Document Detail

Water-soluble renin inhibitors: design of a subnanomolar inhibitor with a prolonged duration of action.
MedLine Citation:
PMID:  2194033     Owner:  NLM     Status:  MEDLINE    
Incorporation of nonreactive polar functionalities at the C- and N-termini of renin inhibitors led to the development of a subnanomolar compound (21) with millimolar solubility. This inhibitor demonstrated excellent efficacy and a long duration of action upon intravenous administration to monkeys. While activity was also observed intraduodenally, a comparison of the blood pressure responses indicated low bioavailability. Subsequent experiments in rats showed that, although the compound was absorbed from the gastrointestinal tract, extensive liver extraction severely limited bioavailability.
S H Rosenberg; K W Woods; H L Sham; H D Kleinert; D L Martin; H Stein; J Cohen; D A Egan; B Bopp; I Merits
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  33     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  1990 Jul 
Date Detail:
Created Date:  1990-08-06     Completed Date:  1990-08-06     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1962-9     Citation Subset:  IM    
Abbott Laboratories, Cardiovascular Research Division, Abbott Park, Illinois 60064.
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MeSH Terms
Biological Availability
Blood Pressure / drug effects*
Drug Design
Enzyme Inhibitors / chemical synthesis*,  pharmacokinetics,  pharmacology
Indicators and Reagents
Macaca fascicularis
Oligopeptides / chemical synthesis*,  pharmacokinetics,  pharmacology
Rats, Inbred Strains
Renin / antagonists & inhibitors*
Structure-Activity Relationship
Tissue Distribution
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Indicators and Reagents; 0/Oligopeptides; EC

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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