Abstract
The structure and pharmacokinetics relationship of 14-beta-adrenoceptor antagonists was investigated in humans. Statistically significant linear and parabolic correlations were found to exist between standard and derived mean pharmacokinetic parameters and the apparent octanol/buffer (pH7.4) partition coefficient of the compounds. The lipophilic/hydrophilic properties were the primary determinants for the pharmacokinetic behavior of the compounds. Most of the pharmacokinetic parameters were also significantly correlated with the plasma protein/plasma water partition coefficient for the compounds. When the values of the pharmacokinetic parameters of the individual compounds were predicted from the regressions on the apparent partition coefficients in octanol/buffer (pH 7.4) and in plasma protein/plasma water, the error was on average 60%.
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An erratum to this article is available at http://dx.doi.org/10.1007/BF01059560.
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Hinderling, P.H., Schmidlin, O. & Seydel, J.K. Quantitative relationships between structure and pharmacokinetics of beta-adrenoceptor blocking agents in man. Journal of Pharmacokinetics and Biopharmaceutics 12, 263–287 (1984). https://doi.org/10.1007/BF01061721
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DOI: https://doi.org/10.1007/BF01061721