Document Detail


Antisecretory and antiulcer effect of T-330, a novel reversible proton pump inhibitor, in rats.
MedLine Citation:
PMID:  9085044     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The antisecretory and antiulcer effects of T-330 (2-[(2-dimethylaminobenzyl)sulfinyl]-1-(3-methylpyridine-2-yl)imidazole) , a novel reversible proton pump inhibitor, were studied in rats. T-330 suppressed dibutyryl cyclic AMP-stimulated acid formation in isolated rat gastric mucosal cells with the IC50 value of 0.57 microM. In chronic fistula rats, intravenous, intraduodenal and oral administration of T-330 inhibited pentagastrin-stimulated gastric acid secretion; the ED50 values calculated from the peak inhibition were 0.36, 0.43 and 0.73 mg/kg, respectively. T-330 also reduced dimaprit-stimulated gastric acid secretion following its intraduodenal injection (ED50 0.85 mg/kg). The antisecretory activities of T-330 following its intraduodenal and oral administration were 3-6- and 4-10-times more potent than those of omeprazole and ranitidine, respectively, while the duration of action of T-330 was apparently shorter than that of omeprazole and was almost equal to that of ranitidine. Oral or duodenal administration of T-330 inhibited the development of acid-related damage (water-immersion- and aspirin-induced gastric lesions, cysteamine-induced duodenal ulcers and reflux esophagitis) with equal or higher potency than omeprazole or ranitidine. Furthermore, T-330 prevented ethanol-induced gastric lesions. These findings indicate that T-330 exerts its antiulcer effect mainly via its potent antisecretory action and partly via its gastroprotective action.
Authors:
M Kinoshita; N Saito; H Tamaki
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  European journal of pharmacology     Volume:  321     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1997 Mar 
Date Detail:
Created Date:  1997-06-12     Completed Date:  1997-06-12     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  325-32     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, Tanabe Seiyaku Co., Ltd., Saitama, Japan.
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MeSH Terms
Descriptor/Qualifier:
Animals
Anti-Ulcer Agents / pharmacology*
Enzyme Inhibitors / pharmacology*
Esophagitis, Peptic / etiology,  physiopathology
Gastric Acid / secretion*
Gastric Fistula
Gastric Mucosa / secretion
H(+)-K(+)-Exchanging ATPase / antagonists & inhibitors*
Histamine H2 Antagonists / pharmacology
Imidazoles / pharmacology*
Male
Omeprazole / pharmacology
Peptic Ulcer / chemically induced,  physiopathology,  prevention & control
Pyridines / pharmacology*
Ranitidine / pharmacology
Rats
Rats, Sprague-Dawley
Chemical
Reg. No./Substance:
0/Anti-Ulcer Agents; 0/Enzyme Inhibitors; 0/Histamine H2 Antagonists; 0/Imidazoles; 0/Pyridines; 0/T 330; 66357-35-5/Ranitidine; 73590-58-6/Omeprazole; EC 3.6.1.10/H(+)-K(+)-Exchanging ATPase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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