Document Detail

Methadone: a potent inhibitor of rat liver aldehyde oxidase.
MedLine Citation:
PMID:  8117328     Owner:  NLM     Status:  MEDLINE    
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 IC50 values of 100-500 microM. The narcotic analgesics D-propoxyphene and, in particular, methadone were potent inhibitors of acridine formation with IC50 values of 15.5 and 0.31 microM, respectively. Further analysis indicates mixed non-competitive type inhibition by methadone with inhibition constants (Kis and Kii, respectively) of 0.03 +/- 0.01 (SE) and 0.57 +/- 0.12 microM.
I G Robertson; R S Gamage
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Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Biochemical pharmacology     Volume:  47     ISSN:  0006-2952     ISO Abbreviation:  Biochem. Pharmacol.     Publication Date:  1994 Feb 
Date Detail:
Created Date:  1994-03-25     Completed Date:  1994-03-25     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  0101032     Medline TA:  Biochem Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  584-7     Citation Subset:  IM    
Department of Pharmacology and Clinical Pharmacology, University of Auckland School of Medicine, New Zealand.
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MeSH Terms
Acridines / analysis,  metabolism
Aldehyde Oxidase
Aldehyde Oxidoreductases / antagonists & inhibitors*
Dextropropoxyphene / pharmacology
Liver / drug effects*,  enzymology
Methadone / pharmacology*
Proadifen / pharmacology
Reg. No./Substance:
0/Acridines; 302-33-0/Proadifen; 469-62-5/Dextropropoxyphene; 578-95-0/acridone; 76-99-3/Methadone; EC 1.2.-/Aldehyde Oxidoreductases; EC Oxidase

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