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两种新型组胺H2受体拮抗剂的抗分泌作用

Antisecretory effects of two new histamine H2-receptor antagonists.

作者信息

Bickel M, Herling A W, Rising T J, Wirth K

出版信息

Arzneimittelforschung. 1986 Sep;36(9):1358-63.

PMID:2878669
Abstract

N-(3-[3-(1-Piperidinylmethyl)phenoxy]propyl)acetoxyaceta mide hydrochloride (Hoe 760) and N-(3-[3-(1-piperidinylmethyl)phenoxy]propyl)glycolamine hydrochloride (Hoe 062) are highly specific H2-receptor antagonists. The compounds are equipotent after intragastrical or intravenous administration. The antagonists inhibited gastric acid secretion in the rat induced by all stimuli tested, carbachol, desglugastrin and histamine. In the Heidenhain pouch dog whose gastric acid secretion was stimulated by food or histamine the two receptor blockers proved to be 4-6 times more potent inhibitors than cimetidine.

摘要

N-(3-[3-(1-哌啶基甲基)苯氧基]丙基)乙酰氧基乙酰胺盐酸盐(Hoe 760)和N-(3-[3-(1-哌啶基甲基)苯氧基]丙基)乙醇胺盐酸盐(Hoe 062)是高度特异性的H2受体拮抗剂。这些化合物经胃内或静脉给药后效价相当。这些拮抗剂抑制了所有测试刺激物(卡巴胆碱、去甘氨酰胃泌素和组胺)诱导的大鼠胃酸分泌。在由食物或组胺刺激胃酸分泌的海登海因小胃犬中,这两种受体阻滞剂被证明是比西咪替丁强4至6倍的抑制剂。

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