Document Detail

N,N-dimethyl-10-(3-quinuclidinyl)-2-phenothiazine sulfonamide (LM 24056): mode of action of its gastric antisecretory effect.
MedLine Citation:
PMID:  6140926     Owner:  NLM     Status:  MEDLINE    
The inhibitory effect on gastric secretion of a phenothiazine molecule, N,N-dimethyl-10-(3-quinuclidinyl)-2-phenothiazine sulfonamide (LM 24056), was studied in dogs equipped with gastric fistula (GF) and Heidenhain denervated pouch (HP). LM 24056 was infused intravenously before exogenous stimulations started: the gastric stimulation ws obtained either by gastrin, by combination of gastrin + bethanechol (subthreshold dose) or by histamine. 1. On gastrin-stimulated secretion, preliminary infusion of LM 24056 results in a weak and non-significant reduction on GF acid secretion, while on HP, the inhibition is significant with 1 and 2 micrograms x kg-1 x h-1 of gastrin. The LM 24056 concentrations which produced 50% inhibition (IC50) of acid secretion is close to 0.5 mg x min-1. 2. LM 24056 exerts a strong inhibitory effect on combination gastrin + bethanechol-stimulated acid and pepsin secretions on GH and HP. IC50 is close to 0.25 mg x min-1. 3. LM 24056 is able to delay the histamine-stimulated acid secretion. There are some differences in the gastric inhibitory effects in relation to the moment of LM 24056 administration regarding exogenous stimulant: LM 24056 seems to be able to compete gastrin and to delay the normal histamine stimulation. The most important inhibitory effect is exerted on combination gastrin + bethanechol. LM 24056 could act as an antigastrinic substance.
J Vatier; J F Bessac; S Bonfils
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Arzneimittel-Forschung     Volume:  33     ISSN:  0004-4172     ISO Abbreviation:  Arzneimittelforschung     Publication Date:  1983  
Date Detail:
Created Date:  1984-02-14     Completed Date:  1984-02-14     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  0372660     Medline TA:  Arzneimittelforschung     Country:  GERMANY, WEST    
Other Details:
Languages:  eng     Pagination:  1573-6     Citation Subset:  IM    
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MeSH Terms
Anti-Ulcer Agents / pharmacology*
Bethanechol Compounds / pharmacology
Depression, Chemical
Gastric Juice / secretion*
Gastric Mucosa / drug effects
Gastrins / pharmacology
Histamine / pharmacology
Pepsin A / secretion
Phenothiazines / pharmacology*
Reg. No./Substance:
0/Anti-Ulcer Agents; 0/Bethanechol Compounds; 0/Gastrins; 0/Phenothiazines; 51-45-6/Histamine; 64099-44-1/LM 24056; 674-38-4/Bethanechol; EC A

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