[3H]-trimetazidine mitochondrial binding sites: Regulation by cations, effect of trimetazidine derivatives and other agents and interaction with an endogenous substance

British Journal of Pharmacology

Volumn 130, Issue 3, 2000, Pages 655-663

  Morin, Didier ^a   Sapena, Rosa ^a   Elimadi, Aziz ^a   Testa, Bernard ^b   Labidalle, Serge ^c   Le Ridant, Alain ^d   Tillement, Jean Paul ^a  

^a FACULTÉ DE MÉDECINE   (France)

^b UNIVERSITY OF LAUSANNE   (Switzerland)

^c UNIVERSITÉ DE TOULOUSE   (France)

^d INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

Author keywords

Brain mitochondria; Rat liver mitochondria; Specific binding sites; Trimetazidine

Indexed keywords

CATION; DEXTROMETHORPHAN; HALOPERIDOL; IFENPRODIL; OPIPRAMOL; PENTAZOCINE; PENTOXYVERINE; PERPHENAZINE; PRENYLAMINE; SIGMA OPIATE RECEPTOR; TRIMETAZIDINE;

ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BINDING SITE; BRAIN MITOCHONDRION; CONTROLLED STUDY; DRUG RECEPTOR BINDING; ISOTOPE LABELING; LIVER MITOCHONDRION; MALE; MITOCHONDRION; NONHUMAN; PH; PRIORITY JOURNAL; RAT;

EID: 0034125617     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0703348     Document Type: Article

References (31)

1. ALBENGRES, E., TILLEMENT, J.P., LE LOUET, H. & MORIN, D. (1998). Trimetazidine: experimental and clinical update review. Cardiovasc. Drug Rev., 16, 359-390.
2. AVDEEF, A. (1992). pH-metric log P. Part 1. Difference plots for determining ion-pair octanol-water partition coefficients of multiprotic substances. Quant. Struct-Act Relat., 11, 510-517.
3. 3H]pentazocine binding to guinea pig cerebellum by divalent cations. Mol. Pharmacol., 42, 882-889.
4. BERNARDI, P. (1996). The permeability transition pore. Control points of a cyclosporin A-sensitive mitochondrial channel involved in cell death. Biochim. Biophys. Acta, 1275, 5-9.
5. BERNARDI, P., VERONESE, P. & PETRONILLI, V. (1993). Modulation of the mitochondrial cyclosporin A-sensitive permeability transition pore. J. Biol. Chem., 268, 1005-1010.
6. CLARKE, F.H. & CAHOON, N.M. (1987). Ionization constants by curve fitting: determination of partition and distribution coefficients of acids and bases and their ions. J. Pharm. Sci., 76, 611-620.
7. DEHAVEN-HUDKINS, D.L., LANYON, L.F., FORD-RICE, F.Y. & ATOR, M.A. (1994). σ recognition sites in brain and peripheral tissues; Characterization and effects of cytochrome P450 inhibitors. Biochem. Pharmacol., 47, 1231-1239.
8. DETRY, J.M. (1993). Clinical features of an anti-anginal drug in angina pectoris. Eur. Heart J., 14 (suppl G), 18-24.
9. 2+-dependent mitochondrial swelling. Fundam. Clin. Pharmacol., 11, 440-447.
10. ELIMADI, A., SETTAF, A., MORIN, D., SAPENA, R., LAMCHOURI, F., CHERRAH, Y. & TILLEMENT, J.P. (1998). Trimetazidine counteracts the hepatic injury associated with ischemia-reperfusion by preserving mitochondrial function. J. Pharmacol. Exp. Ther., 286, 23-28.
11. GUARNIERI, C. & MUSCARI, C. (1993). Effect of trimetazidine on mitochondrial functions and oxidative damage during reperfusion of ischemic hypertrophied rat myocardium. Pharmacology, 46, 324-331.
12. ITZHAK, Y., STEIN, I., ZHANG, S.H., KASSIM, C.O. & CRISTANTE, D. (1991). Binding of σ-ligands to C57BL/6 mouse brain membranes: effects of monoamine oxidase inhibitors and subcellular distribution studies suggest the existence of σ-receptor subtypes. J. Pharmacol. Exp. Ther., 257, 141-148.
13. 3H]-(+)-3-PPP σ binding sites in guinea pig brain membranes. Eur. J. Pharmacol., 176, 247-248.
14. a's and partition and drug distribution coefficients of narcotics and narcotic antagonists and their pH and temperature dependence. J. Med. Chem., 18, 647-655.
15. KLEIN, M. & MUSACCHIO, J.M. (1989). High affinity dextromethorphan binding sites in guinea pig brain. Effect of sigma ligandsand other agents. J. Pharmacol. Exp. Ther., 251, 207-215.
16. LOWRY, O.H., ROSEBROUGH, N.J., FARR, A.L. & RANDALL, R.J. (1951). Protein measurement with the folin phenol reagent. J. Biol. Chem., 93, 265-275.
17. 1 receptor agonist. CNS Drugs Reviews, 4, 1-24.
18. 1 receptor agonist. Eur. J. Pharmacol., 306, 271-279.
19. MAURICE, T. & LOCKHART, B.P. (1997). Neuroprotective and antiamnesic potentials of sigma (σ) receptors ligands. Prog. Neuropsychopharmacol. Biol. Psychiat., 21, 69-102.
20. 3H]SKF-10,047 binding sites (sigma sites) exhibit a unique distribution in rat brain subcellular fractions. Eur. J. Pharmacol., 188, 211-218.
21. MCCANN, D.J., WEISSMAN, A.D. & SU, T.P. (1994). Sigma-1 and Sigma-2 sites in rat brain: comparison of regional, ontogenic, and subcellular patterns. Synapse, 17, 182-189.
22. 3H]-trimetazidine binding sites involved in the regulation of the mitochondrial permeability transition pore. Brit. J. Pharmacol., 123, 1385-1394.
23. QUIRION, R., BOWEN, W.D., ITZHAK, Y., JUNIEN, J.L., MUSACCHIO, J.M., ROTHMAN, R.B., SU, T.P., TAM, S.W. & TAYLOR, D.C. (1992). A proposal for the classification of sigma binding sites. Trends Pharmacol. Sci., 13, 85-86.
24. REYMOND, F., STEYAERT, G., CARRUPT, P.A., MORIN, D., TILLEMENT, J.P., GIRAULT, H.H. & TESTA, B. (1999). The pH-partition profile of the antiischemic drug trimetazidine may explain its reduction of intracellular acidosis. Pharm. Res., 16, 616-624.
25. SALDUCCI, D., CHAUVET-MONGES, A.M., TILLEMENT, J.P., ALBENGRES, E., TESTA, B., CARRUPT, P.A. & CREVAT, A. (1996). Trimetazidine reverses calcium accumulation and impairment of phosphorylation induced by cyclosporine A in isolated rat liver mitochondria. J. Pharmacol. Exp. Ther., 277, 417-422.
26. SIMS, N.R. (1990). Rapid isolation of metabolically active mitochondria from rat brain and subregions using Percoll density gradient centrifugation. J. Neurochem., 55, 698-707.
27. SWILLENS, S., WAELBROECK, M. & CHAMPEIL, P. (1995). Does a radioligand bind to a homogeneous population of non-interacting receptor sites? Trends Pharmacol. Sci., 16, 151-155.
28. URIEN, S. (1995). Micropharm-K, a microcomputer interactive program for the analysis and simulation of pharmacokinetic processes. Pharm. Res., 12, 1225-1230.
29. WEILAND, G.A. & MOLINOFF, P.B. (1981). Minireview: quantitative analysis of drug-receptor interactions: I. Determination of kinetic and equilibrium properties. Life Sci., 29, 313-330.
30. WHITTEMORE, E.R., ILYIN, V.I. & WOODWARD, R.M. (1997). Antagonism of N-methyl-D-aspartate receptors by σ site ligands: potency, subtype-selectivity and mechanisms of inhibition. J. Pharmacol. Exp. Ther., 282, 326-338.
31. ZORATTI, M. & SZABO, I. (1995). The mitochondrial permeability transition. Biochim. Biophys. Acta, 1241, 139-176.