Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
|
pubmed:dateCreated |
1997-3-28
|
pubmed:abstractText |
Phenol has various medical applications but can cause convulsions and cardiac arrhythmia suggestive of K+ channel block. We examined phenol inhibition of the delayed-rectifier RCK1 (Kv1.1) K+ channel cloned from rat brain and expressed in Xenopus laevis oocytes. Phenol (2.5 mM) caused a 43 +/- 5 mV depolarizing shift in the RCK1 half-activation voltage (Vg) but only a 10 +/- 3% decrease in the peak conductance at 80 mV. The 10-90% rise time was slightly increased, but this was not simply the result of the activation shift. By contrast, deactivation kinetics at -40 mV were greatly accelerated. The importance of the phenolic hydroxyl group was assessed by comparing the effects of p-cresol (a phenol) and its structural isomer benzyl alcohol (an aryl alcohol). p-Cresol (1.5 mM) produced a 53 +/- 2 mV depolarizing shift in Vg, but benzyl alcohol was much less effective--20 mM caused a depolarizing shift of only 23 +/- 1 mV. Both isomers also accelerated channel deactivation. Phenol and p-cresol are better hydrogen bond donors than acceptors, whereas benzyl alcohol is a better acceptor than donor. A hydrogen bond between the phenolic hydroxyl and a presently unknown acceptor group may therefore underlie some aspects of K+ channel inhibition. Depolarizing shifts in Vg and accelerated tail kinetics are consistent with 1) preferential phenol binding to resting channels, causing the shift in Vg, and 2) a conducting phenol-bound open state with faster deactivation kinetics than the unbound open state.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/4-cresol,
http://linkedlifedata.com/resource/pubmed/chemical/Benzyl Alcohol,
http://linkedlifedata.com/resource/pubmed/chemical/Benzyl Alcohols,
http://linkedlifedata.com/resource/pubmed/chemical/Cresols,
http://linkedlifedata.com/resource/pubmed/chemical/Phenol,
http://linkedlifedata.com/resource/pubmed/chemical/Phenols,
http://linkedlifedata.com/resource/pubmed/chemical/Potassium Channels
|
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
0026-895X
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
51
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
475-83
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:9058603-Animals,
pubmed-meshheading:9058603-Benzyl Alcohol,
pubmed-meshheading:9058603-Benzyl Alcohols,
pubmed-meshheading:9058603-Brain,
pubmed-meshheading:9058603-Cloning, Molecular,
pubmed-meshheading:9058603-Cresols,
pubmed-meshheading:9058603-Ion Channel Gating,
pubmed-meshheading:9058603-Membrane Potentials,
pubmed-meshheading:9058603-Oocytes,
pubmed-meshheading:9058603-Phenol,
pubmed-meshheading:9058603-Phenols,
pubmed-meshheading:9058603-Potassium Channels,
pubmed-meshheading:9058603-Rats,
pubmed-meshheading:9058603-Xenopus laevis
|
pubmed:year |
1997
|
pubmed:articleTitle |
Voltage-dependent inhibition of RCK1 K+ channels by phenol, p-cresol, and benzyl alcohol.
|
pubmed:affiliation |
Department of Anatomy and Physiology, University of Dundee, Scotland.
|
pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
|