Chiu P J, Barnett A, Tetzloff G, Kaminski J
Arch Int Pharmacodyn Ther. 1984 Jul;270(1):116-27.
This report describes the gastric antisecretory properties of SCH 32651 (3-amino-2-methyl-8-phenylmethoxyimidazo[1,2-a] pyrazine HCl . 1/3 H2O). In the pyloric ligated rat, SCH 32651 inhibited gastric acid secretion; the oral ID50 (95% confidence limits) was 23.7 (13.8-39.2) mg/kg. In Heidenhain pouch dogs, SCH 32651 antagonized histamine-stimulated acid secretion with an ID50 of 1.44 (0.55-3.91) mg/kg p.o. SCH 32651 was also active against secretory responses to dimaprit, pentagastrin and feeding in dogs. In all test models SCH 32651 showed similar potency to cimetidine. Chronic administration of SCH 32651 or cimetidine caused slight tolerance and its antisecretory effect was readily reversible on cessation of dosing. The data indicate that SCH 32651 is an orally effective novel antisecretory drug.
本报告描述了SCH 32651(3-氨基-2-甲基-8-苄氧基咪唑并[1,2-a]吡嗪盐酸盐·1/3水合物)的胃抗分泌特性。在幽门结扎大鼠中,SCH 32651抑制胃酸分泌;口服半数抑制剂量(ID50,95%置信限)为23.7(13.8 - 39.2)mg/kg。在海登海因小胃犬中,SCH 32651拮抗组胺刺激的胃酸分泌,口服ID50为1.44(0.55 - 3.91)mg/kg。SCH 32651对犬体内地马普明、五肽胃泌素和进食引起的分泌反应也有活性。在所有测试模型中,SCH 32651显示出与西咪替丁相似的效力。长期给予SCH 32651或西咪替丁会引起轻微耐受性,且停药后其抗分泌作用可迅速逆转。数据表明,SCH 32651是一种口服有效的新型抗分泌药物。