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PMID: 8388270 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S.

Procaine effects on single sarcoplasmic reticulum Ca2+ release channels.

Biophysical journal ·Vol. 64 ·No. 4 ·1993-04-00 ·Pages 991-1003

Zahradníková A, Palade P

Abstract

The effects of the Ca(2+)-induced Ca2+ release blocker procaine on individual sarcoplasmic reticulum Ca2+ release channels have been examined in planar lipid bilayers. Procaine did not reduce the single channel conductance nor appreciably shorten the mean open times of the channel; rather, it increased the longest closed time. These results indicated that procaine interacted selectively with a closed state of the channel rather than with an open state. Gating of the sarcoplasmic reticulum Ca2+ release channel was described by a modified scheme of Ashley and Williams (1990. J. Gen. Physiol. 95:981-1005), including an additional long-lived closed state. Computer simulations determined that procaine was more likely to interact with this long-lived Ca(2+)-bound closed state of the channel rather than with other states of the channel. Simulations with the same model were also able to reproduce a prominent Ca(2+)-sensitive transition between "random" and "bursting" forms of gating of the channel, variations of which may account for "gearshift" behavior reported in studies with this and other single channels.

MeSH Terms
Animals Binding Sites Biophysical Phenomena Biophysics Calcium Channels/drug effects,metabolism Dogs Heart/drug effects In Vitro Techniques Ion Channel Gating/drug effects Kinetics Lipid Bilayers Models, Biological Muscle Proteins/drug effects,metabolism Myocardium/metabolism Procaine/pharmacology Ryanodine Receptor Calcium Release Channel Sarcoplasmic Reticulum/drug effects,metabolism
Chemicals
Calcium Channels Lipid Bilayers Muscle Proteins Ryanodine Receptor Calcium Release Channel Procaine
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Zahradníková A
Department of Physiology and Biophysics, University of Texas Medical Branch, Galveston 77555.
Palade P
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Article Info
Journal
Biophysical journal
Abbr.
Biophys J
ISSN
0006-3495
DOI
10.1016/S0006-3495(93)81465-6
Published
1993-04-00
Pages
991-1003
Language
English
Region
United States
NLM ID
0370626
PMCID
PMC1262417
Subset
IM
Grants
NHLBI NIH HHS · P01 HL37044 · United States
NHLBI NIH HHS · R01 HL 42527 · United States
External Links
PubMed source DOI: 10.1016/S0006-3495(93)81465-6 PMC Full Text View journal details
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