期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 182, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.111643
关键词
CNS; BBB; Brain; Penetration; Pharmacokinetics; Drug design; Free drug hypothesis
资金
- American Lebanese Syrian Associated Charities
- St. Jude Children's Research Hospital
Developing drugs for CNS related diseases continues to be one of the most challenging endeavors in drug discovery. This is at least in part related to the existence of the Blood Brain Barrier (BBB), a complex multicellular organization that provides selective access to required nutrients and hormones, while removing waste and restricting exposure to potential harmful toxins, pathogens, and xenobiotics. Consequently, designing and selecting molecules that can overcame this protection system are unique and critical aspects of the CNS drug discovery. Here we review modern CNS pharmacokinetic concepts and methods suitable for early drug discovery, and medicinal chemistry strategies towards molecules with optimal CNS exposure. (C) 2019 Elsevier Masson SAS. All rights reserved.
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