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非诺替明在大鼠和犬体内的抗分泌活性。

Antisecretory activity of fenoctimine in rat and dog.

作者信息

Jacoby H I, Bonfilio A C, Corcoran T, Lopez I, Scott M

出版信息

Dig Dis Sci. 1984 Dec;29(12):1131-6. doi: 10.1007/BF01317088.

Abstract

Fenoctimine (4-(diphenylmethyl)-1-[(octylimino)methyl]piperidine) sulfate was evaluated for gastric antisecretory activity in the acute gastric fistula rat and chronic gastric fistula dog. It showed potent gastric antisecretory activity of long duration in the rat, and was more potent on a mg/kg basis than cimetidine. In the dog, fenoctimine showed significant activity against gastrin tetrapeptide, histamine, and bethanechol. It was least potent against bethanechol, indicating a lack of significant anticholinergic activity in the dog at the doses tested. It had a long duration of action in the dog with doses of 6 mg/kg, showing significant activity even at 24 hr. Fenoctimine does not appear to fit the spectrum of activity associated with other known antisecretory agents and may have a unique mechanism of action related to effects directly on parietal cells.

摘要

对硫酸非诺替明(4-(二苯甲基)-1-[(辛基亚氨基)甲基]哌啶)在急性胃瘘大鼠和慢性胃瘘犬中进行了胃抗分泌活性评估。它在大鼠中显示出强效且作用持久的胃抗分泌活性,以毫克/千克计比西咪替丁更有效。在犬中,非诺替明对胃泌素四肽、组胺和氨甲酰甲胆碱显示出显著活性。它对氨甲酰甲胆碱的活性最低,表明在所测试剂量下犬中缺乏显著的抗胆碱能活性。在犬中,6毫克/千克剂量的非诺替明作用持续时间长,甚至在24小时时仍显示出显著活性。非诺替明似乎不符合与其他已知抗分泌剂相关的活性谱,可能具有与直接作用于壁细胞的效应相关的独特作用机制。

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