An investigation into the formation of stable, protein-reactive and cytotoxic metabolites from tacrine in vitro. Studies with human and rat liver microsomes

Biochemical Pharmacology

Volumn 46, Issue 1, 1993, Pages 13-20

  Madden, Stephen ^a   Woolf, Thomas F ^b   Pool, William F ^b   Park, B Kevin ^a  

^a UNIVERSITY OF LIVERPOOL   (United Kingdom)

^b PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ASCORBIC ACID; CYCLOHEXANE OXIDE; CYTOCHROME P450 ISOENZYME; DRUG METABOLITE; ENOXACIN; GLUTATHIONE; HUMAN SERUM ALBUMIN; RADIOISOTOPE; REDUCED NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE; TACRINE;

ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; CYTOTOXICITY; DRUG METABOLISM; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; HUMAN TISSUE; LIVER MICROSOME; LYMPHOCYTE; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; RAT; SMOKING;

ADULT; ANIMAL; ASCORBIC ACID; BIOTRANSFORMATION; CELL DEATH; COMPARATIVE STUDY; ENOXACIN; GLUTATHIONE; HUMAN; LYMPHOCYTES; MALE; MICROSOMES, LIVER; NADP; RATS; TACRINE;

EID: 0027326685     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/0006-2952(93)90342-T     Document Type: Article

References (38)

1. Psychotomometics as anticholinergic agents. I. Cyclohexylpiperidene derivatives: anticholinesterase activity and antagonistic activity to acetylcholine
2. Oral tetrahydroaminoacridine in long term treatment of senile dementia, Alzheimer type
3. Tetrahydroaminoacridine and lecithin in Alzheimer's disease
4. A controlled trial of tacrine in Alzheimer's patients
5. Clinical experience with and side effects of tacrine hydrochloride in Alzheimer's disease: a pilot study
6. Effects of tetrahydroaminoacridine on liver function in patients with Alzheimer's disease
7. Metabolic basis of adverse drug reactions
8. N-acetyl-p-benzoquinone imine: a cytochrome P450 mediated oxidation of acetaminophen
9. Synthesis, decomposition kinetics, and preliminary toxicological studies of N-acetyl-p-benzoquinone imine, a proposed toxic metabolite of acetaminophen
10. An investigation of the formation of cytotoxic, protein-reactive and stable metabolites from carbamazepine in vitro
11. Bioactivation of dapsone to a cytotoxic metabolite by human hepatic microsomal enzymes
12. The use of cimetidine as a selective inhibitor of dapsone N-hydroxylation in man
13. Drug-protein conjugates XIV. Mechanisms of formation of protein-arylating intermediates from amodiaquine, a myelotoxin and hepatotoxin in man
14. The mechanism of bioactivation and antigen formation of amodiaquine in the rat
15. Activation mechanisms to chemical toxicity
16. The role of aflatoxin metabolism in its toxin lesion
17. Acetaminophen-induced hepatic necrosis. I. Role of drug metabolism
18. Halothane hepatitis. A model of immune mediated drug hepatotoxicity
19. Identification of the urinary metabolites of tacrine in the rat
20. High performance liquid chromatography for the determination of tacrine and its metabolites in plasma
21. Measurement and characterisation of membrane bound and soluble epoxide hydrolase activities in resting mononuclear leukocytes from human blood
22. Mixed function oxidase and glutathione S-transferase activities in normal human lymphocytes
23. An in vitro study of the microsomal and cellular toxicity of phenytoin, sorbinil and mianserin
24. Acetaminophen toxicity in human lymphocytes in vitro
25. Metabolism of ciamexon by human liver microsomes: an investigation into the formation of stable, chemically reactive and cytotoxic metabolites
26. Metabolism of the contraceptive steroid desogestrel by human liver in vitro
27. Protein measurement with the Folin phenol reagent
28. The carbon monoxide binding pigment of liver microsomes
29. Glutathione depletion: its effect on other antioxidant systems and hepatocellular damage
30. 2+
31. Depletion of glutathione by ciamexon in the rat
32. Direct and metabolism dependent toxicity of sulphasalazine and its principal metabolites towards human erythrocytes and leucocytes
33. in vitro/in vivo correlations in tacrine metabolism and its stimulation by 3-methylcholanthrene
34. The inducibility and catalytic activity of cytochromes P450c (P450IA1) and P450d (P450IA2) in rat tissues
35. Use of caffeine metabolite ratios to explore CYP1A2 and xanthine oxidase activities
36. Drug interaction with quinolones
37. Ciprofloxacincaffeine a drug interaction using in vivo and in vitro investigations
38. Quinolone antibacterial agents: relationship between structure and in vitro inhibition of human cytochrome P450 isoform CYP1A2