Document Detail


Fendiline inhibits L-type calcium channels in guinea-pig ventricular myocytes: a whole-cell patch-clamp study.
MedLine Citation:
PMID:  8485628     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
1. Fendiline, a diphenylalkylamine type of antianginal drug, was examined for its effects on L-type calcium channels in guinea-pig ventricular myocytes by the whole-cell patch-clamp technique. 2. Fendiline (0.3-100 microM) applied extracellularly inhibited the calcium channel current (ICa) in a concentration- and time-dependent manner. The IC50 of fendiline was 17.0 +/- 2.43 microM and the Hill slope was 1.39 +/- 0.23. 3. Inhibition of ICa by fendiline appeared with an onset of less than 3 s. 4. Fendiline inhibited ICa at all the membrane potentials tested and shifted the current-voltage curve upwards. The overall calcium channel conductance (gCa) of the cell was reduced and conductance-voltage curve was shifted to the left in the presence of fendiline. 5. Isoprenaline (0.5-1 microM), a beta-adrenoceptor agonist, partially reversed the inhibitory effect of fendiline on ICa. 6. It is suggested that fendiline applied extracellularly blocks L-type calcium channels and reduces calcium channel conductance of the cell. The calcium channels thus inhibited are, nevertheless, still available for beta-adrenoceptor stimulation.
Authors:
O Tripathi; W Schreibmayer; H A Tritthart
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  British journal of pharmacology     Volume:  108     ISSN:  0007-1188     ISO Abbreviation:  Br. J. Pharmacol.     Publication Date:  1993 Apr 
Date Detail:
Created Date:  1993-06-04     Completed Date:  1993-06-04     Revised Date:  2009-11-18    
Medline Journal Info:
Nlm Unique ID:  7502536     Medline TA:  Br J Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  865-9     Citation Subset:  IM    
Affiliation:
Institute of Medical Physics and Biophysics, Karl-Franzens University, School of Medicine, Graz, Austria.
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MeSH Terms
Descriptor/Qualifier:
Animals
Calcium Channel Blockers / pharmacology*
Choline / pharmacology
Culture Media
Electrophysiology
Fendiline / pharmacology*
Guinea Pigs
Heart / drug effects
Isoproterenol / pharmacology
Membrane Potentials / drug effects
Myocardium / cytology,  metabolism*
Tetrodotoxin / pharmacology
Chemical
Reg. No./Substance:
0/Calcium Channel Blockers; 0/Culture Media; 13042-18-7/Fendiline; 4368-28-9/Tetrodotoxin; 62-49-7/Choline; 7683-59-2/Isoproterenol
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