Bilge S Sirri, Kesim Yuksel, Kurt Mehmet, Aksoz Elif, Celik Suleyman
University of Ondokuz Mayis, Department of Pharmacology, Kurupelit, Samsun, Turkey.
Int J Urol. 2005 Sep;12(9):829-34. doi: 10.1111/j.1442-2042.2005.01127.x.
To evaluate the effect of sildenafil, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-selective type 5 phosphodiesterase, on isolated rat vas deferens and its connections with the purinergic system.
Epididymal and prostatic portions of isolated vas deferens were placed in organ baths containing Krebs' solution. Contractions were induced by noradrenaline (NA), adenosine triphosphate (ATP), alpha,beta-methylene ATP and electrical field stimulation (EFS). The effect of sildenafil on the contractions was compared with suramin and Evans blue (EB).
NA, ATP, alpha,beta-methylene ATP and EFS caused contractions in both portions of vas deferens. NA-induced contractions were unaffected by sildenafil and suramin but potentiated by EB. ATP-induced contractions were non-competitively inhibited in both portions by sildenafil and suramin but potentiated by EB. alpha,beta-methylene ATP-induced contractions were unaffected by sildenafil but were inhibited in both portions by suramin and EB. EFS-induced contractions were inhibited by sildenafil and suramin while potentiated by EB.
Sildenafil inhibited the contractions in both portions of vas deferens, as did suramin. We have suggested that purinergic system has a role in this antagonism and it seems to be mediated by an ATP-dependent mechanism instead of a receptor interaction.
评估环磷酸鸟苷(cGMP)特异性5型磷酸二酯酶的选择性抑制剂西地那非对离体大鼠输精管的作用及其与嘌呤能系统的联系。
将离体输精管的附睾段和前列腺段置于含有 Krebs 溶液的器官浴槽中。通过去甲肾上腺素(NA)、三磷酸腺苷(ATP)、α,β-亚甲基三磷酸腺苷和电场刺激(EFS)诱导收缩。将西地那非对收缩的作用与苏拉明和伊文思蓝(EB)进行比较。
NA、ATP、α,β-亚甲基三磷酸腺苷和 EFS 均可引起输精管两段的收缩。NA 诱导的收缩不受西地那非和苏拉明的影响,但被 EB 增强。ATP 诱导的收缩在两段均被西地那非和苏拉明非竞争性抑制,但被 EB 增强。α,β-亚甲基三磷酸腺苷诱导的收缩不受西地那非影响,但在两段均被苏拉明和 EB 抑制。EFS 诱导的收缩被西地那非和苏拉明抑制,而被 EB 增强。
西地那非与苏拉明一样,抑制了输精管两段的收缩。我们认为嘌呤能系统在这种拮抗作用中起作用,并且似乎是由一种依赖 ATP 的机制介导,而不是受体相互作用。