质子泵抑制剂奥美拉唑、兰索拉唑和泮托拉唑可引起大鼠食管下括约肌松弛。
Proton pump inhibitors omeprazole, lansoprazole and pantoprazole induce relaxation in the rat lower oesophageal sphincter.
机构信息
Department of Pharmacology, Medical Faculty, Mersin University Campus Yenişehir, Mersin, Turkey.
出版信息
J Pharm Pharmacol. 2011 Oct;63(10):1295-300. doi: 10.1111/j.2042-7158.2011.01333.x. Epub 2011 Jul 19.
OBJECTIVES
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.
METHODS
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.
KEY FINDINGS
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.
CONCLUSIONS
Omeprazole, lansoprazole and pantoprazole had a suppressor effect on lower oesophageal sphincter contractions.
目的
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。
方法
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。
主要发现
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。
结论
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。
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