This work was supported in part by a grant from D.R.E.T. (contract 95-167). We thank Dr. R. G. Duggleby for helpful discussions.

  • 1
    Andersen P.H. (1989) The dopamine uptake inhibitor GBR 12909 : selectivity and molecular mechanism of action.Eur. J. Pharmacol. 166,493504.
  • 2
    Billaud G., Costentin J., Bonnet J. -J. (1993) Specific binding of [3H]GBR 12783 to the dopamine neuronal carrier included in polarized membranes. Eur. J. Pharmacol. 247,333340.
  • 3
    Billaud G., Menard J., Marcellin N., Kamenka J., Costentin J., Bonnet J. -J. (1994) Thermodynamics of the binding of BTCP (GK13) and related derivatives on the dopamine neuronal carrier.Eur. J. Pharmacol. 268,357363.
  • 4
    Boja J.W., Mitchell W.M., Patel A., Kopajtic T.A., Carroll F.I., Lewin A.H., Abraham P., Kuhar M.J. (1992) High-affinity binding of [125I]RTI-55 to dopamine and serotonin transporters in rat brain. Synapse 12,2736.
  • 5
    Bonnet J. & Costentin J. (1986) GBR 12783, a potent and selective inhibitor of dopamine uptake : biochemical studies in vivo and exvivo.Eur. J. Pharmacol. 121,199209.
  • 6
    Bonnet J., Lemasson M., Costentin J. (1984) Simultaneous evaluation by a double labelling method of drug-induced uptake inhibition and release of dopamine in synaptosomal preparation of rat striatum.Biochem. Pharmacol. 33,21292135.
  • 7
    Bonnet J., Protais P., Chagraoui A., Costentin J. (1986) High-affinity [3H]GBR 12783 binding to a specific site associated with the neuronal dopamine uptake complex in the central nervous system. Eur. J. Pharmacol. 126,211222.
  • 8
    Bonnet J., Benmansour S., Costentin J., Parker E.J., Cubeddu L.X. (1990) Thermodynamic analyses of the binding of substrates and uptake inhibitors on the neuronal carrier of dopamine labeled with [3H]GBR 12783 or [3H]mazindol. J. Pharmacol. Exp. Ther. 253,12061214.
  • 9
    Carroll F.I., Lewin A.H., Kuhar M.J. (1997) Dopamine transporter uptake blockers. Structure-activity relationships, in Neurotransmitter Transporters.Structure, Function and Regulation (Reith M. E. A., ed), pp. 263295. Humana Press, Totowa, New Jersey.
  • 10
    Heikkila R.E., Orlansky H., Cohen G. (1975) Studies on the distinction between uptake inhibition and release of [3H]dopamine in rat brain tissue slices. Biochem. Pharmacol. 24,847852.
  • 11
    Héron C., Costentin J., Bonnet J. -J. (1994) Evidence that pure uptake inhibitors including cocaine interact slowly with the dopamine neuronal carrier.Eur. J. Pharmacol. 264,391398.
  • 12
    Héron C., Billaud G., Costentin J., Bonnet J. -J. (1996) Complex ionic control of [3H]GBR 12783 binding to the dopamine neuronal carrier. Eur. J. Pharmacol. 301,195202.
  • 13
    Kuhar M.J., Ritz M.C., Boja J.W. (1991) The dopamine hypothesis of the reinforcing properties of cocaine.Trends Neurosci. 14,299302.
  • 14
    Lowry O.H., Rosebrough N.J., Farr A.L., Randall R.J. (1951) Protein measurement with the Folin phenol reagent.J. Biol. Chem. 193,265275.
  • 15
    Madras B.K., Fahey M.A., Bergman J., Canfield D.R., Spealman R.D. (1989) Effects of cocaine and related drugs in nonhuman primates. I. [3H]Cocaine binding sites in caudate-putamen. J. Pharmacol. Exp. Ther. 251,131141.
  • 16
    Morrison J.F. & Walsh C.T. (1988) The behavior and significance of slow-binding enzyme inhibitors, inAdvances in Enzymology and Related Areas of Molecular Biology,Vol. 61 (Meister A., ed), pp. 201301. J. Wiley and Sons, New York.
  • 17
    Raiteri M., Cerrito F., Cervoni A.M., Levi G. (1979) Dopamine can be released by two mechanisms differentially affected by the dopamine transport inhibitor nomifensine.J. Pharmacol. Exp. Ther. 208,195202.
  • 18
    Reith M.E.A., Sershen H., Lajtha A. (1986) Binding sites for [3H]cocaine in mouse striatum and cerebral cortex have different dissociation kinetics. J. Neurochem. 46,309312.
  • 19
    Ritz M.C., Lamb R.J., Goldberg S.R., Kuhar M.J. (1987) Cocaine receptors on dopamine transporters are related to self-administration of cocaine.Science 237,12191223.
  • 20
    Rocha B.A., Fumagalli F., Gainetdinov R.R., Jones S.R., Ator R., Giros B., Miller G.W., Caron M.G. (1998) Cocaine self-administration in dopamine-transporter knockout mice.Nat. Neurosci. 1,132137.
  • 21
    Rothman R.B., Mele A., Reid A.A., Akunne H., Greig N., Thurkauf A., Rice K.C., Pert A. (1989) Tight binding dopamine reuptake inhibitors as cocaine antagonists. A strategy for drug development.FEBS Lett. 257,341344.
  • 22
    Rothman R.B., Mele A., Reid A.A., Akunne H.C., Greig N., Thurkauf A., De Costa B.R., Rice K.C., Pert A. (1991) GBR 12909 antagonizes the ability of cocaine to elevate extracellular levels of dopamine.Pharmacol. Biochem. Behav. 40,387397.
  • 23
    Saadouni S., Refahi-Lyamani F., Costentin J., Bonnet J. -J. (1994) Cocaine and GBR 12783 recognize nonidentical, overlapping binding domains on the dopamine neuronal carrier.Eur. J. Pharmacol. 268,187197.
  • 24
    Schwarz G. (1978) Estimating the dimension of a model.Ann. Stat. 6,461464.
  • 25
    Szedlacsek S.E. & Duggleby R.G. (1995) Kinetics of slow and tight-binding inhibitors, inMethods in Enzymology,Vol. 249 (Purich D. L., ed), pp. 144180. Academic Press, San Diego.
  • 26
    Trendelenburg U. (1991) Functional aspects of the neuronal uptake of noradrenaline.Trends Pharmacol. Sci. 121,334337.
  • 27
    Van der Zee P., Koger H.S., Gootjes J., Hespe W. (1980) Aryl 1,4-dialk(en)ylpiperazines as selective and very potent inhibitors of dopamine uptake.Eur. J. Med. Chem. 15,363370.
  • 28
    Vignon J., Pinet V., Cerruti C., Kamenka J., Chicheportiche R. (1988) [3H]BTCP : a new phencyclidine analog selective for the dopamine uptake complex. Eur. J. Pharmacol. 148,427436.
  • 29
    Xu C., Coffey L.L., Reith M.E.A. (1995) Translocation of dopamine and binding of 2β-carbomethoxy-3β-(4-fluorophenyl)-tropane (WIN 35,428) measured under identical conditions in rat striatal synaptosomal preparations. Inhibition by various blockers. Biochem. Pharmacol. 49,339350.
  • 30
    Zimanyi I., Lajtha A., Reith M.E.A. (1989) Comparison of characteristics of dopamine uptake and mazindol binding in mouse striatum.Naunyn Schmiedebergs Arch. Pharmacol. 340,626632.