Premium
The application of in situ and in vitro models for screening blood–brain barrier permeation
Author(s) -
Read K. D.
Publication year - 2003
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1046/j.1471-4159.85.s2.7_2.x
Subject(s) - blood–brain barrier , penetration (warfare) , in vitro , permeation , central nervous system , chemistry , pharmacology , drug , neuroscience , biophysics , in situ , biology , biochemistry , membrane , engineering , operations research , organic chemistry
The properties of the blood–brain barrier (BBB) are relevant to any program for drug discovery and development. Compounds chosen for their specificity at CNS target sites need to cross the BBB for biological action, yet high affinity for central sites does not guarantee BBB penetration. Conversely, compounds designed to act peripherally need to be tailored for low BBB penetration in order to avoid CNS side‐effects. A combination of in situ and in vitro models of the BBB, together with chemical understanding of the mechanisms of BBB penetration, can aid design and selection of compounds with appropriate properties to permeate, or to be excluded from, the CNS.