目的:  研究西地那非衍生物SDN447，即3-(6,7-二氢-1-甲基-7-氧代-3-丙基-1H-吡唑并[4,3-d]嘧啶-5-基)-N-(正丁氧羰基）苯磺酰胺的药代动力学特征以及对去势后丙酸睾酮诱导大鼠前列腺增生模型的影响。方法: SD雄性大鼠灌胃给药，液相色谱串联质谱分析给药后0.2、0.5、1、1.5、2、4、6和8 h大鼠血浆中SDN447浓度，用Winnonlin 6.3软件计算药代动力学参数。SD雄性大鼠去势后皮下注射丙酸睾酮（5 mg·kg-1·d-1）构建前列腺增生模型，灌胃给药。40 d后，检测大鼠前列腺湿重、前列腺指数，观察前列腺组织形态学变化。结果：  药代动力学结果表明，SDN447相较于西地那非半衰期延长。与模型组比较，SDN447给药组大鼠前列腺湿重和前列腺指数明显降低（P<0.05）。HE染色结果表明，SDN447给药组大鼠前列腺腺上皮乳头和细胞层数较模型组减少。结论： SDN447比西地那非半衰期延长，可以显著抑制大鼠前列腺增生。

Objective: To study pharmacokinetics feature of 3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4，3-d]pyrimidine-5-yl)-N-(n-butyloxycarbonyl)benzenesulfonamide(SDN447),a new sildenafil derivative,and effect on prostatic hyperplasia rats model induced by castration and testosterone propionate. Methods: SD male rats were treated with SDN447 by lavage,and LC-MS/MS was used for drug concentration determination of SDN447 in rats plasma,then the pharmacokinetic parameters were calculated by Winnonlin 6.3 software.After removing of bilateral testes of male rats and subcutaneously injecting of testosterone propionate, the drug groups were fed with SDN447.Prostate glandular wet weight， the index of prostate gland and the morphological changes were examined after 40 days. Results: SDN447 achieved longer halflife compared to sildenafil in rats.SDN447 could significantly reduce the prostate wet weight and the index of prostate gland in rats with benign prostatic hyperplasia. Under optical microscope,the hyperplastic glandular epithelium papilla remitted in SDN447 groups. Conclusion: SDN447 has anti-BPH properties and longer halflife in rat.