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Myofibrillar Ca++ activation and heart failure--Ca++ sensitization by the cardiotonic agent APP 201-533.

Abstract
Certain forms of cardiac failure appear to be associated with a decrease in the Ca++ sensitivity of the contractile structures, possibly due to troponin I phosphorylation. Interference of cardiotonic drugs with myofibrillar Ca++ activation instead of enhancement of Ca++ influx may therefore provide a more causal therapeutic concept in the treatment of cardiac insufficiency. APP 201-533 (3-Amino-6-methyl-5-phenyl-2(1H)-pyridinone) (the structure of which is shown below) is a novel cardiotonic agent acting neither via beta adrenoceptor stimulation nor inhibition of Na+/K+ ATPase. In the 100 microM concentration range, it increases the Ca++ sensitivity and the Ca++ affinity of functionally isolated cardiac contractile structures. This coincides with an inhibitory effect on the cAMP-dependent protein kinase from rat liver. A possible relation with the regulation of troponin I phosphorylation is discussed.
AuthorsJ W Herzig, L H Botelho, R J Solaro
JournalBasic research in cardiology (Basic Res Cardiol) Vol. 84 Suppl 1 Pg. 117-24 ( 1989) ISSN: 0300-8428 [Print] Germany
PMID2818453 (Publication Type: Journal Article)
Chemical References
  • Cardiotonic Agents
  • Pyridones
  • 3-amino-6-methyl-5-phenyl-2(1H)-pyridinone
  • Protein Kinases
  • Calcium
Topics
  • Animals
  • Calcium (metabolism)
  • Cardiotonic Agents (pharmacology)
  • Dogs
  • Heart Failure (metabolism)
  • In Vitro Techniques
  • Liver (enzymology)
  • Myocardial Contraction (drug effects)
  • Myofibrils (metabolism)
  • Protein Kinases (analysis)
  • Pyridones (pharmacology)
  • Rats

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