Specific binding of 1-[2-(diphenylmethoxy)ethyl]-4(3-phenyl propyl) piperazine (GBR-12935), an inhibitor of the dopamine transporter, to human CYP2D6

Biochemical Pharmacology

Volumn 53, Issue 12, 1997, Pages 1937-1939

  Hiroi, Toyoko ^a   Imaoka, Susumu ^a   Chow, Toshio ^a   Yabusaki, Yoshiyasu ^b   Funae, Yoshihiko ^a  

^a OSAKA CITY UNIVERSITY GRADUATE SCHOOL OF MEDICINE   (Japan)

^b SUMITOMO CHEMICAL CO LTD   (Japan)

Author keywords

Cytochrome P450 2D forms; Dopamine transporter; Human; Piperazine acceptor

Indexed keywords

1 [2 (BENZHYDRYLOXY)ETHYL] 4 (3 PHENYLPROPYL)PIPERAZINE; BUFURALOL; CYTOCHROME P450; DESIPRAMINE; DOPAMINE; DOPAMINE TRANSPORTER; IMIPRAMINE; PROPRANOLOL; QUINIDINE; QUININE;

ARTICLE; BINDING SITE; BRAIN CORTEX; DRUG PROTEIN BINDING; ENZYME POLYMORPHISM; PRIORITY JOURNAL; SACCHAROMYCES CEREVISIAE; YEAST CELL;

CARRIER PROTEINS; CYTOCHROME P-450 CYP2D6; DOPAMINE; DOPAMINE PLASMA MEMBRANE TRANSPORT PROTEINS; GENE EXPRESSION; HUMANS; KINETICS; MEMBRANE GLYCOPROTEINS; MEMBRANE TRANSPORT PROTEINS; MITOCHONDRIA; NERVE TISSUE PROTEINS; PIPERAZINES; QUINIDINE; QUININE; SACCHAROMYCES CEREVISIAE;

EID: 0030790463     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(97)00172-X     Document Type: Article

References (18)

1. Tyndale RF, Sunahara R, Inaba T, Kalow W, Gonzalez FJ and Niznik HB, Neuronal cytochrome P450IID1 (debrisoquine/ sparteine-type): Potent inhibition of activity by (-)-cocaine and nucleotide sequence identity to human hepatic P450 gene CYP2D6. Mol Pharmacol 40: 63-68, 1991.
2. Matsuo Y, Iwahashi K and Ichikawa Y, Debrisoquine 4-monooxygenase and bufuralol 1′-monooxygenase activities in bovine and rabbit tissues. Biochem Pharmacol 43: 1911-1919, 1992.
3. Komori M, A novel P450 expressed at the high level in rat brain. Biochem Biophys Res Commun 196: 721-728, 1993.
4. Jiang Q, Voigt JM and Colby HD, Molecular cloning and sequencing of a guinea pig cytochrome P4502D (CYP2D16): High level expression in adrenal microsomes. Biochem Biophys Res Commun 209: 1149-1156, 1995.
5. Carcillo JA, Parise RA, Adedoyin A, Frye R, Branch RA and Romkes M, CYP2D6 mRNA expression in circulating peripheral blood mononuclear cells correlates with in vivo debrisoquine hydroxylase activity in extensive metabolizers. Res Commun Mol Pathol Pharmacol 91: 149-159, 1996.
6. 3H]GBR 12935 binding in vitro to rat striatal membranes: Labeling of the dopamine uptake complex. J Neurochem 48: 1887-1896, 1987.
7. 3H]GBR-12935 binding to dopamine uptake sites in the human brain. Brain Res 457: 122-129, 1988.
8. 3H]GBR-12935 binding proteins. Arch Biochem Biophys 276: 424-432, 1990.
9. 1 receptor with quinine. J Pharmacol Exp Ther 268: 959-964, 1994.
10. Hiroi T, Ohishi N, Imaoka S, Yabusaki Y, Fukui H and Funae Y, Mepyramine, a histamine H1 receptor antagonist, inhibits the metabolic activity of rat and human P450 2D forms. J Pharmacol Exp Ther 272: 939-944, 1995.
11. Imaoka S, Yamada T, Hiroi T, Hayashi K, Sakaki T, Yabusaki Y and Funae Y, Multiple forms of human P450 expressed in Saccharomyces cerevisiae. Systematic characterization and comparison with those of the rat. Biochem Pharmacol 51: 1041-1050, 1996.
12. Eshleman AJ, Neve RL, Janowsky A and Neve KA, Characterization of a recombinant human dopamine transporter in multiple cell lines. J Pharmacol Exp Ther 274: 276-283, 1995.
13. Kobayashi S, Murray S, Watson D, Sesardic D, Davies DS and Boobis AR, The specificity of inhibition of debrisoquine 4-hydroxylase activity by quinidine and quinine in the rat is the inverse of that in man. Biochem Pharmacol 38: 2795-2799, 1989.
14. De Groot MJ, Bijloo GJ, Hansen KT and Vermeulen NPE, Computer prediction and experimental validation of cytochrome P4502D6-dependent oxidation of GBR 12909. Drug Metab Dispos 23: 667-669, 1995.
15. 3H]GBR-12935 binding to human cerebral cortex is not to dopamine uptake sites. J Neurochem 62: 338-341, 1994.
16. 3H]GBR 12935 labels mainly the piperazine acceptor site in the rat prefrontal cortex. Brain Res 674: 205-210, 1995.
17. Norris PJ, Hardwick JP and Emson PC, Regional distribution of cytochrome P450 2D1 in the rat central nervous system. J Comp Neural 366: 244-258, 1996.
18. 3H]GBR-12935 binding to cytochrome P450 in the human brain. J Neurochem 62: 342-348, 1994.