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一、质子泵抑制剂的开发过程和现状世界上最初的质子泵抑制剂(protonpump inhi-bitor PPI)是奥美拉唑(omeprazole瑞典Hassle社)。所谓质子泵抑制剂是它能特异地抑制壁细胞质子泵即H~+·K~+ —ATP酶,后者是将氢离子释出壁细胞外的最终环节。从1967年开始研究,从500多种化合物中寻找出苯并咪唑衍生物,显示出强力抑酸作用。该剂不同于抗胆硷作用和H_2受体阻断作用药物,而是一种有全新作用机制药物。1973年报告其抑制酸分泌的最终环节即质子泵,从而明确了苯并咪唑衍生物的抑酸作用是对质子泵作用的结果。1979年开发了奥美拉唑。1980
First, proton pump inhibitor development process and the status quo The world’s first proton pump inhibitor (protonpump inhi-bitor PPI) is omeprazole (omeprazole Hassle, Sweden). The so-called proton pump inhibitor is that it can specifically inhibit the parietal proton pump H ~ + · K ~ + -ATP enzyme, which is released to the hydrogen ion parietal cells outside the final link. Starting from 1967, looking for benzimidazole derivatives from more than 500 compounds showed strong acid suppression. This agent is different from the anti-cholinergic and H 2 receptor blocking drugs, but a new mechanism of action drugs. In 1973, it reported the proton pump, which is the final part of the acid secretion inhibition, which made it clear that the acid-suppressing effect of the benzimidazole derivatives is the result of the proton pump. In 1979, omeprazole was developed. 1980