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      Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects for Peripheral Drugs 

      Case Studies of CNS Drug Optimization-Medicinal Chemistry and CNS Biology Perspectives

      John Wiley & Sons, Inc

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          Most cited references 35

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          Synopsis of some recent tactical application of bioisosteres in drug design.

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            Drug-like properties and the causes of poor solubility and poor permeability

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              The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery.

              Data from in vitro plasma protein binding experiments that determine the fraction of protein-bound drug are frequently used in drug discovery to guide structure design and to prioritize compounds for in vivo studies. However, we consider that these practices are usually misleading, because in vivo efficacy is determined by the free (unbound) drug concentration surrounding the therapeutic target, not by the free drug fraction. These practices yield no enhancement of the in vivo free drug concentration. So, decisions based on free drug fraction could result in the wrong compounds being advanced through drug discovery programmes. This Perspective provides guidance on the application of plasma protein binding information in drug discovery.
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                Author and book information

                Book
                9781118788523
                9781118788356
                January 30 2015
                10.1002/9781118788523
                Product
                Book Chapter
                January 02 2015
                : 425-445
                10.1002/9781118788523.ch19

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