pubmed-article:3263633 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:3263633 | lifeskim:mentions | umls-concept:C0034493 | lld:lifeskim |
pubmed-article:3263633 | lifeskim:mentions | umls-concept:C0018787 | lld:lifeskim |
pubmed-article:3263633 | lifeskim:mentions | umls-concept:C1522564 | lld:lifeskim |
pubmed-article:3263633 | lifeskim:mentions | umls-concept:C0005116 | lld:lifeskim |
pubmed-article:3263633 | lifeskim:mentions | umls-concept:C0205409 | lld:lifeskim |
pubmed-article:3263633 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
pubmed-article:3263633 | lifeskim:mentions | umls-concept:C0022702 | lld:lifeskim |
pubmed-article:3263633 | pubmed:issue | 2 | lld:pubmed |
pubmed-article:3263633 | pubmed:dateCreated | 1988-11-30 | lld:pubmed |
pubmed-article:3263633 | 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) | lld:pubmed |
pubmed-article:3263633 | pubmed:language | eng | lld:pubmed |
pubmed-article:3263633 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:3263633 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:3263633 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:3263633 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:3263633 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:3263633 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:3263633 | pubmed:month | Aug | lld:pubmed |
pubmed-article:3263633 | pubmed:issn | 0901-9928 | lld:pubmed |
pubmed-article:3263633 | pubmed:author | pubmed-author:Nielsen-Kudsk... | lld:pubmed |
pubmed-article:3263633 | pubmed:author | pubmed-author:JakobsenPP | lld:pubmed |
pubmed-article:3263633 | pubmed:author | pubmed-author:AskholtJJ | lld:pubmed |
pubmed-article:3263633 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:3263633 | pubmed:volume | 63 | lld:pubmed |
pubmed-article:3263633 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:3263633 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:3263633 | pubmed:pagination | 122-8 | lld:pubmed |
pubmed-article:3263633 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
pubmed-article:3263633 | pubmed:meshHeading | pubmed-meshheading:3263633-... | lld:pubmed |
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pubmed-article:3263633 | pubmed:meshHeading | pubmed-meshheading:3263633-... | lld:pubmed |
pubmed-article:3263633 | pubmed:year | 1988 | lld:pubmed |
pubmed-article:3263633 | pubmed:articleTitle | Bepridil, myocardial accumulation kinetics and dynamic effects in the isolated rabbit heart. | lld:pubmed |
pubmed-article:3263633 | pubmed:affiliation | Institute of Pharmacology, University of Aarhus, Denmark. | lld:pubmed |
pubmed-article:3263633 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:3263633 | pubmed:publicationType | In Vitro | lld:pubmed |