| Fendiline inhibits L-type calcium channels in guinea-pig ventricular myocytes: a whole-cell patch-clamp study. | |
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MedLine Citation:
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PMID: 8485628 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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O Tripathi; W Schreibmayer; H A Tritthart |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: British journal of pharmacology Volume: 108 ISSN: 0007-1188 ISO Abbreviation: Br. J. Pharmacol. Publication Date: 1993 Apr |
Date Detail:
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Created Date: 1993-06-04 Completed Date: 1993-06-04 Revised Date: 2009-11-18 |
Medline Journal Info:
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Nlm Unique ID: 7502536 Medline TA: Br J Pharmacol Country: ENGLAND |
Other Details:
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Languages: eng Pagination: 865-9 Citation Subset: IM |
Affiliation:
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Institute of Medical Physics and Biophysics, Karl-Franzens University, School of Medicine, Graz, Austria. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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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:
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0/Calcium Channel Blockers; 0/Culture Media; 13042-18-7/Fendiline; 4368-28-9/Tetrodotoxin; 62-49-7/Choline; 7683-59-2/Isoproterenol |
| Comments/Corrections | |
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