Uchida M, Ohba S, Ikarashi Y, Misaki N, Kawano O
Pharmacological Laboratory, Grelan Pharmaceutical Co., Ltd., Tokyo, Japan.
Arzneimittelforschung. 1993 Aug;43(8):873-6.
Effects of IGN-2098 (5,6-dimethyl-2-[4-[3-(1-piperidinomethyl)phenoxy]- (z)-2-butenylamino]-4(1H)-pyrimidone dihydrochloride, CAS 126869-04-3) a novel histamine H2-antagonist, on histamine-induced gastric acid secretion were investigated in Heidenhain pouch dogs in comparison with those of famotidine, roxatidine acetate HCl and cimetidine. Orally administered IGN-2098 (0.03-1.0 mg/kg), famotidine (0.01-0.3 mg/kg), roxatidine acetate HCl (0.1-1.0 mg/kg) and cimetidine (0.3-3.0 mg/kg) showed dose-dependent inhibition on histamine-induced gastric acid secretion, and ED50 values of IGN-2098, famotidine, roxatidine acetate HCl and cimetidine were 0.077, 0.024, 0.200 and 0.585 mg/kg, respectively. IGN-2098 was effective even at 6 h after administration and ED50 value was 0.315 mg/kg. IGN-2098 was effective also by intravenous route. The inhibitory effect of IGN-2098 on histamine-induced gastric secretion was not affected by the repeated administration of IGN-2098 (1 mg/kg b.i.d. for 14 days). These results show that IGN-2098 is a potent and long acting antisecretory agent and is a useful antisecretory drug for the treatment of peptic ulcer disease.
研究了新型组胺H2拮抗剂IGN - 2098（5,6 - 二甲基 - 2 - [4 - [3 - (1 - 哌啶甲基)苯氧基] - (Z) - 2 - 丁烯基氨基] - 4(1H) - 嘧啶酮二盐酸盐，CAS 126869 - 04 - 3）对海登海因小胃犬组胺诱导胃酸分泌的影响，并与法莫替丁、罗沙替丁醋酸酯盐酸盐和西咪替丁进行了比较。口服给予IGN - 2098（0.03 - 1.0 mg/kg）、法莫替丁（0.01 - 0.3 mg/kg）、罗沙替丁醋酸酯盐酸盐（0.1 - 1.0 mg/kg）和西咪替丁（0.3 - 3.0 mg/kg）对组胺诱导的胃酸分泌均呈现剂量依赖性抑制，IGN - 2098、法莫替丁、罗沙替丁醋酸酯盐酸盐和西咪替丁的ED50值分别为0.077、0.024、0.200和0.585 mg/kg。IGN - 2098在给药后6小时仍有效，ED50值为0.315 mg/kg。IGN - 2098静脉给药也有效。重复给予IGN - 2098（1 mg/kg，每日两次，共14天）不影响其对组胺诱导胃酸分泌的抑制作用。这些结果表明，IGN - 2098是一种强效且长效的抗分泌剂，是治疗消化性溃疡疾病的有用抗分泌药物。
