Document Detail

Highly selective synthetic inhibitors with regard to plasma-kallikrein activities.
MedLine Citation:
PMID:  2610076     Owner:  NLM     Status:  MEDLINE    
The synthetic inhibitors of plasma kallikrein (PK) were found, which are called PKSI-1007, PKSI-0180 and PKSI-0527 in our laboratories. (1) The inhibitors inhibited PK competitively with D-Pro-Phe-Arg-pNA and the Ki values obtained were considerably small, 10(-6) M-10(-7) M. However, the Ki values for glandular kallikrein (GK), plasmin (PL), thrombin (TH) and factor Xa (FXa) were larger. In particular, a selectivity of PKSI-0527 towards PK was very high and the toxicity was weak (i.v. LD50 for mice is over 100 mg/kg). (2) The inhibitors were effective (a) to prevent the bradykinin formation in the kaolin-activated human plasma and the acid-treated ascites taken from the mice bearing Sarcoma 180, (b) to prolong the coagulation time by contact activation, and (c) to inhibit the enhancement of ADP-platelet aggregation by PK. The results indicated that the some PKSI-inhibitors will be much useful for the basic studies, furthermore they deem to be even promising towards the clinical application.
S Okamoto; U Okamoto; K Wanaka; A Hijikata-Okunomiya; M Bohgaki; T Naito; N Horie; Y Okada
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Advances in experimental medicine and biology     Volume:  247B     ISSN:  0065-2598     ISO Abbreviation:  Adv. Exp. Med. Biol.     Publication Date:  1989  
Date Detail:
Created Date:  1990-02-09     Completed Date:  1990-02-09     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  0121103     Medline TA:  Adv Exp Med Biol     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  29-34     Citation Subset:  IM    
Kobe Research Projects on Thrombosis and Haemostasis, Saiseikai-Hospital, Japan.
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MeSH Terms
Amino Acid Sequence
Arginine / analogs & derivatives,  pharmacology
Bradykinin / biosynthesis
Kallikreins / antagonists & inhibitors,  blood*,  pharmacology*,  toxicity
Molecular Sequence Data
Platelet Aggregation Inhibitors / pharmacology
Sarcoma 180 / metabolism
Reg. No./Substance:
0/Platelet Aggregation Inhibitors; 123847-40-5/PKSI 1007; 58-82-2/Bradykinin; 74-79-3/Arginine; EC 3.4.21.-/Kallikreins

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