Linked Life Data

2455036

Source:http://linkedlifedata.com/resource/pubmed/id/2455036

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1988-7-29
pubmed:abstractText
Effects of the 5-hydroxytryptamine receptor antagonist ICS 205-930 [(3 alpha-tropanyl)-1H-indole-3-carboxylic acid ester] on cardiac membrane currents were investigated in single isolated ventricular cells using the whole-cell patch clamp method. Ca++ and K+ currents were studied in guinea pig ventricular cells and Na+ currents were studied in ventricular cells from cultured neonatal rat; these cells are more suitable for Na+ current measurements than are ventricular cells from guinea pig. Under current clamp conditions, ICS 205-930 at 3 x 10(-5) M prolonged the action potential plateau and increased its amplitude of guinea pig cell. The effect was reversible. Increasing the concentration to 3 x 10(-4) M shortened the plateau, reduced its amplitude and depolarized the resting membrane potential. The effects between 10(-7) and 10(-3) M were examined under voltage-clamp conditions. ICS 205-930 produced a concentration-dependent suppression of inwardly rectifying K+ currents with an IC50 of 1.95 x 10(-5) M at a test potential of -40 mV. The effects were time-and voltage-dependent and the IC50 increased to 1.16 x 10(-4) M at -100 mV. The time-dependent outward current and the time-dependent outward tail currents upon repolarization to between -10 and -30 mV also were blocked by the drug in a concentration-dependent manner with IC50 of 3.7 x 10(-5) M. Ca++ currents and Na+ currents also were inhibited in the presence of higher concentration of ICS 205-930 (greater than 10(-4) M), although potency was stronger on Na+ currents. The results show that ICS 205-930 exerts mixed class III and class I antiarrhythmic properties in ventricular myocytes.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
245
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
773-8
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1988
pubmed:articleTitle
5-Hydroxytryptamine antagonist ICS 205-930 blocks cardiac potassium, sodium and calcium currents.
pubmed:affiliation
Department of Physiology and Molecular Biophysics, Baylor College of Medicine, Texas Medical Center, Houston.
pubmed:publicationType
Journal Article, In Vitro, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't