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See Latest ArticlesModulation of LogD(7.4) and pKa to achieve the optimum balance of blood clearance and volume of distribution for a series of tetrahydropyran H3 antagonists
Drug Metabolism and Disposition, 06/23/09
Hay TL et al. - This relationship was rationalized in respect to the interactions of the ionisable centres with phospholipid heads in the cell membrane and/or lysosomal trapping. Compounds in the weak second base sub-series showed optimal volumes of distribution and when combined with a LogD(7.4) of 0.1, driving to moderate blood clearance, one compound showed the optimal pharmacokinetic profile.
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