西地那非衍生物对雄性家兔和小鼠性行为的影响研究  

Effects of the Sildenafil and Its Derivatives on Sexual Behavior of Male Rabbits

作　　者：杨菊 周岐新[2] 

机构地区：[1]重庆市生物化学及分子药理学重点实验室,重庆市400016 [2]重庆医科大学药学院药理教研室,重庆市400016

出　　处：《中国药房》2007年第16期1223-1225,共3页China Pharmacy

摘　　要：目的:观察西地那非(Sil)衍生物(PP和TS)对家兔离体阴茎海绵体(RCC)舒张作用和对♂小鼠性行为的影响。方法:♂小鼠口服不同剂量的PP和TS后进行交配实验,观测性行为变化,并与Sil的作用进行比较;采用经典量-效曲线法测定PP和TS对一氧化氮(NO)介导的离体RCC的舒张作用。结果:3药均呈剂量依赖性增强♂小鼠性行为能力,缩短性行为潜伏期,TS增强性行为的半数有效量作用明显大于Sil和PP;均呈浓度依赖性增强硝普钠(SNP,NO供体)舒张RCC作用,使浓度-效应曲线平行左移;Sil+SNP和PP+SNP舒张RCC的半数抑制量值明显低于TS+SNP。结论:Sil衍生物能增强NO介导的离体RCC舒张作用,改善♂小鼠性行为能力,PP与Sil作用相当而TS作用相对较弱。OBJECTIVE： To observe the effects of sildenafil （Sil） and its derivatives - PP and TS on the relaxation of isolated rabbit corpus eavernosum （RCC） tissue and sexual behavior of male mice. METHODS： Mate test was performed on male mice after oral administration of diferatent doses of PP and TS to observe the sexual behavior change of male mice, which were compared with the effect of Sil; the effect of PP and TS on NO- mediated relaxation of isolated RCC was determined by means of classical dose-effect curve. RESULTS： All the thrree drugs （Sil, PP and TS） enhanced the sexual behavior of male mice in a dose - dependent manner and shortened the latency of sexual behaviors, and the effect of IS at ED50 value on sexual behavior was significantly greater than that Of Sil and PP. And all the 3 drugs dose - dependently enhanced the relaxation of RCC caused by sodium nitroprusside （SNP, the donor of NO） and made the concentrationeffect curves parallelly shift to the left. The IC50 values of Sil ＋ SNP or PP ＋ SNP were markedly lower than that of TS ＋ SNP for relaxation of RCC. CONCLUSION ： Both Sil and its derivatives - PP and TS can enhance the NO - mediated isolated relaxation of RCC and improve the sexual behaviors of male mice; however, the effects of Sil and PP are equivalent, which are stronger than that of TS.

关 键 词：西地那非 衍生物 性行为 家兔川 鼠 

分 类 号：R965[医药卫生—药理学] R698[医药卫生—药学]