Document Detail


A comparison of some of the pharmacological properties of etintidine, a new histamine H2-receptor antagonist, with those of cimetidine, ranitidine and tiotidine.
MedLine Citation:
PMID:  6129316     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Etintidine is a competitive antagonist of histamine H2-receptors in the isolated spontaneously beating guinea-pig right atrium with a pA2 value of 6.6 relative to values of 6.2, 6.7 and 7.3 for cimetidine, ranitidine and tiotidine, respectively. Low affinities for histamine H1 (pA2 = 4.2), cholinergic (pA2 = 4.4) and beta adrenergic (pA2 = 3.8) receptors indicated that etintidine has a high degree of specificity for the H2-receptor. The other antagonists studied also exhibited low affinities for these receptors; however, relative to these compounds, etintidine demonstrated a somewhat greater affinity for cholinergic receptors. Etintidine also antagonized basal gastric acid secretion in the conscious gastric fistula rat and histamine, pentagastrin, carbachol, 2-deoxy-D-glucose and meal-stimulated gastric acid secretion in conscious gastric fistula and Heidenhain pouch dogs. After oral administration to conscious Heidenhain pouch dogs, ED50 values for the inhibition of near maximal gastric acid secretion stimulated by histamine were 7.1, 5.4, 0.74 and 0.69 mumol/kg for cimetidine, etintidine, ranitidine and tiotidine, respectively. Onset and duration of the gastric antisecretory activities of the four compounds were similar. The order of potency as histamine H2-receptor and gastric antisecretory antagonists was cimetidine less than etintidine less than ranitidine less than tiotidine. Based on the high degree of specificity for the H2-receptor and its potent gastric antisecretory activity, etintidine may prove to be a useful agent in the treatment of peptic ulcer disease.
Authors:
R L Cavanagh; J J Usakewicz; J P Buyniski
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Publication Detail:
Type:  Comparative Study; In Vitro; Journal Article    
Journal Detail:
Title:  The Journal of pharmacology and experimental therapeutics     Volume:  224     ISSN:  0022-3565     ISO Abbreviation:  J. Pharmacol. Exp. Ther.     Publication Date:  1983 Jan 
Date Detail:
Created Date:  1983-02-14     Completed Date:  1983-02-14     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0376362     Medline TA:  J Pharmacol Exp Ther     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  171-9     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Adrenergic beta-Antagonists
Animals
Cimetidine / pharmacology
Dogs
Female
Furans / pharmacology
Gastric Juice / secretion
Guanidines / pharmacology
Guinea Pigs
Heart Rate / drug effects
Histamine H1 Antagonists
Histamine H2 Antagonists / pharmacology*
Imidazoles / pharmacology*
Male
Myocardial Contraction / drug effects
Parasympatholytics
Ranitidine
Rats
Rats, Inbred Strains
Thiazoles / pharmacology
Uterine Contraction / drug effects
Chemical
Reg. No./Substance:
0/Adrenergic beta-Antagonists; 0/Furans; 0/Guanidines; 0/Histamine H1 Antagonists; 0/Histamine H2 Antagonists; 0/Imidazoles; 0/Parasympatholytics; 0/Thiazoles; 51481-61-9/Cimetidine; 66357-35-5/Ranitidine; 69014-14-8/tiotidine; 69539-53-3/etintidine

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


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