Selecting Good 'Drug-Like' Properties to Optimize Small Molecule Blood-Brain Barrier Penetration.

摘要: The success rate to achieve clinical approval of drugs developed treat diseases the central nervous system (CNS) is lowest all disease indications. A large contributor this poor failure small molecules pass through blood-brain barrier (BBB), a composed capillary endothelial cells connected by tight junctions that functions extrude xenobiotics from brain. Designing be BBB penetrant has been subject intensive research and resulted in series guidelines attain best possible chances penetration. This review will analyze current state thinking ranking importance various physicochemical properties required select molecules, describe model systems determine penetration, summarize data analysis methods provide an outlook on further developments field.