三种H_2受体拮抗剂诱导鼠胃壁细胞H_2受体脱敏的比较  

Differences among desensitization of histamine H_2 receptor induced by three H_2 receptor antagonists on rat gastric parietal cells

作　　者：李玲[1] 罗和生[1] 刘艳[1] 

机构地区：[1]武汉大学人民医院消化内科,湖北省武汉市430060

出　　处：《世界华人消化杂志》2005年第17期2145-2147,共3页World Chinese Journal of Digestology

摘　　要：目的:研究3种H2受体拮抗剂对鼠胃粘膜壁细胞H2受体脱敏的诱导能力.方法:用酶消化法分离壁细胞后分为西咪替丁,雷尼替丁和法莫替丁3组,检测不同时间、不同浓度的H2受体拮抗剂对各组壁细胞H+-K+-ATP酶活力的影响.结果:不同时间、不同药物浓度干预后,各组细胞酶活力均发生显著变化.法莫替丁组细胞酶活力在1、2、4h时(589.34±2.7,812.82±8.35,637.15±4.59)均明显高于雷尼替丁组(169.38±93.64,343.46±44.88,234.07±4.72)和西咪替丁组(118.42±5.91,110.62±1.28,102.43±3.44,P<0.01),而雷尼替丁组在2、4h时才与西咪替丁组有显著性差异(P<0.01).在10、100mg/L条件下,法莫替丁组细胞酶活力(178.21±20.38,225.65±16.41)均明显高于雷尼替丁组(70.88±21.44,128.03±8.22)和西咪替丁组(123.62±4.32,125.40±7.45,P<0.01),当浓度增高至1000mg/L法莫替丁、雷尼替丁组均明显高于西咪替丁组(233.44±6.24,131.58±11.50vs109.88±0.69,P<0.01,P<0.05).结论:三种H2受体拮抗剂对壁细胞H2受体脱敏的诱导能力存在一定的差别,其中法莫替丁最强,西咪替丁最弱.AIM： To investigate the differences of the desensitization of the histamine H2 receptor induced by three H2 receptor antagonists on the gastric parietal cells in rats. METHODS： The gastric parietal cells were isolated by pronase digestion and then divided into three groups： cimetidine, ranitidine and famotidine treatment group. The activity of the H^＋-K^＋-ATPase was detected by H^＋- K^＋-ATPase kit after the cells were treated with different concentrations of the antagonists for different times. RESULTS： Significant changes of the H^＋-K^＋-ATPase activity were observed after the cells were treated with different concentrations of the antagonists at different times. The activities of H^＋-K^＋-ATPase were significantly higher in famotidine group at 1, 2, and 4 h （589.34±2.7, 812.82±8.35, 637.15±4.59） than those in ranitidine （169.38±93.64, 343.46±44.88, 234.07±4.72） and cimetidine （118.42±5.91, 110.62±1.28, 102.43±3.44） group （P 〈0.01）. The activity in ranitidine group was markedly higner than that in cimetidine group at 2 and 4 h. Famotidine increased the activities of H^＋-K^＋- ATPase significantly at the concentrations of 10 and 100 mg/L（178.21±20.38, 225.65±16.41） as compared with ranitidine and cimetidine did （70.88±21.44,128.03±8.22 ; 123.62±4.32, 125.40±7.45）（P 〈0.01）. At the concentration of 1000 mg/L, both famotidine and ranitidine increased the activity of H^＋-K^＋-ATPase obviously as compared with cimetidine did （233.44±6.24, 131.58±11.50 vs 109.88±0.69, P〈0.01, P〈0.05）. CONCLUSION： Three H2 receptor antagonists can induce different desensitization of the H2 receptor, among which famotidine induces the strongest and cimetidine does the weakest.

关 键 词：脱敏 H2受体 H2受体拮抗剂 H^+-K^+-ATP酶 

分 类 号：R573[医药卫生—消化系统]