Sodium inactivation mechanism modulates QX-314 block of sodium channels in squid axons

J. Z. Yeh

doi:10.1016/S0006-3495(78)85403-4

Sodium inactivation mechanism modulates QX-314 block of sodium channels in squid axons

J. Z. Yeh^*

^*Corresponding author for this work

Pharmacology

Research output: Contribution to journal › Article › peer-review

26 Scopus citations

Abstract

Blocking action of Na channels by QX-314, a quaternary derivative of lidocaine, was studied in internally perfused and voltage-clamped axons of squid. In axons with intact Na inactivation, QX-314 exhibited both a frequency- and a voltage-dependent block of Na channels. Repetitive pulsing to more positive potentials enhanced the degree of block. Both frequency- and voltage-dependent blocks disappeared in axons in which Na inactivation had been destroyed by either pronase or N-bromoacetamide treatment. These results support the notion that Na inactivation not only modulates the frequency-dependent block but also involves the voltage-dependent binding reaction between QX-314 and Na channels.

Original language	English (US)
Pages (from-to)	569-574
Number of pages	6
Journal	Biophysical Journal
Volume	24
Issue number	2
DOIs	https://doi.org/10.1016/S0006-3495(78)85403-4
State	Published - 1978

ASJC Scopus subject areas

Biophysics

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10.1016/S0006-3495(78)85403-4

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@article{4a2c751b2128480189b31d58223af028,

title = "Sodium inactivation mechanism modulates QX-314 block of sodium channels in squid axons",

abstract = "Blocking action of Na channels by QX-314, a quaternary derivative of lidocaine, was studied in internally perfused and voltage-clamped axons of squid. In axons with intact Na inactivation, QX-314 exhibited both a frequency- and a voltage-dependent block of Na channels. Repetitive pulsing to more positive potentials enhanced the degree of block. Both frequency- and voltage-dependent blocks disappeared in axons in which Na inactivation had been destroyed by either pronase or N-bromoacetamide treatment. These results support the notion that Na inactivation not only modulates the frequency-dependent block but also involves the voltage-dependent binding reaction between QX-314 and Na channels.",

author = "Yeh, {J. Z.}",

note = "Funding Information: I wish to thank Dr. Toshio Narahashi for support and encouragement at all stages of this work. Thanks are also due to Drs. Roger Anwyl and Chau H. Wu for comment on the manuscript, and to Amy Bicego, June Canzoneri, and Jessie Williams for secretarial assistance. This work was supported by U.S. Public Health Service grants NS14144, RR 05370, and GM 24866. The experiments were performed at the Marine Biological Laboratory, Woods Hole, Mass. Receivedfor publication 3 January 1978 and in revisedform 26 July 1978.",

year = "1978",

doi = "10.1016/S0006-3495(78)85403-4",

language = "English (US)",

volume = "24",

pages = "569--574",

journal = "Biophysical Journal",

issn = "0006-3495",

publisher = "Biophysical Society",

number = "2",

}

TY - JOUR

T1 - Sodium inactivation mechanism modulates QX-314 block of sodium channels in squid axons

AU - Yeh, J. Z.

N1 - Funding Information: I wish to thank Dr. Toshio Narahashi for support and encouragement at all stages of this work. Thanks are also due to Drs. Roger Anwyl and Chau H. Wu for comment on the manuscript, and to Amy Bicego, June Canzoneri, and Jessie Williams for secretarial assistance. This work was supported by U.S. Public Health Service grants NS14144, RR 05370, and GM 24866. The experiments were performed at the Marine Biological Laboratory, Woods Hole, Mass. Receivedfor publication 3 January 1978 and in revisedform 26 July 1978.

PY - 1978

Y1 - 1978

N2 - Blocking action of Na channels by QX-314, a quaternary derivative of lidocaine, was studied in internally perfused and voltage-clamped axons of squid. In axons with intact Na inactivation, QX-314 exhibited both a frequency- and a voltage-dependent block of Na channels. Repetitive pulsing to more positive potentials enhanced the degree of block. Both frequency- and voltage-dependent blocks disappeared in axons in which Na inactivation had been destroyed by either pronase or N-bromoacetamide treatment. These results support the notion that Na inactivation not only modulates the frequency-dependent block but also involves the voltage-dependent binding reaction between QX-314 and Na channels.

AB - Blocking action of Na channels by QX-314, a quaternary derivative of lidocaine, was studied in internally perfused and voltage-clamped axons of squid. In axons with intact Na inactivation, QX-314 exhibited both a frequency- and a voltage-dependent block of Na channels. Repetitive pulsing to more positive potentials enhanced the degree of block. Both frequency- and voltage-dependent blocks disappeared in axons in which Na inactivation had been destroyed by either pronase or N-bromoacetamide treatment. These results support the notion that Na inactivation not only modulates the frequency-dependent block but also involves the voltage-dependent binding reaction between QX-314 and Na channels.

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U2 - 10.1016/S0006-3495(78)85403-4

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AN - SCOPUS:0018114378

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JO - Biophysical Journal

JF - Biophysical Journal

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ER -

Sodium inactivation mechanism modulates QX-314 block of sodium channels in squid axons

Abstract

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