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H-2受体拮抗剂(简称H_2阻滞剂)现已作为治疗和预防酸性消化性胃部疾病,如胃溃疡、Zolling-Ellison综合征(ZES)、胃食管返流和急性应激性溃疡和糜烂等。现介绍四种H_2阻滞剂西咪替丁、雷尼替丁、法莫替丁和尼扎替丁。胃作用方面分泌胃酸的壁细胞上的组胺受体属H_2受体,它不被苯海拉明等H_1阻滞剂所阻断。组胺占据H_2受体后,从主细胞及其它细胞释放活化腺苷酸环化酶,增加细胞内cAMP浓度,而cAMP进一步活化壁细胞上质子泵,H~+、K~+-ATP酶,分泌H~+以对抗在钾离子交
H-2 receptor antagonists (referred to as H-2 blockers) are now used to treat and prevent acidic peptic ulcer diseases such as gastric ulcer, Zolling-Ellison syndrome (ZES), gastroesophageal reflux disease and acute stress ulcer And erosion and so on. Four H 2 blockers, cimetidine, ranitidine, famotidine and nizatidine are now introduced. Histamine receptors on the parietal cells that secrete gastric acid in the stomach are H 2 receptors that are not blocked by H 1 blockers such as diphenhydramine. Histamine occupies H_2 receptor, release of activated adenylyl cyclase from the main cells and other cells, increasing intracellular cAMP concentration, and cAMP further activation of parietal cells proton pump, H ~ +, K ~ + -ATP enzyme, Secretion of H ~ + to confront potassium ion exchange