The absorption, distribution, and excretion in mice of a quinolinemethanol antimalarial, 2,8-bis(trifluoromethyl)-4-(1-hydroxy-3-(N-t-butylamino)propyl)quinoline phosphate (WR 184,806)

Abstract

Approximately 75% of the radioactivity derived from WR 184806-14C was excreted in the feces with the remainder in the urine after po administration. At least 77-85% of the dose was absorbed by 2-8 hr; lungs, liver, skeletal muscle, kidneys, small intestine (less contents) and residual carcass were major sites of deposition of total radioactivity. Within these tissues the radioactivity present was predominantly as WR 184,806 rather than its metabolites. Peak blood plasma levels of WR 184,806 occurred at 2-4 and 7-10 hr. The peak erythrocyte level of WR 184,806 occurred at 6 hr. The presence in the urine and feces of unchanged WR 184,806 was confirmed by thin-layer chromatography and inverse isotope dilution.