| A novel chymase inhibitor, 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[,4-dioxo-1-phenyl-7-(2-pyridyloxy)]2-heptyl]acetamide (NK3201), suppressed intimal hyperplasia after balloon injury. | |
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MedLine Citation:
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PMID: 12538841 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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In this study, we investigated whether an orally active chymase inhibitor, 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-2-heptyl]acetamide (NK3201), prevents intimal hyperplasia in carotid arteries injured by a balloon catheter in dog. Each dog was administered NK3201 (1 mg/kg per day, p.o.) or placebo beginning 5 days before balloon injury and continuing through the experiments. Four weeks after balloon injury, NK3201 did not affect the plasma renin and angiotensin-converting enzyme activities. The chymase activity was significantly increased in the injured arteries, whereas the angiotensin-converting enzyme activity was not. NK3201 significantly reduced the chymase activity in the injured arteries. The intimal area in the placebo- and NK3201-treated group and was 0.46 +/- 0.06 and 0.24 +/- 0.04 mm2, respectively, and this difference was significant. In this study, we demonstrated for the first time that a chymase inhibitor prevented the development of intimal hyperplasia in the balloon-injured arteries. |
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Authors:
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Shinji Takai; Hiroshi Sakonjo; Kohzo Fukuda; Denan Jin; Masato Sakaguchi; Keiichi Kamoshita; Koichi Ishida; Yoshikazu Sukenaga; Mizuo Miyazaki |
Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: The Journal of pharmacology and experimental therapeutics Volume: 304 ISSN: 0022-3565 ISO Abbreviation: J. Pharmacol. Exp. Ther. Publication Date: 2003 Feb |
Date Detail:
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Created Date: 2003-01-22 Completed Date: 2003-03-03 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0376362 Medline TA: J Pharmacol Exp Ther Country: United States |
Other Details:
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Languages: eng Pagination: 841-4 Citation Subset: IM |
Affiliation:
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Department of Pharmacology, Osaka Medical College, Takatsuki City, Osaka, Japan. pha010@art.osaka-med.ac.jp |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Acetamides
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pharmacology*,
therapeutic use Animals Balloon Dilatation / adverse effects* Carotid Artery, Common / drug effects*, enzymology, pathology* Chymases Dogs Hyperplasia Pyrimidines / pharmacology*, therapeutic use Serine Endopeptidases / metabolism* Serine Proteinase Inhibitors / pharmacology*, therapeutic use Tunica Intima / drug effects*, enzymology, injuries, pathology* |
| Chemical | |
Reg. No./Substance:
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0/Acetamides; 0/NK3201; 0/Pyrimidines; 0/Serine Proteinase Inhibitors; EC 3.4.21.-/Serine Endopeptidases; EC 3.4.21.39/Chymases |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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