Biomedical Research Centre, Sheffield Hallam University, Howard Street, Sheffield S1 1WB, UK.
Eur J Pharmacol. 2011 Jun 25;660(2-3):431-7. doi: 10.1016/j.ejphar.2011.03.053. Epub 2011 Apr 9.
Increased phasic activity in the bladder smooth muscle of animal models and patients with detrusor overactivity has been suggested to underlie the pathophysiology of overactive bladder. Potassium (K+) channels are key regulators of bladder smooth muscle tone and thus may play a role in this altered phasic activity. In this study the effects of K+ channel modulators on the phasic activity of bladder strips from the streptozotocin-induced diabetic rat model of bladder dysfunction were investigated. Bladder strips from rats 1 week following streptozotocin administration and age-matched controls were mounted in tissue baths at 37 °C and the effects of K+ channel modulators on resting basal tension or phasic activity induced by a low concentration of carbachol (0.5 μM) were investigated. Activation of BKCa channels by NS1619 had a minor inhibitory effect on carbachol-induced phasic activity of bladder strips from control and diabetic rats, and significantly inhibited amplitude only at 30 μM. Activation of KATP channels by cromakalim inhibited the frequency of carbachol-induced phasic activity of bladder strips, although strips from diabetic rats showed a trend towards being less sensitive to cromakalim. The BKCa channel blocker iberiotoxin was able to induce phasic activity in resting tissues, with diabetic bladder strips demonstrating significantly enhanced phasic activity compared to controls. In contrast, inhibition of SKCa and KATP channels did not induce phasic activity in resting tissues. In conclusion, responses of diabetic rat bladder to BKCa and KATP channel modulators are altered, suggesting altered function and/or expression of channels which may contribute to bladder dysfunction in this model.
在逼尿肌过度活动的动物模型和患者中,膀胱平滑肌的相位活动增加被认为是膀胱过度活动症的病理生理学基础。钾 (K+) 通道是膀胱平滑肌张力的关键调节剂,因此可能在这种相位活动改变中发挥作用。在这项研究中,研究了 K+通道调节剂对链脲佐菌素诱导的糖尿病膀胱功能障碍大鼠模型膀胱条带的相位活动的影响。在链脲佐菌素给药后 1 周和年龄匹配的对照大鼠的膀胱条带在 37°C 的组织浴中进行了安装,并研究了 K+通道调节剂对基础静息张力或低浓度卡巴胆碱 (0.5 μM) 诱导的相位活动的影响。NS1619 激活 BKCa 通道对对照和糖尿病大鼠膀胱条带的卡巴胆碱诱导的相位活动仅有轻微的抑制作用,仅在 30 μM 时才显著抑制幅度。克罗卡林激活 KATP 通道抑制了卡巴胆碱诱导的膀胱条带的相位活动频率,尽管糖尿病大鼠的条带对克罗卡林的敏感性呈下降趋势。BKCa 通道阻滞剂 Iberiotoxin 能够在静息组织中诱导相位活动,与对照相比,糖尿病膀胱条带显示出明显增强的相位活动。相比之下,抑制 SKCa 和 KATP 通道不会在静息组织中诱导相位活动。总之,糖尿病大鼠膀胱对 BKCa 和 KATP 通道调节剂的反应发生改变,表明通道的功能和/或表达发生改变,这可能导致该模型中的膀胱功能障碍。