Abstract
Several drugs with structural similarities to SKF-525A were tested for their ability to inhibit rat liver aldehyde oxidase using the experimental antitumour agent N-[(2'-dimethylamino)ethyl]acridine-4-carboxamide (AC; NSC 601316; acridine carboxamide) as substrate. The antihistamine d-chlorpheniramine, and the antiarrhythmics disopyramide, procainamide and lignocaine were ineffective in inhibiting this reaction. The antihistamines diphenhydramine, pheniramine, doxylamine, orphenadrine, methapyrilene and pyrilamine, gave ic 50 values of 100–500 μM. The narcotic analgesics d-propoxyphene and, in particular, methadone were potent inhibitors of acridone formation with ic 50 values of 15.5 and 0.31 μM, respectively. Further analysis indicates mixed non-competitive type inhibition by methadone with inhibition constants ( K is and K ii , respectively) of 0.03 ± 0.01 (SE) and 0.57 ± 0.12μM.
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