| N,N-dimethyl-10-(3-quinuclidinyl)-2-phenothiazine sulfonamide (LM 24056): mode of action of its gastric antisecretory effect. | |
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MedLine Citation:
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PMID: 6140926 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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J Vatier; J F Bessac; S Bonfils |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Arzneimittel-Forschung Volume: 33 ISSN: 0004-4172 ISO Abbreviation: Arzneimittelforschung Publication Date: 1983 |
Date Detail:
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Created Date: 1984-02-14 Completed Date: 1984-02-14 Revised Date: 2003-11-14 |
Medline Journal Info:
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Nlm Unique ID: 0372660 Medline TA: Arzneimittelforschung Country: GERMANY, WEST |
Other Details:
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Languages: eng Pagination: 1573-6 Citation Subset: IM |
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* Bethanechol Bethanechol Compounds / pharmacology Depression, Chemical Dogs Gastric Juice / secretion* Gastric Mucosa / drug effects Gastrins / pharmacology Histamine / pharmacology Pepsin A / secretion Phenothiazines / pharmacology* |
| Chemical | |
Reg. No./Substance:
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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 3.4.23.1/Pepsin A |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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