Literature DB >> 3289270

Distribution coefficient, a convenient term for the relation of predictable physico-chemical properties to metabolic processes.

C N Manners1, D W Payling, D A Smith.   

Abstract

1. The consequences of metabolic transformation on lipophilicity have been considered using the terms log P (partition coefficient) and log D (distribution coefficient). 2. Transformations which result in no change in the degree of ionisation can be readily predicted by the use of fragmental constants and log P. 3. If metabolism alters the degree of ionization then the distribution coefficient, log D, at physiological pH is a more appropriate term to use. Intuitive empirical observations may be incorrect and lead to false assumptions about the lipophilicity or water solubility of metabolites. 4. Metabolism may form zwitterionic molecules. These metabolites need special consideration since their penetration into lipid phases may be greater than expected.

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Year:  1988        PMID: 3289270     DOI: 10.3109/00498258809041669

Source DB:  PubMed          Journal:  Xenobiotica        ISSN: 0049-8254            Impact factor:   1.908


  6 in total

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2.  Insight into the lipophilicity of the aromatic N-oxide moiety.

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4.  High-throughput in-silico prediction of ionization equilibria for pharmacokinetic modeling.

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Review 5.  Design of drugs through a consideration of drug metabolism and pharmacokinetics.

Authors:  D A Smith
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  6 in total

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