Linked Life Data

10575200

Source:http://linkedlifedata.com/resource/pubmed/id/10575200

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4-5
pubmed:dateCreated
2000-5-8
pubmed:abstractText
ATP-dependent potassium (K(ATP)) channels exist in high density in the sarcolemmal membrane of heart muscle cells. Under normoxic conditions these channels are closed, but they become active when the intracellular ATP level falls. This leads to a shortening of the action potential duration, rendering the heart susceptible for life-threatening arrhythmias. Molecular biology has revealed that K(ATP) channels consist of heteromultimers of the inwardly rectifying channel Kir6.2 and the sulfonylurea receptor SUR. To date, three types of SURs were identified, representing the pancreatic (SUR1), the cardiac (SUR2A) and the smooth muscle (SUR2B) K(ATP) channel. In order to develop a novel therapeutic principle against ischemia-induced life-threatening arrhythmias leading to sudden cardiac death, the cardioselective K(ATP) channel blocker HMR 1883 was developed. This substance inhibits the sarcolemmal cardiac K(ATP) channel activated by the channel opener rilmakalim half-maximally at concentrations of 0.6-2.2 micromol/l, and substantially affects pancreatic K(ATP) channels at 9-50 times higher concentrations. K(ATP) channels of the coronary vascular system are only slightly blocked by HMR 1883 when activated by hypoxia. The substance was potently effective in preventing ventricular fibrillation in a conscious dog model, and thus can be considered to be a potential novel drug candidate against sudden cardiac death.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
1015-8987
pubmed:author
pubmed:copyrightInfo
Copyright 1999 S. Karger AG, Basel
pubmed:issnType
Print
pubmed:volume
9
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
227-41
pubmed:dateRevised
2009-12-30
pubmed:meshHeading
pubmed:year
1999
pubmed:articleTitle
Molecular basis, pharmacology and physiological role of cardiac K(ATP) channels.
pubmed:affiliation
Hoechst Marion Roussel, DG Cardiovascular Frankfurt/Main, Germany.
pubmed:publicationType
Journal Article, Review