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新型促胃肠动力药莫沙必利代谢产物的合成及其生物活性

Synthesis and biological activities of metabolites of mosapride, a new gastroprokinetic agent.

作者信息

Kato S, Morie T, Yoshida N

机构信息

Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1995 Apr;43(4):699-702. doi: 10.1248/cpb.43.699.

DOI:10.1248/cpb.43.699
PMID:7600620
Abstract

In order to confirm the proposed structures of two metabolites 3 and 4 of the gastroprokinetic agent mosapride [4-amino-5-chloro-2-ethoxy-N-([4-(4-fluorobenzyl)-2-morpholinyl] methyl)benzamide, 2], the compounds were synthesized and their biological activity was examined. The structures of the metabolites were confirmed by means of comparison with the synthetic compounds. The serotonin 5-HT4 receptor agonistic activities of the metabolites were found to be less than that of mosapride.

摘要

为了确证促胃肠动力药莫沙必利[4-氨基-5-氯-2-乙氧基-N-([4-(4-氟苄基)-2-吗啉基]甲基)苯甲酰胺,2]的两种代谢产物3和4的推测结构,合成了这些化合物并检测了它们的生物活性。通过与合成化合物进行比较确证了代谢产物的结构。发现这些代谢产物的5-羟色胺5-HT4受体激动活性低于莫沙必利。

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Synthesis and biological activities of metabolites of mosapride, a new gastroprokinetic agent.新型促胃肠动力药莫沙必利代谢产物的合成及其生物活性
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Synthesis and biological activity of 4-amino-5-chloro-2-ethoxy-3-hydroxybenzamides, metabolites of a new gastroprokinetic agent, mosapride.新型促胃肠动力药莫沙必利的代谢产物4-氨基-5-氯-2-乙氧基-3-羟基苯甲酰胺的合成及生物活性
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Affinity of mosapride citrate, a new gastroprokinetic agent, for 5-HT4 receptors in guinea pig ileum.新型促胃肠动力药枸橼酸莫沙必利对豚鼠回肠5-HT4受体的亲和力。
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The synthesis and biological evaluation of a new bioactive metabolite of mosapride as a potential gastroprokinetic agent.莫沙必利生物活性代谢物的合成及生物学评价:一种新型胃动力药物。
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Novel benzamides as selective and potent gastrokinetic agents. 2. Synthesis and structure-activity relationships of 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2- morpholinyl]methyl] benzamide citrate (AS-4370) and related compounds.
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[Pharmacological effects of the gastroprokinetic agent mosapride citrate].[促胃肠动力药枸橼酸莫沙必利的药理作用]
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