| A caffeine analogue (1,3,7-trimethyl-6-thioxo-2-oxopurine) with a negative inotropic and chronotropic effect. | |
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MedLine Citation:
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PMID: 2997629 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Cardiac effects of thio-xanthine derivatives, S-caffeine and S-theophylline, were studied on isolated guinea-pig atria and on partially purified cardiac cAMP phosphodiesterase enzymes. Theophylline and caffeine were taken as reference compounds. On electrically driven left atria S-caffeine (0.01-1 mmol/l) decreased contractile tension in a concentration dependent manner. On spontaneously beating atria, the same concentrations of S-caffeine showed negative inotropic as well as negative chronotropic effects. On electrically driven left atria, S-theophylline (0.01-1 mmol/l) increased heart contractile tension but, at higher concentrations, a reversal of the stimulating effect was observed. Both S-caffeine and S-theophylline inhibited bovine heart cAMP phosphodiesterase activity to a comparable extent. Their inhibitory potencies were about three and nine times higher than those of theophylline or caffeine but consistently lower than that of IBMX. The results show that the replacement of O with S in the methylxanthine molecule drastically modifies the effects induced by the drugs on cardiac function without changing those on cAMP phosphodiesterase. |
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Authors:
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G Fassina; R M Gaion; L Caparrotta; F Carpenedo |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Naunyn-Schmiedeberg's archives of pharmacology Volume: 330 ISSN: 0028-1298 ISO Abbreviation: Naunyn Schmiedebergs Arch. Pharmacol. Publication Date: 1985 Sep |
Date Detail:
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Created Date: 1985-12-19 Completed Date: 1985-12-19 Revised Date: 2007-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0326264 Medline TA: Naunyn Schmiedebergs Arch Pharmacol Country: GERMANY, WEST |
Other Details:
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Languages: eng Pagination: 222-6 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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3',5'-Cyclic-AMP Phosphodiesterases
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metabolism Animals Caffeine / analogs & derivatives*, pharmacology Depression, Chemical Female Guinea Pigs Heart Rate / drug effects* Male Muscle Proteins / metabolism Myocardial Contraction / drug effects* Myocardium / enzymology Phosphoric Diester Hydrolases / metabolism Theophylline / pharmacology Xanthines / pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Muscle Proteins; 0/Xanthines; 13182-58-6/6-thiocaffeine; 58-08-2/Caffeine; 58-55-9/Theophylline; EC 3.1.4.-/Phosphoric Diester Hydrolases; EC 3.1.4.17/3',5'-Cyclic-AMP Phosphodiesterases |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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