Carbonyl reduction of timiperone in human liver cytosol

Pharmacology and Toxicology

Volumn 83, Issue 4, 1998, Pages 164-168

  Shimoda, Kazutaka ^a   Shibasaki, Morikazu ^b   Inaba, Tadanobu ^c   Cheung, Siu Wah ^d   Someya, Toshiyuki ^e   Takahashi, Saburo ^f  

^a SHIGA UNIVERSITY OF MEDICAL SCIENCE   (Japan)

^b The University of Shiga Prefecture   (Japan)

^c UNIVERSITY OF TORONTO   (Canada)

^d CENTRE FOR ADDICTION AND MENTAL HEALTH   (Canada)

^e NIIGATA UNIVERSITY   (Japan)

^f National Hospital Organization   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

CARBONYL REDUCTASE; ETACRYNIC ACID; HALOPERIDOL; MENADIONE; NEUROLEPTIC AGENT; PHENOBARBITAL; TIMIPERONE;

ARTICLE; CONTROLLED STUDY; DRUG CLEARANCE; DRUG METABOLISM; DRUG TRANSFORMATION; ENZYME ACTIVITY; ENZYME KINETICS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; HUMAN TISSUE; LIVER CYTOSOL; MICHAELIS CONSTANT; PRIORITY JOURNAL; REDUCTION;

EID: 0031768954     PISSN: 09019928     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1600-0773.1998.tb01463.x     Document Type: Article

References (20)

1. Campbell, M. E., D. M. Grant, T. Inaba & W. Kakow: Biotransformation of caffeine, paraxanthine, theophylline and theobromine by polycyclic aromatic hydrocarbon inducible cytochrome(s) P-450 in human liver microsomes. Drug. Metab. Dispos. 1987, 15, 237-249.
2. Ereshefsky, L., C. M. Davis, C. A. Harrington, M. W. Jann, J. L. Browning, S. R. Saklad & N. R. Burch: Haloperidol and reduced haloperidol plasma levels in selected schizophrenic patients. J. Clin. Psychopharmacol. 1984, 4, 138-142.
3. Inaba, T., M. Jurima, W. A. Hahon & Kalow: In vitro inhibition studies of two isozymes of human liver cytochrome P-450: mephenytoin p-hydroxylase and sparteine monooxygenase. Drug. Metab. Dispos. 1985, 13, 443-448.
4. Inaba, T., W. Kalow, T. Someya, S. Takahashi, S. W. Cheung & S. W. Tang: Haloperidol reduction can be assayed in human red blood cells. Can. J. Physiol. Pharmacol. 1989, 67, 1468-1469.
5. Inaba, T. & J. Kovacs: Haloperidol reductase in human and guinea pig livers. Drug. Metab. Dispos. 1989, 17, 330-333.
6. Kariya, T., Y. Shimozono, H. Itoh, H. Mori, M. Murasaki, K. Sugano, M. Toru & I Yamashita: A comparison of the clinical effects of timiperone, a new bulyrophenone derivative, and a halopendol on schizophrenia using double-blind technique. J. Int. Med. Res. 1983, 11, 66-77.
7. Ko, G. N., E. R. Korpi & D. G. Kirsh: Haloperidol and reduced haloperidol concentrations in plasma and red blood cells from chronic schizophrenic patients. J. Clin. Psychopharmacol. 1989, 9, 186-190.
8. Korpi, E. R., D. T. Costakos & R. J. Wyatt: Interconversions of haloperidol and reduced haloperidol in guinea pig and rat liver microsomes. Biochem. Pharmacol. 1985a, 343, 2923-2927.
9. Korpi, E. R., D. T. Costakos & R. J. Wyatt: Rapid formation of reduced haloperidol in guinea pigs following haloperidol administration. Acta pharmacol. et toxicol. 1985b, 56, 94-98.
10. Moses, E. L., P. Varghese, J. M. Walker & W. D. Bowen: Metabolites of haloperidol exhibit high affinity and biological activity at sigma receptors. Soc. Neurosci. Abstr. 1989, 15, 265.
11. Nakazawa, T., K. Ohara, Y. Sawa, T. Edakubo, H. Matsui, J. Sawa, K. Kawaguchi, S. Hattori & M. Nakajima: Comparison of efficacy of timiperone, a new hutyrophenone derivative, and clocapramine in schizophrenia: A multicenter double-blind study. J. Int. Med. Res. 1983, 11, 247-258.
12. Shibasaki, M., T. Someya & S. Takahashi: Relation of plasma and red blood cells reduced haloperidol concentrations to haloperidol reductase activity assayed in red blood cells in psychiatric population. Prog. Neuropsychopharmacol. Biol. Psychiatry. 1993, 17, 257-267.
13. Shoslak, M., J. M. Perel, R. L. Stiller, W. Wyman & S. Curran: Plasma haloperidol and clincial response: A role for reduced haloperidol in antipsychotic activity. J. Clin. Psychopharmacol. 1987, 7, 394-400.
14. Someya, T., T. Inaba, R. F. Tyndale, S. W. Tang & S. Takahashi: Conversion of bromperidol to reduced bromperidol in human liver. Neuropsychopharmacology 1991a, 5, 177-182.
15. Someya, T., M. Shibasaki, T. Kato, T. Noguchi, N. Ishida & S. Takahashi: Haloperidol reductase activity in red blood cells from oriental patients on haloperidol. Prog. Neuropsychopharmacol. Biol. Psychiatry 1991b, 15, 275-278.
16. 3H-spiroperidol binding to rat striatal dopamine receptors. Eur. J. Pharmacol. 1979, 59, 245-251.
17. Tachizawa, H., K. Sudo, H. Sasano & M. Sano: Disposition and metabolism of timiperone in the rat, dog, and monkey. Drug. Metab. Dispos. 1981, 9, 442-448.
18. Tyndale, R. F., W. Kalow & T. Inaba: Oxidation of reduced haloperidol to haloperidol: involvement of human P450IID6 (sparteine/ debrisoquine monooxygenase). Brit. J. Clin. Pharmacol. 1991, 31, 655-660.
19. Wong, J. M. Y., W. A. Mahon, W. Kalow & T. Inaba: Carbonyl (Phenone) reductase in human liver: structure activity relationship among substrate. Drug. Metab. Dispos. 1992, 20, 465-466.
20. Yamasaki, T. H. Kojima, T. Sakurai, A. Kasahara, S. Watanabe, M. Fujiwara & S. Ueki: Pharmacological studies on timiperone, a new neuroleptic drug. part 1. Arzneimittelforsch. (Drug. Res) 1981, 31, 701-707.