Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1988-6-8
pubmed:abstractText
Octanol-water partition coefficients have been used as a principal parameter for the analysis of quantitative structure-activity relationships (QSAR). With ionized drugs, however, the correlation is not impressive. Although clinical local anesthetics exist mainly in the ionized form at physiological pH, the nerve-blocking potency is correlated with the oil-water partition coefficients of the un-ionized species. In the present report, the adsorption of 18 local anesthetics onto activated carbon surfaces was compared with oil-water partition coefficients for correlation with the minimum nerve-blocking (MBC) potency. The log octanol-water partition coefficients showed large differences between the charged and uncharged species (lidocaine: 0.49 and 1.82, procaine: -0.56 and 1.74, respectively), whereas the log carbon surface adsorbabilities showed much smaller differences (lidocaine: 3.00 and 3.04, and procaine 2.95 and 3.00, respectively). An excellent correlation was found between the log carbon surface adsorption and the log MBC values in both ionized and un-ionized drugs.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0022-3549
pubmed:author
pubmed:issnType
Print
pubmed:volume
77
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
166-8
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1988
pubmed:articleTitle
Activated carbon as a biological model: comparison between activated carbon adsorption and oil-water partition coefficient for drug activity correlation.
pubmed:affiliation
Department of Anesthesia, University of Utah School of Medicine, Salt Lake City 84132.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, U.S. Gov't, P.H.S., Research Support, U.S. Gov't, Non-P.H.S.