| Antimuscarinic action of an alkane-bis-ammonium compound alone and in combination with (+)-benzetimide. | |
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MedLine Citation:
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PMID: 1242377 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Heptane-1,7-bis-(dimethyl-3'-phthalimidopropylammonium bromide) ('C7/3-phthalimido-propyl') in concentrations of 10(-7) to 0.5 X 10(-3) inhibited negative inotropic responses to carbachol or acetylcholine to a similar extent in the electrically stimulated isolated guinea-pig left atrium. However, the degree of antagonism of responses to carbachol was less than expected for a competitive antagonist when the higher concentrations of 'C7/3-phthalimido-propyl' were employed. When 'C7/3-phthalimido-propyl' was combined with competitive antagonists such as (+)-benzetimide, atropine or homatropine the degree of antagonism was greater than expected for combination of 2 competitive antagonists. Qualitatively similar results were obtained in the presence of practolol (1.5 X 10(-5) M). The results obtained with 'C7/3-phthalimido-propyl' are shown to agree with theoretical predictions for a metaffinoid antagonist which influences the affinities of both agonists and competitive antagonists by combining with a regulatory site distinct from, but interdependent with the binding sites for agonists and competitive antagonists. Further, it is shown that the alkane-bis-ammonium compound produces a much greater reduction in the affinity of carbachol than that of the competitive antagonists and as a consequence causes 'supra-additive' effects when combined with a competitive antagonist. The reduction in the affinity of (+)-benzetimide produced by 'C7/3-phthalimido-propyl' did not differ significantly from the reduction in the affinities of atropine or homatropine. |
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Authors:
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F Mitchelson |
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Publication Detail:
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Type: In Vitro; Journal Article |
Journal Detail:
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Title: European journal of pharmacology Volume: 33 ISSN: 0014-2999 ISO Abbreviation: Eur. J. Pharmacol. Publication Date: 1975 Sep-Oct |
Date Detail:
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Created Date: 1976-01-26 Completed Date: 1976-01-26 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 1254354 Medline TA: Eur J Pharmacol Country: NETHERLANDS |
Other Details:
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Languages: eng Pagination: 237-46 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Acetylcholine
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pharmacology Animals Atropine / pharmacology Carbachol / pharmacology Dexetimide / pharmacology* Drug Interactions Electric Stimulation Guinea Pigs Heart Atria / drug effects Heart Rate / drug effects Mathematics Models, Biological Parasympatholytics / pharmacology* Phthalimides / pharmacology* Piperidines / pharmacology* Practolol / pharmacology Quaternary Ammonium Compounds / pharmacology* Tropanes / pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Parasympatholytics; 0/Phthalimides; 0/Piperidines; 0/Quaternary Ammonium Compounds; 0/Tropanes; 21888-98-2/Dexetimide; 51-55-8/Atropine; 51-83-2/Carbachol; 51-84-3/Acetylcholine; 6673-35-4/Practolol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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