In vitro screening of blood-brain barrier penetration of monoquaternary acetylcholinesterase reactivators

摘要

The HPLC method for prediction of drug penetration into the CNS was examined in our study. In this in vitro study, we determined the ability of monoquaternary AChE reactivators to penetrate through blood-brain barrier (BBB). Three reactivators varying in the position of oxime group on the pyridinium ring (2-PAM, 3-PAM and 4-PAM) were evaluated. As a result, the position of the oxime group on the pyridine ring plays a role for penetration of oximes into brain. The best position of oxime group seems to be position four. The location on the position two and three is not favorable for penetrating through BBB.