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| Effect of sildenafil derivative SDN447 on benign prostatic hyperplasia in rats |
| XU Liu-liu, LIN Yan, LI Xiao-xi |
| (Center of Metabolic Disease Research, Nanjing Medical University, Nanjing Jiangsu 210029, China) |
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Abstract 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 halflife 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 halflife in rat.
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Received: 11 March 2016
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2016, Vol. 26 
