| The group at C2 of N-ethylnicotinamide determines the vasodilator potencies and mechanisms of action of nicorandil and its congeners in canine coronary arteries. | |
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MedLine Citation:
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PMID: 1839805 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The relaxant mechanisms of action of nicorandil and its congeners (SG-86, SG-103, SG-209 and SG-212) on large coronary arteries were investigated in isolated canine circumflex arteries contracted with 25 mmol/l KCl or 10(-7) mol/l U46619, a thromboxane A2 analogue. SG-212, SG-86, SG-209 and SG-103 were obtained by replacement of the nitroxy group of nicorandil by bromine, the hydroxy, acetoxy and nicotinoyloxy groups, respectively. Nicorandil (10(-6)-10(-3) mol/l), SG-212 (3 x 10(-4)-10(-2) mol/l), SG-209 (10(-4)-10(-2) mol/l), SG-103 (3 x 10(-4)-10(-2) mol/l), and SG-86 (10(-3)-10(-2) mol/l) all produced a concentration-dependent relaxation in KCl- or U46619-contracted arteries. The order of relaxant potency was as follows: Nicorandil much greater than SG-209 greater than SG-212 = SG-103 greater than SG-86. The relaxant effect of nicorandil was not affected by glibenclamide but antagonized by methylene blue. In the presence of glibenclamide, the concentration-relaxation curves for SG-209 underwent rightward parallel shifts. The relaxant effect of SG-209, however, was not affected by methylene blue. The concentration-relaxation curves for SG-212 underwent rightward parallel shifts only to a limited extent in the presence of glibenclamide, but they were not affected by methylene blue. The relaxant effect of SG-103 was affected by neither glibenclamide or methylene blue. The relaxant effect of SG-86 was not affected by glibenclamide. The relaxant effect of nicorandil accompanied an increase in cyclic-GMP levels but that of SG-209 did not.(ABSTRACT TRUNCATED AT 250 WORDS) |
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Authors:
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K Satoh; H Yamada; F Yoneyama; N Taira |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Naunyn-Schmiedeberg's archives of pharmacology Volume: 344 ISSN: 0028-1298 ISO Abbreviation: Naunyn Schmiedebergs Arch. Pharmacol. Publication Date: 1991 Nov |
Date Detail:
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Created Date: 1992-06-03 Completed Date: 1992-06-03 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0326264 Medline TA: Naunyn Schmiedebergs Arch Pharmacol Country: GERMANY |
Other Details:
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Languages: eng Pagination: 589-95 Citation Subset: IM |
Affiliation:
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Department of Pharmacology, Tohoku University School of Medicine, Sendai, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid Animals Coronary Vessels / drug effects* Dogs Female Male Niacinamide / analogs & derivatives*, pharmacology Nicorandil Potassium Chloride / antagonists & inhibitors Prostaglandin Endoperoxides, Synthetic / antagonists & inhibitors Vasodilation / drug effects* Vasodilator Agents / pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/Prostaglandin Endoperoxides, Synthetic; 0/Vasodilator Agents; 4314-66-3/N-ethylnicotinamide; 65141-46-0/Nicorandil; 7447-40-7/Potassium Chloride; 76898-47-0/15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid; 98-92-0/Niacinamide |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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