Strategies to optimize brain penetration in drug discovery.
作者： Cuiping Chen , Xingrong Liu
DOI:
关键词: Fast onset 、 Biophysics 、 Penetration (firestop) 、 Central nervous system 、 Plasma binding 、 Drug discovery 、 Efflux 、 Brain tissue 、 Chemistry 、 Transport activity
摘要: The kinetics of brain penetration has two components, extent and rate. Achieving a high is an important focus for central nervous system (CNS) drug discovery. Optimal can be achieved by reducing efflux transport at the blood-brain barrier (BBB), it critical to ensure that total brain/plasma ratio (the most commonly used parameter measuring penetration) due activity BBB not related non-specific tissue binding or low plasma binding. Rapid essential those drugs require fast onset action in CNS. This increasing passive permeability
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