| Centrally mediated inhibitory effect of 5-[2-(diethylamino)ethyl]amino-5,11-dihydro[1]benzoxepino[3,4- b]pyridine trihydrochloride (KW-5805) on gastric acid secretion in rats. | |
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MedLine Citation:
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PMID: 2313937 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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KW-5805, 5-[2-(diethylamino)ethyl]amino-5,11-dihydro[1]benzoxepino[3,4- b]pyridine trihydrochloride, is a new tricyclic compound with antiulcer activities. Its effect on stimulated gastric acid secretion was investigated in the perfused stomach of anesthetized rats. KW-5805 at 0.3-10 mg/kg, i.v., dose-dependently inhibited gastric acid secretion stimulated by 2-deoxy-D-glucose (2-DG). On the other hand, the compound at 10-20 mg/kg, i.v., exerted a moderate decrease in gastric acid secretion stimulated by bethanechol; and at 10 mg/kg, i.v., it produced no change in gastric acid secretion evoked peripherally by vagal electrical stimulation. When applied intracerebroventricularly at 1-5 micrograms/rat, this compound dose-relatedly reduced gastric acid secretion stimulated by 2-DG. Three main metabolites (KF-10504, KF-9530 and KF-10847) of KW-5805 at 1 mg/kg, i.v., caused no significant decrease in gastric acid secretion stimulated by 2-DG. Doxepin, a tricyclic compound, definitely depressed the 2-DG stimulated gastric acid secretion at 1 mg/kg, i.v. It is suggested that intravenous administration of KW-5805 inhibits gastric acid secretion stimulated by 2-DG, mainly via centrally mediated mechanisms, and that biotransformation of KW-5805 to the metabolites contributes little to the development of the antisecretory effect. |
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Authors:
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S Yano; Y Kimura; S Horie; K Ito; N Yamada; M Mizuno; K Watanabe |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Japanese journal of pharmacology Volume: 52 ISSN: 0021-5198 ISO Abbreviation: Jpn. J. Pharmacol. Publication Date: 1990 Feb |
Date Detail:
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Created Date: 1990-04-26 Completed Date: 1990-04-26 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 2983305R Medline TA: Jpn J Pharmacol Country: JAPAN |
Other Details:
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Languages: eng Pagination: 287-93 Citation Subset: IM |
Affiliation:
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Department of Drug Evaluation and Toxicological Sciences, Faculty of Pharmaceutical Sciences, Chiba University, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anti-Ulcer Agents / pharmacology* Benzoxepins / pharmacology* Bethanechol Compounds / pharmacology Brain / drug effects*, physiology Deoxyglucose / pharmacology Doxepin / pharmacology Electric Stimulation Gastric Acid / secretion* Injections, Intraventricular Male Rats Rats, Inbred Strains Vagus Nerve / physiology |
| Chemical | |
Reg. No./Substance:
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0/Anti-Ulcer Agents; 0/Benzoxepins; 0/Bethanechol Compounds; 113302-01-5/KW 5805; 154-17-6/Deoxyglucose; 1668-19-5/Doxepin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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