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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1990-9-17
pubmed:abstractText
Whole cell clamp experiments were used to study the mechanism of action of amiloride on cardiac T-type Ca channels in guinea pig ventricular myocytes. Two hundred fifty microM amiloride blocked the T-type Ca channel for approximately 50%, whereas this concentration did not suppress the L-type Ca channel. The Kd value for the block of the T-type Ca channel was 233 microM and the Hill coefficient was 1.1. The drug showed a rapid onset of action and a quick wash out with complete reversibility. Amiloride blocked the T-type Ca channel without frequency-dependency, i.e., block was established at the holding potential (-90 mV) without being dependent on activation and inactivation of the channel. Amiloride reduced the amplitude of the T-type Ca current at all potentials without changing steady-state activation and inactivation. Amiloride did not affect the T-type Ca current when the drug was applied intracellularly via the pipette solution. In summary, amiloride blocked the T-type Ca channel in a channel state- and voltage-independent way.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
254
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
546-51
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1990
pubmed:articleTitle
Mechanism of cardiac T-type Ca channel blockade by amiloride.
pubmed:affiliation
Laboratory of Physiology, KU Leuven, Campus Gasthuisberg, Belgium.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't