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PMID: 2436062 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Quinidine inhibition of the muscarine receptor-activated K+ channel current in atrial cells of guinea pig.

Naunyn-Schmiedeberg's archives of pharmacology ·Vol. 335 ·No. 2 ·1987-02-00 ·Pages 216-8

Kurachi Y, Nakajima T, Sugimoto T

Abstract

Postsynaptic mechanisms underlying the anticholinergic effects of quinidine were examined in single atrial cells, using the tight-seal whole-cell recording technique. The solution in the glass pipettes contained guanosine-5'-triphosphate (GTP) or guanosine-5'-O-(3-thiotriphosphate) (GTP-gamma S, a non-hydrolyzable GTP analogue). In both cases, acetylcholine (ACh), applied to the bath, induced a specific K+ current. In GTP-loaded cells, quinidine in the bath solution depressed the ACh-induced K+ current concentration-dependently. Atropine also blocked the K+ current. On the other hand, in GTP-gamma S-loaded cells, the ACh-induced current was not blocked by atropine and persisted even when ACh was washed out from the bath, indicating that GTP-gamma S causes uncoupling of the K+ channels from the muscarine receptors. Quinidine, however, did depress the increased K+ current concentration-dependently. The percent inhibition curves for quinidine to depress the K+ current were very similar between GTP-loaded and GTP-gamma S-loaded cells. From these observations, we suggest that direct inhibition of the muscarine receptor-activated K+ channel current by quinidine, and not blockade of the muscarine receptor itself, is mainly responsible for the anticholinergic effects of the drug in atrial myocytes.

MeSH Terms
Acetylcholine/pharmacology Animals Atropine/pharmacology Guanosine 5'-O-(3-Thiotriphosphate) Guanosine Triphosphate/analogs & derivatives,pharmacology Guinea Pigs Heart/drug effects In Vitro Techniques Ion Channels/drug effects Myocardium/metabolism Quinidine/pharmacology Receptors, Muscarinic/drug effects Thionucleotides/pharmacology
Chemicals
Ion Channels Receptors, Muscarinic Thionucleotides Guanosine 5'-O-(3-Thiotriphosphate) Atropine Guanosine Triphosphate Quinidine Acetylcholine
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Kurachi Y
Nakajima T
Sugimoto T
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22 references, click to expand
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Article Info
Journal
Naunyn-Schmiedeberg's archives of pharmacology
Abbr.
Naunyn Schmiedebergs Arch Pharmacol
ISSN
0028-1298
Published
1987-02-00
Pages
216-8
Language
English
Region
Germany
NLM ID
0326264
Subset
IM
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