Document Detail

Ca2+ channel activation by CGP 48506, a new positive inotropic benzodiazocine derivative.
MedLine Citation:
PMID:  8925868     Owner:  NLM     Status:  MEDLINE    
Effects on L-type Ca2+ channels of a new positive inotropic compound, the active (+)-enantiomer of the Ca2+ sensitizer 5-methyl-6-phenyl-1,3,5,6,-tetrahydro-3,6,-methano-1,5-benzodiazocine -2,4-dione (CGP 48506), were studied in guinea-pig cardiomyocytes. Whole-cell currents (physiological solutions, 2 mM Ca2+) were enhanced approximately 1.8-fold (10(-4) M, n = 7). Slowing of (de)activation kinetics became apparent under conditions where K+ currents were fully eliminated and Ca(2+)-dependent inactivation was minimized (n = 7). Single-channel current (70 mM Ba2+) and mean open time were increased approximately 2.5-fold (10(-4) M, n = 5), because the drug specifically enhanced sweeps containing long openings (mode 2). Therefore, CGP 48506 stimulates Ca2+ channels in a manner reminiscent of, but not identical to chemically distinct activators like Bay K 8644.
S Herzig
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  European journal of pharmacology     Volume:  295     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1996 Jan 
Date Detail:
Created Date:  1996-10-29     Completed Date:  1996-10-29     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  113-7     Citation Subset:  IM    
Department of Pharmacology, University of Kiel, Germany.
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MeSH Terms
Azocines / pharmacology*
Calcium / metabolism
Calcium Channels / drug effects*
Cardiotonic Agents / pharmacology*
Guinea Pigs
Heart / drug effects
Reg. No./Substance:
0/Azocines; 0/Calcium Channels; 0/Cardiotonic Agents; 166020-57-1/BA 41899; 7440-70-2/Calcium

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