium nitroprusside (SNP) in a dose-dependent fashion. In pentobarbital-anesthetized dogs, the intravenous administration of DA-8159 (1≈300 μg/kg) potentiated the increase in ICP induced by the intracavernosal SNP in a dose-related manner. These findings suggest that DA-8159 has significant therapeutic potential in the treatment of erectile dysfunction.