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cp-86,948是一种H_2受体拮抗剂,具有粘膜保护特性及抗胃液分泌活性。其与豚鼠心房组胺H_2-受体的亲合力较甲氰咪胍大15倍,较雷尼替丁大7倍。结扎幽门的大鼠经十二指肠给药时CP-66,948抑制胃酸分泌的平均有效剂量(ED_(50))为2mg/kg,其抑制胃酸分泌的作用较甲氰咪胍大5倍,较雷尼替丁大8倍,而且CP-66,948在用药6小时后仍能抑制94%的胃酸分泌,此时甲氰咪胍已无抑制作用。在组胺刺激的有Heidenhain小胃的狗中,口饲或静脉注射甲氰咪胍、雷尼替丁或CP-66,948后,均可引起剂量依赖的总胃酸排泌量减少,三种药物的ED_(50)值分别为0.lmg和
cp-86,948 is a H 2 receptor antagonist with mucosal protective properties and anti-gastric secretion activity. Its affinity with guinea pig atrial histamine H 2 -receptor 15 times larger than cimetidine, seven times larger than ranitidine. The mean effective dose (ED_ (50)) of CP-66,948 to inhibit gastric acid secretion when administered to the pylorus in duodenum was 2 mg / kg, and its effect of inhibiting gastric acid secretion was 5 times larger than that of cimetidine Ranitidine 8 times larger, and CP-66,948 still inhibit 94% of gastric acid secretion 6 hours after drug use, at this time cimetidine has no inhibitory effect. In histamine-stimulated dogs with Heidenhain Stomach, either oral or intravenous injection of cimetidine, ranitidine or CP-66,948 resulted in a dose-dependent decrease in total gastric acid secretion, ED_ (50) values were 0.lmg and