BCH-2763, a novel potent parenteral thrombin inhibitor, is an effective antithrombotic agent in rodent models of arterial and venous thrombosis--comparisons with heparin, r-hirudin, hirulog, inogatran and argatroban - PubMed
This site needs JavaScript to work properly. Please enable it to take advantage of the complete set of features!
Clipboard, Search History, and several other advanced features are temporarily unavailable.
Skip to main page content
An official website of the United States government
Here's how you know
The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before
sharing sensitive information, make sure you’re on a federal
government site.
The site is secure.
The https:// ensures that you are connecting to the
official website and that any information you provide is encrypted
and transmitted securely.
Log in
Show account info
Close
Account
Logged in as:
username
Dashboard
Publications
Account settings
Log out
Access keys
NCBI Homepage
MyNCBI Homepage
Main Content
Main Navigation
Search:
Search
Advanced
Clipboard
User Guide
Save
Email
Send to
Clipboard
My Bibliography
Collections
Citation manager
Display options
Display options
Format
Abstract
PubMed
PMID
Save citation to file
Format:
Summary (text)
PubMed
PMID
Abstract (text)
CSV
Create file
Cancel
Email citation
Email address has not been verified. Go to
My NCBI account settings
to confirm your email and then refresh this page.
To:
Subject:
Body:
Format:
Summary
Summary (text)
Abstract
Abstract (text)
MeSH and other data
Send email
Cancel
Add to Collections
Create a new collection
Add to an existing collection
Name your collection:
Name must be less than 100 characters
Choose a collection:
Unable to load your collection due to an error
Please try again
Add
Cancel
Add to My Bibliography
My Bibliography
Unable to load your delegates due to an error
Please try again
Add
Cancel
Your saved search
Name of saved search:
Search terms:
Test search terms
Would you like email updates of new search results?
Saved Search Alert Radio Buttons
Yes
No
Email:
(change)
Frequency:
Monthly
Weekly
Daily
Which day?
The first Sunday
The first Monday
The first Tuesday
The first Wednesday
The first Thursday
The first Friday
The first Saturday
The first day
The first weekday
Which day?
Sunday
Monday
Tuesday
Wednesday
Thursday
Friday
Saturday
Report format:
Summary
Summary (text)
Abstract
Abstract (text)
PubMed
Send at most:
1 item
5 items
10 items
20 items
50 items
100 items
200 items
Send even when there aren't any new results
Optional text in email:
Save
Cancel
Create a file for external citation management software
Create file
Cancel
Your RSS Feed
Name of RSS Feed:
Number of items displayed:
5
10
15
20
50
100
Create RSS
Cancel
RSS Link
Copy
Actions
Cite
Collections
Add to Collections
Create a new collection
Add to an existing collection
Name your collection:
Name must be less than 100 characters
Choose a collection:
Unable to load your collection due to an error
Please try again
Add
Cancel
Permalink
Permalink
Copy
Display options
Display options
Format
AbstractPubMedPMID
Page navigation
Title & authors
Abstract
Publication types
MeSH terms
Substances
LinkOut - more resources
Title & authors
Abstract
Publication types
MeSH terms
Substances
LinkOut - more resources
Comparative Study
Thromb Haemost
Actions
Search in PubMed
Search in NLM Catalog
Add to Search
. 1998 Feb;79(2):431-8.
BCH-2763, a novel potent parenteral thrombin inhibitor, is an effective antithrombotic agent in rodent models of arterial and venous thrombosis--comparisons with heparin, r-hirudin, hirulog, inogatran and argatroban
C D Finkle 
1
, A St Pierre, L Leblond, I Deschenes, J DiMaio, P D Winocour
Affiliations
Expand
Affiliation
1 BioChem Therapeutic Inc., Laval, Quebec, Canada.
PMID:
9493603
Item in Clipboard
Comparative Study
BCH-2763, a novel potent parenteral thrombin inhibitor, is an effective antithrombotic agent in rodent models of arterial and venous thrombosis--comparisons with heparin, r-hirudin, hirulog, inogatran and argatroban
C D Finkle et al.
Thromb Haemost.
1998 Feb.
Show details
Display options
Display options
Format
Abstract
PubMed
PMID
Thromb Haemost
Actions
Search in PubMed
Search in NLM Catalog
Add to Search
. 1998 Feb;79(2):431-8.
Authors
C D Finkle 
1
, A St Pierre, L Leblond, I Deschenes, J DiMaio, P D Winocour
Affiliation
1 BioChem Therapeutic Inc., Laval, Quebec, Canada.
PMID:
9493603
Item in Clipboard
Cite
Display options
Display options
Format
AbstractPubMedPMID
Abstract
Current clinical use of heparin as an antithrombotic agent is limited by suboptimal efficacy and safety considerations. Thrombin's central role in thrombosis makes it an attractive target to develop more effective and safer antithrombotic agents. BCH-2763 is a novel, potent (Ki: 0.11 nM), low molecular weight (1.51 kDa), bivalent direct thrombin inhibitor. The antithrombotic efficacy of BCH-2763 in vivo following i.v. bolus plus infusion in rats was compared in arterial and venous thrombosis models with two other bivalent direct thrombin inhibitors, r-hirudin and hirulog, with two catalytic site-directed thrombin inhibitors, inogatran and argatroban, and with heparin. In vivo efficacy was related to inhibition in vitro of fibrin clot formation, thrombin-induced aggregation of rat or human washed platelets and activity of free and plasma clot-bound thrombin. All the direct thrombin inhibitors were effective on both arterial and venous thrombosis at markedly lower fold aPTT increases than heparin. The antithrombotic doses of all inhibitors against venous thrombosis were less than against arterial thrombosis. The rank order of potency based on doses (mg/kg/h) required for full efficacy against arterial thrombosis was BCH-2763 (1.2) > inogatran (1.5) > r-hirudin (1.8) > hirulog (3.3) > argatroban (> 3.0); heparin required a markedly higher dose (5.7). In venous thrombosis the doses required for full efficacy were substantially lower for the bivalent (BCH-2763: 0.12; r-hirudin: 0.12; hirulog: 0.18) than for the catalytic site-directed (inogatran: 0.48; argatroban: 0.90) thrombin inhibitors; the dose required for heparin was 0.19. All the direct thrombin inhibitors caused similar shifts in aPTT at doses required to inhibit arterial thrombosis, but BCH-2763 inhibited venous thrombosis at lower aPTT fold increases. In vivo antithrombotic efficacy of direct thrombin inhibitors correlated with their inhibitory activity in vitro against fibrin clot formation and platelet aggregation. In contrast to heparin, all the direct thrombin inhibitors inhibited plasma clot-bound thrombin, but the relative IC50s did not correlate with their antithrombotic efficacy. In summary, direct thrombin inhibitors are more effective than heparin in inhibiting arterial and venous thrombosis in rats with less aPTT increases. BCH-2763 is effective at lower doses than the other direct thrombin inhibitors and for venous thrombosis at a smaller aPTT increase. BCH-2763 may offer an improved therapeutic index in the treatment of thromboembolic complications over heparin and other direct thrombin inhibitors.
PubMed Disclaimer
Publication types
Comparative Study
Actions
Search in PubMed
Search in MeSH
Add to Search
MeSH terms
Animals
Actions
Search in PubMed
Search in MeSH
Add to Search
Anticoagulants / administration & dosage*
Actions
Search in PubMed
Search in MeSH
Add to Search
Arginine / analogs & derivatives
Actions
Search in PubMed
Search in MeSH
Add to Search
Arteries / pathology
Actions
Search in PubMed
Search in MeSH
Add to Search
Glycine / administration & dosage
Actions
Search in PubMed
Search in MeSH
Add to Search
Glycine / analogs & derivatives*
Actions
Search in PubMed
Search in MeSH
Add to Search
Heparin / administration & dosage*
Actions
Search in PubMed
Search in MeSH
Add to Search
Hirudins / administration & dosage
Actions
Search in PubMed
Search in MeSH
Add to Search
Hirudins / analogs & derivatives*
Actions
Search in PubMed
Search in MeSH
Add to Search
Humans
Actions
Search in PubMed
Search in MeSH
Add to Search
Infusions, Intravenous
Actions
Search in PubMed
Search in MeSH
Add to Search
Oligopeptides / administration & dosage*
Actions
Search in PubMed
Search in MeSH
Add to Search
Peptide Fragments / administration & dosage*
Actions
Search in PubMed
Search in MeSH
Add to Search
Pipecolic Acids / administration & dosage*
Actions
Search in PubMed
Search in MeSH
Add to Search
Piperidines / administration & dosage*
Actions
Search in PubMed
Search in MeSH
Add to Search
Rats
Actions
Search in PubMed
Search in MeSH
Add to Search
Rats, Sprague-Dawley
Actions
Search in PubMed
Search in MeSH
Add to Search
Recombinant Proteins / administration & dosage
Actions
Search in PubMed
Search in MeSH
Add to Search
Sulfonamides
Actions
Search in PubMed
Search in MeSH
Add to Search
Thrombin / antagonists & inhibitors*
Actions
Search in PubMed
Search in MeSH
Add to Search
Thrombosis / drug therapy*
Actions
Search in PubMed
Search in MeSH
Add to Search
Veins / pathology
Actions
Search in PubMed
Search in MeSH
Add to Search
Substances
Anticoagulants
Actions
Search in PubMed
Search in MeSH
Add to Search
CX 397
Actions
Search in PubMed
Search in MeSH
Add to Search
Hirudins
Actions
Search in PubMed
Search in MeSH
Add to Search
Oligopeptides
Actions
Search in PubMed
Search in MeSH
Add to Search
Peptide Fragments
Actions
Search in PubMed
Search in MeSH
Add to Search
Pipecolic Acids
Actions
Search in PubMed
Search in MeSH
Add to Search
Piperidines
Actions
Search in PubMed
Search in MeSH
Add to Search
Recombinant Proteins
Actions
Search in PubMed
Search in MeSH
Add to Search
Sulfonamides
Actions
Search in PubMed
Search in MeSH
Add to Search
BCH 2763
Actions
Search in PubMed
Search in MeSH
Add to Search
inogatran
Actions
Search in PubMed
Search in MeSH
Add to Search
Heparin
Actions
Search in PubMed
Search in MeSH
Add to Search
Arginine
Actions
Search in PubMed
Search in MeSH
Add to Search
Thrombin
Actions
Search in PubMed
Search in MeSH
Add to Search
argatroban
Actions
Search in PubMed
Search in MeSH
Add to Search
Glycine
Actions
Search in PubMed
Search in MeSH
Add to Search
bivalirudin
Actions
Search in PubMed
Search in MeSH
Add to Search
LinkOut - more resources
Other Literature Sources
The Lens - Patent Citations Database
Medical
MedlinePlus Health Information
[x]
Cite
Copy
Download .nbib
.nbib
Format:
AMA
APA
MLA
NLM
Send To
Clipboard
Email
Save
My Bibliography
Collections
Citation Manager
[x]
NCBI Literature Resources
MeSH
PMC
Bookshelf
Disclaimer
The PubMed wordmark and PubMed logo are registered trademarks of the U.S. Department of Health and Human Services (HHS). Unauthorized use of these marks is strictly prohibited.
Follow NCBI
Twitter
Facebook
LinkedIn
GitHub
Connect with NLM
Twitter
SM-Facebook
SM-Youtube
National Library of Medicine
8600 Rockville Pike
Bethesda, MD 20894
Web Policies
FOIA
HHS Vulnerability Disclosure
Help
Accessibility
Careers
NLM
NIH
HHS
USA.gov