Document Detail

Nafamostat mesilate is an extremely potent inhibitor of human tryptase.
MedLine Citation:
PMID:  12939527     Owner:  NLM     Status:  MEDLINE    
Previously, nafamostat mesilate was found to be a potent inhibitor of human tryptase. In present study, we performed a kinetic study to determine its K(i) value for tryptase and compared it with that of gabexate mesilate. Nafamostat mesilate inhibited human tryptase in a competitive manner. The apparent K(i) value was estimated to be 95.3 pM, which was 1000 times lower than that of gabexate mesilate (95.1 nM). These results strongly indicated that nafamostat mesilate is an extremely potent inhibitor of tryptase and suggested that some of its beneficial effects in the treatment of clinical status may be due to tryptase inhibition.
Shuji Mori; Yoshinori Itoh; Ryoko Shinohata; Toshiaki Sendo; Ryozo Oishi; Masahiro Nishibori
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Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of pharmacological sciences     Volume:  92     ISSN:  1347-8613     ISO Abbreviation:  J. Pharmacol. Sci.     Publication Date:  2003 Aug 
Date Detail:
Created Date:  2003-08-26     Completed Date:  2004-05-11     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  101167001     Medline TA:  J Pharmacol Sci     Country:  Japan    
Other Details:
Languages:  eng     Pagination:  420-3     Citation Subset:  IM    
Department of Pharmacology, Okayama University Graduate School of Medicine and Dentistry, Okayama, Japan.
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MeSH Terms
Binding, Competitive
Dose-Response Relationship, Drug
Gabexate / metabolism,  pharmacology
Guanidines / metabolism,  pharmacology*
Serine Endopeptidases / metabolism*
Serine Proteinase Inhibitors / metabolism,  pharmacology*
Reg. No./Substance:
0/Guanidines; 0/Serine Proteinase Inhibitors; 39492-01-8/Gabexate; 81525-10-2/nafamostat; EC 3.4.21.-/Serine Endopeptidases; EC

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