Büyükafşar Kansu, Levent Adnan, Ark Mustafa
Department of Pharmacology, Medical Faculty, Mersin University, Campus Yenişehir, Mersin 33169, Turkey.
Br J Pharmacol. 2003 Oct;140(4):743-9. doi: 10.1038/sj.bjp.0705479. Epub 2003 Sep 22.
The effects of two Rho-kinase inhibitors, Y-27632 and fasudil, were investigated on the contractions produced by electrical field stimulation (EFS, 40 V, 1 mS, 2, 4, 8 and 16 Hz, for 20 s), KCl (30 - 60 mm), phenylephrine (Phe) (10-5 - 10-4 m), adenosine-3', 5'-triphosphate (ATP) (10-4 - 10-3 m) and alpha,beta-methylene ATP (10-5 m). EFS produced frequency-dependent reproducible contractile activity, which was almost abolished by guanethidine (10-5 m, for 1 h). This contraction consisted of two components (a phasic initial contraction followed by a tonic one), and it was inhibited by Y-27632 and fasudil (both at 10-5 m). However, these inhibitors had no effect on resting tension of the tissue. Contractions elicited by KCl (30 - 60 mm) were insensitive to guanethidine (10-5 m, for 1 h), but suppressed by Y-27632 (10-5 m) and fasudil (10-5 m). In addition, the contractions induced by Phe (an alpha1-adrenoceptor agonist) and ATP (a purinergic agent) were inhibited significantly by Y-27632 (10-5 m). Phasic contractions evoked by the selective P2X purinoceptor agonist alpha,beta-methylene ATP were also suppressed by Y-27632 (10-5 m). Western blot analysis revealed that the mouse vas deferens expresses Rho-kinase (ROKalpha, ROCK-2 isoform) protein with a molecular weight of approximately 160 kDa. As a positive control, the presence of this protein was also shown in homogenates of smooth muscle from the rat mesenteric artery. In conclusion, Rho-kinase protein is expressed in the mouse vas deferens, and it mediates neurogenic contractile activity as well as the contractions induced by KCl, Phe, ATP and alpha,beta-methylene ATP. Owing to the suppressive effects of Rho-kinase inhibitors on the contractile activity of the vas deferens, the possibility that these compounds might impair ejaculation must be taken into account when considering them as potential agents in the treatment of erectile dysfunction.
研究了两种Rho激酶抑制剂Y-27632和法舒地尔对电场刺激(EFS,40V,1ms,2、4、8和16Hz,持续20s)、氯化钾(30 - 60mM)、去氧肾上腺素(Phe)(10⁻⁵ - 10⁻⁴M)、三磷酸腺苷(ATP)(10⁻⁴ - 10⁻³M)和α,β-亚甲基ATP(10⁻⁵M)所引发收缩的影响。EFS产生频率依赖性的可重复性收缩活动,胍乙啶(10⁻⁵M,作用1小时)几乎可将其消除。这种收缩由两个部分组成(一个相性初始收缩随后是一个强直性收缩),并且它被Y-27632和法舒地尔(均为10⁻⁵M)抑制。然而,这些抑制剂对组织的静息张力没有影响。氯化钾(30 - 60mM)引发的收缩对胍乙啶(10⁻⁵M,作用1小时)不敏感,但被Y-27632(10⁻⁵M)和法舒地尔(10⁻⁵M)抑制。此外,去氧肾上腺素(一种α1肾上腺素能受体激动剂)和ATP(一种嘌呤能药物)诱导的收缩被Y-27632(10⁻⁵M)显著抑制。选择性P2X嘌呤受体激动剂α,β-亚甲基ATP引发的相性收缩也被Y-27632(10⁻⁵M)抑制。蛋白质印迹分析显示,小鼠输精管表达分子量约为160kDa的Rho激酶(ROKα,ROCK-2亚型)蛋白。作为阳性对照,在大鼠肠系膜动脉平滑肌匀浆中也显示出该蛋白的存在。总之,Rho激酶蛋白在小鼠输精管中表达,并且它介导神经源性收缩活动以及由氯化钾、去氧肾上腺素、ATP和α,β-亚甲基ATP诱导的收缩。由于Rho激酶抑制剂对输精管收缩活动的抑制作用,在将这些化合物视为治疗勃起功能障碍的潜在药物时,必须考虑它们可能损害射精的可能性。