Linked Life Data

3263633

Source:http://linkedlifedata.com/resource/pubmed/id/3263633

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1988-11-30
pubmed:abstractText
Both myocardial uptake and disposition of bepridil in the isolated rabbit heart showed two-compartment characteristics which possibly reflects the existence of superficial and deep binding sites. Terminal accumulation and disposition half-lives were 218 and 196 min., respectively. The half-times of the initial distributory processes were about 33 min. At a drug concentration in the perfusion liquid of 0.54 micrograms ml-1 (1.27 microM) the average concentration of bepridil in the myocardium at steady state was about 489 micrograms g-1 (1161 microM) with 43% referable to the deepest, presumably intracellular compartment. Increasing bepridil concentrations from 3 to 2333 ng ml-1 (7-5542 nM) in the perfusion liquid caused a terminal decrease in coronary flowrate to 58% of the mean control flowrate. Amplitude and velocity of myocardial contraction both decreased in a biphasic way to about 28.6 and 13.6%, respectively. Apparent dynamic steady states developed within about 20 min. Inhibitory Em-values related to the first phase were 39.8 and 53.2%, and to the second phase 97.7 and 98.5%, respectively. Heart beating frequency also decreased biphasically to 53.9% and showed inhibitory Em-values of 17.2 and 47.5% related to the two phases. Myocardial oxygen consumption decreased to 55.6%. The electrocardiographic PQ- and QRS-intervals increased to 147 and 133%, respectively. The frequency-corrected QT-interval also increased significantly from 100 to 123%. Our findings demonstrate a slow and very pronounced accumulation of bepridil in the rabbit heart. Biphasic and very marked negative inotropic and chronotropic effects and a less than proportional decrease in oxygen consumption developed much faster.(ABSTRACT TRUNCATED AT 250 WORDS)
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0901-9928
pubmed:author
pubmed:issnType
Print
pubmed:volume
63
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
122-8
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1988
pubmed:articleTitle
Bepridil, myocardial accumulation kinetics and dynamic effects in the isolated rabbit heart.
pubmed:affiliation
Institute of Pharmacology, University of Aarhus, Denmark.
pubmed:publicationType
Journal Article, In Vitro