Document Detail

Adenosine A1 receptor antagonists in clinical research and development.
MedLine Citation:
PMID:  20592713     Owner:  NLM     Status:  MEDLINE    
Selective adenosine A1 receptor antagonists targeting renal microcirculation are novel pharmacologic agents that are currently under development for the treatment of acute heart failure as well as for chronic heart failure. Despite several studies showing improvement of renal function and/or increased diuresis with adenosine A1 antagonists, particularly in chronic heart failure, these findings were not confirmed in a large phase III trial in acute heart failure patients. However, lessons can be learned from these and other studies, and there might still be a potential role for the clinical use of adenosine A1 antagonists.We review the role of adenosine A1 receptors in the regulation of renal function, and emerging data regarding the safety and efficacy of A1 adenosine receptor antagonists based on all available completed and reported clinical trials using A1 adenosine receptor antagonists. The majority of trials were done in heart failure patients. However, there is clear clinical evidence for a role of this new class in hepatorenal syndrome, hypotension on dialysis, and radiocontrast media-induced nephropathy.
Berthold Hocher
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Publication Detail:
Type:  Journal Article; Review     Date:  2010-06-30
Journal Detail:
Title:  Kidney international     Volume:  78     ISSN:  1523-1755     ISO Abbreviation:  Kidney Int.     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-08-13     Completed Date:  2010-11-22     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0323470     Medline TA:  Kidney Int     Country:  United States    
Other Details:
Languages:  eng     Pagination:  438-45     Citation Subset:  IM    
Institute of Nutritional Science, University of Potsdam, Potsdam, Germany.
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MeSH Terms
Adenosine / physiology
Adenosine A1 Receptor Antagonists / therapeutic use*
Clinical Trials as Topic
Diuretics / therapeutic use
Drug Resistance
Heart Failure / drug therapy*
Kidney / physiopathology
Kidney Failure, Chronic / physiopathology
Liver Cirrhosis / physiopathology
Receptor, Adenosine A1 / physiology
Reg. No./Substance:
0/Adenosine A1 Receptor Antagonists; 0/Diuretics; 0/Receptor, Adenosine A1; 58-61-7/Adenosine

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