Document Detail

Sivelestat relaxes vascular smooth muscle contraction in human gastric arteries.
MedLine Citation:
PMID:  21755354     Owner:  NLM     Status:  Publisher    
Sivelestat sodium hydrate (sivelestat) is a novel synthetic drug and specific inhibitor of neutrophil elastase that has been approved in Japan as a treatment for acute lung injury associated with systemic inflammatory response syndrome. It is important to determine how sivelestat affects hemodynamics and the regulatory mechanisms of vascular smooth muscle (VSM). We recently found that sivelestat relaxes porcine coronary artery VSM via selective inhibition of Ca(2+) sensitization induced by a receptor agonist without affecting the normal Ca(2+)-induced contraction. Although sivelestat relaxes porcine artery, its effects on human artery are unknown; therefore, the purpose of the present study was to assess the effects of sivelestat on human artery. In the present study, sivelestat induced concentration-dependent (1 × 10(-6) to 3 × 10(-4) M) vasorelaxation in U46619 (1 nM) and sphingosylphosphorylcholine (SPC) (30 mM)-precontracted human gastric artery with or without endothelium, but sivelestat did not induce vasorelaxation in conditions of high K(+) (40 mM) depolarization. Sivelestat inhibited VSM contraction by an agonist and SPC, and it did not affect Ca(2+)-induced normal physiologic contraction.
Hiroko Amemori; Yoshinori Maeda; Arisu Torikai; Mikio Nakashima
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-7-14
Journal Detail:
Title:  Journal of physiology and biochemistry     Volume:  -     ISSN:  1877-8755     ISO Abbreviation:  -     Publication Date:  2011 Jul 
Date Detail:
Created Date:  2011-7-14     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9812509     Medline TA:  J Physiol Biochem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Department of Anesthesiology and Critical Care Medicine, Saga Medical School, 5-1-1 Nabeshima, Saga, 849-8501, Japan,
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