Comparison of pulmonary accumulation of pyrilamine and pyrilamine N-oxide.
Our previous studies have indicated that a phenothiazine drug, chlorpromazine, and a tricyclic antidepressant, imipramine, are metabolized by the isolated perfused rat lungs via N-oxidation from whence their N-oxides are released into the circulation. This work was undertaken to compare the pulmonary accumulation of another pneumophilic tertiary amine drug, pyrilamine, with that of its N-oxide. Approximately 10-fold greater accumulation of pyrilamine than that of its N-oxide was observed in the mouse lung after a single pass perfusion with 40 microM of the drug for a 3 min period. The largest difference between accumulation of pyrilamine and its N-oxide was noted in the lung among the various tissue slices tested, suggesting the tissue specificity of affinity.
D000631:Aminopyridines / Q000378:metabolism*; D000818:Animals; D003497:Cyclic N-Oxides / Q000378:metabolism*; D066298:In Vitro Techniques; D007700:Kinetics; D008168:Lung / Q000378:metabolism*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D011738:Pyrilamine / Q000031:analogs & derivatives / Q000378:metabolism*
D000631:Aminopyridines; D003497:Cyclic N-Oxides; C049169:pyrilamine N-oxide; D011738:Pyrilamine