| Dual actions of cilnidipine in human internal thoracic artery: Inhibition of calcium channels and enhancement of endothelial nitric oxide synthase. | |
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MedLine Citation:
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PMID: 20599230 Owner: NLM Status: In-Data-Review |
Abstract/OtherAbstract:
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OBJECTIVE: Cilnidipine is a novel, long-action L/N-type dihydropyridine calcium channel blocker that has recently been used for antihypertensive therapy. We investigated the vasorelaxation effect of cilnidipine with regard to its calcium channel blockage and nitric oxide-cyclic guanosine monophosphate-dependent mechanism in human internal thoracic artery. METHODS: Fresh human internal thoracic arteries taken from discarded tissues of patients undergoing coronary artery bypass surgery were studied. Concentration-relaxation curves for cilnidipine in comparison with nifedipine were studied. The expression level of endothelial nitric oxide synthase mRNA was assayed by quantitative real-time polymerase chain reaction, and the phosphorylation of endothelial nitric oxide synthase at Ser(1177) was determined by Western blotting analysis. RESULTS: Cilnidipine and nifedipine caused nearly full relaxation in potassium-precontracted internal thoracic artery. Pretreatment with cilnidipine at the clinical plasma concentration significantly depressed the maximal contraction. Endothelium denudation (47.7% ± 7.0%, P < .05) and inhibition of endothelial nitric oxide synthase (48.6% ± 6.1%, P < .05) or guanylate cyclase (41.6% ± 3.8%, P < .01) significantly reduced the cilnidipine-induced endothelium-dependent relaxation (73.9% ± 6.4%). Cilnidipine increased the expression of endothelial nitric oxide synthase mRNA by 42.4% (P < .05) and enhanced phosphorylation level of endothelial nitric oxide synthase at Ser(1177) by 37.0% (P < .05). CONCLUSIONS: The new generation of calcium channel antagonist cilnidipine relaxes human arteries through calcium channel antagonism and increases production of nitric oxide by enhancement of endothelial nitric oxide synthase. The dual mechanisms of cilnidipine in human arteries demonstrated in this study may prove particularly important in vasorelaxing therapy in cardiovascular diseases. |
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Authors:
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Li Fan; Qin Yang; Xiao-Qiu Xiao; Kevin L Grove; Yu Huang; Zhi-Wu Chen; Anthony Furnary; Guo-Wei He |
Publication Detail:
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Type: Journal Article Date: 2010-07-06 |
Journal Detail:
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Title: The Journal of thoracic and cardiovascular surgery Volume: 141 ISSN: 1097-685X ISO Abbreviation: J. Thorac. Cardiovasc. Surg. Publication Date: 2011 Apr |
Date Detail:
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Created Date: 2011-03-22 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0376343 Medline TA: J Thorac Cardiovasc Surg Country: United States |
Other Details:
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Languages: eng Pagination: 1063-9 Citation Subset: AIM; IM |
Copyright Information:
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Copyright © 2011 The American Association for Thoracic Surgery. Published by Mosby, Inc. All rights reserved. |
Affiliation:
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Cardiovascular Research, Starr Academic Center, Providence Heart and Vascular Institute, Department of Surgery, Oregon Health and Science University, Portland, Ore; Department of Pharmacology, Anhui Medical University, Hefei, Anhui, China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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