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In the search for new oximes with higher reactivation potency and a broader spectrum, K‐27 and K‐48, have recently been synthesized. To test if their superior efficacy was related to better penetration across the blood–brain barrier, their brain entry was compared with that of obidoxime, when administered either alone or after the organophosphate paraoxon (POX). Rats received 50 µmol obidoxime, K‐27 or K‐48, either alone or in addition to 1 µmol POX. Oxime concentrations at various points in time in brain and plasma were measured using HPLC.

The obidoxime C_max in brain was 1.3% of the plasma C_max when injected alone, and 1.5% when injected following POX. The ratio of the area under the curve (AUC) brain to plasma for obidoxime was around 6%, irrespective of whether it was administered alone or after POX. For K‐27, C_max (brain) was 0.6% of C_max (plasma) when injected alone, and 0.7% when …