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See Latest ArticlesMolecular properties and CYP2D6 substrates: central nervous system therapeutics case study and pattern analysis of a substrate database
Drug Metabolism and Disposition, 08/10/09
Chico LK et al. – The results also identified an unexpected issue in CNS drug discovery, in that some property trends correlative with CYP2D6 substrates overlap previously reported properties that correlate with CNS penetrance. These results suggest the need for a careful balance in the design and synthesis of new CNS therapeutic candidates to avoid CYP2D6 substrate status while maintaining CNS penetrance.
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