Abstract
The blood–brain barrier (BBB) permeability to [ 3H]-azidodeoxythymidine (AZT), deoxythiacytidine (3TC™), and thymidine was studied using both an intravenous injection/external organ (IV/EO) method and an internal carotid artery perfusion (ICAP) technique in parallel with [ 14C]-sucrose as a plasma volume marker. The brain volumes of distribution ( V D) of the three compounds approximated that of sucrose with either method. Although the lipid solubility of AZT, as determined by the 1-octanol/buffer partition coefficient ( P), was 16-fold higher than that of thymidine, the BBB permeability-surface area (PS) products were almost identical, consistent with preferential efflux of AZT from brain to blood.
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