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PMID: 6205402 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Dihydropyridine derivatives prolong the open state of Ca channels in cultured cardiac cells.

Proceedings of the National Academy of Sciences of the United States of America ·Vol. 81 ·No. 15 ·1984-08-00 ·Pages 4824-7

Kokubun S, Reuter H

Abstract

The dihydropyridine derivatives CGP 28392 and BAY K 8644 exert a strong positive inotropic effect in mammalian cardiac muscle, presumably by increasing Ca influx during the action potential. Analysis of the drug effects at the level of single Ca channels by means of the patch-clamp method revealed complicated changes in the kinetics of channel gating. The prevailing effect is a prolongation of the mean open time of Ca channels. In addition, the intervals between channel openings can be slightly prolonged. Ensemble averages of single-channel traces showed a concentration-dependent increase in the mean current amplitude by the drugs. In contrast to beta-adrenoceptor agonists, the increase in Ca current by the dihydropyridine derivatives is not associated with an increase in the intracellular cyclic AMP level.

MeSH Terms
3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester Animals Calcium Channel Blockers Cells, Cultured Heart/drug effects Ion Channels/drug effects Kinetics Nifedipine/analogs & derivatives,pharmacology Pyridines/pharmacology Rats
Chemicals
Calcium Channel Blockers Ion Channels Pyridines 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester CGP 28392 Nifedipine
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Kokubun S
Reuter H
References (14)
14 references, click to expand
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Article Info
Journal
Proceedings of the National Academy of Sciences of the United States of America
Abbr.
Proc Natl Acad Sci U S A
ISSN
0027-8424
DOI
10.1073/pnas.81.15.4824
Published
1984-08-00
Pages
4824-7
Language
English
Region
United States
NLM ID
7505876
PMCID
PMC391583
Subset
IM
External Links
PubMed source DOI: 10.1073/pnas.81.15.4824 PMC Full Text View journal details
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