Department of Pharmacology, Medical Faculty, Mersin University Campus Yenişehir, Mersin, Turkey.
J Pharm Pharmacol. 2011 Oct;63(10):1295-300. doi: 10.1111/j.2042-7158.2011.01333.x. Epub 2011 Jul 19.
We aimed to investigate effects of the proton pump inhibitors (PPIs) omeprazole, lansoprazole and pantoprazole, which are currently used for the treatment of hyperacidity and gastro-oesophageal reflux, on the reactivity of the isolated rat lower oesophageal sphincter.
Omeprazole, lansoprazole and pantoprazole (all 10(-9) -10(-3) m, cumulatively) were tested on carbachol-induced (10(-6) m) contraction. In addition, the effects of PPI preincubation (all 10(-3) m) on the contractions induced by cumulative carbachol (10(-9) -10(-5) m), angiotensin-2 (10(-9) -10(-5) m) or electrical field stimulation (EFS; 40 V, 32 Hz, 1 ms, 10 s) were assessed. Finally, the effects of PPI on the spontaneous contractile activity of the tissue were also evaluated.
PPI relaxed precontracted lower oesophageal sphincter in a concentration-dependent manner and suppressed carbachol-, angiotensin- and EFS-induced contractions. Furthermore, PPI attenuated spontaneous contractile activity of the tissue.
Omeprazole, lansoprazole and pantoprazole had a suppressor effect on lower oesophageal sphincter contractions.
我们旨在研究目前用于治疗胃酸过多和胃食管反流的质子泵抑制剂（PPIs）奥美拉唑、兰索拉唑和泮托拉唑对离体大鼠食管下括约肌反应性的影响。
用累积剂量的卡巴胆碱（10-6m）诱导收缩，测试奥美拉唑、兰索拉唑和泮托拉唑（均为 10-9-10-3m）的作用。此外，还评估了 PPI 预孵育（均为 10-3m）对累积剂量的卡巴胆碱（10-9-10-5m）、血管紧张素-2（10-9-10-5m）或电刺激（EFS；40V、32Hz、1ms、10s）引起的收缩的影响。最后，还评估了 PPI 对组织自发收缩活动的影响。
PPI 以浓度依赖的方式松弛预先收缩的食管下括约肌，并抑制卡巴胆碱、血管紧张素和 EFS 诱导的收缩。此外，PPI 减弱了组织的自发性收缩活动。
奥美拉唑、兰索拉唑和泮托拉唑对食管下括约肌收缩具有抑制作用。
