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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1999-1-4
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pubmed:abstractText |
Based on volume-flow relationships, CNS agents that are highly lipid soluble (log octanol-water partition coefficient > 2) are expected to have equilibration half-times (T1/2 kE0) that are proportional to brain solubility. Propofol, the most lipophilic anaesthetic in clinical use, has T1/2 kE0 values of 1.7 and 2.9 min in rats and humans, respectively, compared with an expected value of at least 8 min. As a first step in exploring this discrepancy between observed and predicted values, we determined the steady state brain:plasma and brain:blood partition coefficients in rats after a 4-h infusion of propofol. Brain:plasma and brain:blood partition coefficients were 8.2 (SD 1.6) and 3.0 (0.5), respectively. T1/2 kE0 predictions based on brain: blood partitioning in rats are more in agreement with the observed equilibration half-time, suggesting that drug bound to the formed elements of blood participates in the uptake and transfer of propofol to its effect site.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0007-0912
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
81
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
422-4
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:9861134-Analysis of Variance,
pubmed-meshheading:9861134-Anesthetics, Intravenous,
pubmed-meshheading:9861134-Animals,
pubmed-meshheading:9861134-Blood-Brain Barrier,
pubmed-meshheading:9861134-Brain,
pubmed-meshheading:9861134-Male,
pubmed-meshheading:9861134-Models, Biological,
pubmed-meshheading:9861134-Propofol,
pubmed-meshheading:9861134-Rats,
pubmed-meshheading:9861134-Rats, Wistar,
pubmed-meshheading:9861134-Solubility
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pubmed:year |
1998
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pubmed:articleTitle |
Steady-state propofol brain:plasma and brain:blood partition coefficients and the effect-site equilibration paradox.
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pubmed:affiliation |
Department of Pharmaceutics, State University of New York at Buffalo, Amherst 14260, USA.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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