Document Detail

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.
MedLine Citation:
PMID:  2313937     Owner:  NLM     Status:  MEDLINE    
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.
S Yano; Y Kimura; S Horie; K Ito; N Yamada; M Mizuno; K Watanabe
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Japanese journal of pharmacology     Volume:  52     ISSN:  0021-5198     ISO Abbreviation:  Jpn. J. Pharmacol.     Publication Date:  1990 Feb 
Date Detail:
Created Date:  1990-04-26     Completed Date:  1990-04-26     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  2983305R     Medline TA:  Jpn J Pharmacol     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  287-93     Citation Subset:  IM    
Department of Drug Evaluation and Toxicological Sciences, Faculty of Pharmaceutical Sciences, Chiba University, Japan.
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MeSH Terms
Anti-Ulcer Agents / pharmacology*
Benzoxepins / pharmacology*
Bethanechol Compounds / pharmacology
Brain / drug effects*,  physiology
Deoxyglucose / pharmacology
Doxepin / pharmacology
Electric Stimulation
Gastric Acid / secretion*
Injections, Intraventricular
Rats, Inbred Strains
Vagus Nerve / physiology
Reg. No./Substance:
0/Anti-Ulcer Agents; 0/Benzoxepins; 0/Bethanechol Compounds; 113302-01-5/KW 5805; 154-17-6/Deoxyglucose; 1668-19-5/Doxepin

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