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  • 1
    Electronic Resource
    Electronic Resource
    Binding domains for blockers and substrates on the dopamine transporter in rat striatal membranes studied by protection against N-ethylmaleimide-induced reduction of [3H]WIN 35,428 binding (1996)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 355 (1996), S. 64-73 
    Details
    ISSN: 1432-1912
    Keywords: Key words Dopamine transporter ; WIN 35 ; 428 binding ; N-ethylmaleimide ; Sulfhydryl groups ; Rat striatum
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Binding sites for 2β-carbomethoxy-3β-(4-fluorophenyl)[3H]tropane ([3H]WIN 35,428) on rat striatal membranes were alkylated with N-ethylmaleimide (NEM), and the protective potency was measured of the blockers cocaine, N[1-(2-benzo[b]thiophenyl) cyclohexyl]piperidine (BTCP), benztropine, WIN 35,428, and nomifensine, and of the substrates dopamine, norepinephrine, S(+)-amphetamine, tyramine, and metaraminol. In general, the protective potency was lower (at least 3 times) than the potency in inhibiting [3H]WIN 35,428 binding with the compounds present under the same experimental conditions used for the NEM-induced alkylation. However, the disparity was substantially greater for all substrates tested (10- to 93-fold) than for the blockers (2- to 6-fold), especially cocaine and BTCP (3-fold). [3H]WIN 35,428 binding was best described by a 1-site model under the present conditions. The results are discussed in terms of models involving blocker-induced conformational changes and overlapping nonidentical binding domains for blockers and substrates.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/PL00004919
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  • 2
    Electronic Resource
    Electronic Resource
    Translocation of dopamine and binding of WIN 35, 428 measured under identical conditions in cells expressing the cloned human dopamine transporter (1996)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 354 (1996), S. 295-304 
    Details
    ISSN: 1432-1912
    Keywords: Key words Human dopamine transporter ; WIN 35 ; 428 binding ; Dopamine uptake ; Cocaine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  Translocation of [3H]dopamine and binding of [3H]WIN 35, 428 were measured in intact C6 glioma cells expressing the cloned human dopamine transporter (hDAT) under identical conditions of assay buffer (phosphate-Krebs) and temperature (25 °C) with uptake at initial velocity and binding at equilibrium. In the intact cells, [3H]dopamine uptake was a one-component process; in contrast, [3H]WIN 35, 428 binding included both a high-affinity component, inhibitable by micromolar concentrations of dopamine, and a low-affinity component only partially inhibited by millimolar concentrations of dopamine. Binding (high-affinity) over uptake K i ratios were on the average 2.3 for the inhibitors WIN 35, 428, cocaine, GBR 12909, and BTCP. The potency of dopamine in inhibiting its own translocation was close to that in inhibiting [3H]WIN 35, 428 binding consonant with a more rapid reorientation step of the DAT in the C6-hDAT system than in rat striatal synaptosomes. The similarity in turnover values of the DAT estimated in the current experiments with the C6-hDAT system and in our previous study on rat striatal synaptosomes, performed under comparable conditions, suggest that all DAT’s inserted into the C6 cell membrane are functionally active.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00171060
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Extracellular dopamine, norepinephrine, and serotonin in the ventral tegmental area and nucleus accumbens of freely moving rats during intracerebral dialysis following systemic administration of cocaine and other uptake blockers (1997)
    Springer
    Psychopharmacology 134 (1997), S. 309-317 
    Details
    ISSN: 1432-2072
    Keywords: Key words Microdialysis ; Dopamine ; Serotonin ; Norepinephrine ; Ventral tegmental area ; Nucleus accumbens ; Cocaine ; GBR 12935 ; Desipramine ; Citalopram ; Uptake blockers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Extracellular levels of dopamine (DA), serotonin (5-HT), and norepinephrine (NE) were measured by microdialysis in conscious rats equipped with dual probes, one in the ventral tegmental area (VTA) and another one in the contralateral nucleus accumbens (NACC). Dialysate content of all amines in both regions was essentially abolished by local infusion of tetrodotoxin (1 μM) or Ca2+-free buffer. Injection of the selective DA uptake blocker GBR 12935 (15 mg/kg IP) increased DA, as well as NE and, to a lesser extent, 5-HT in the VTA; it increased DA more than 5-HT in the NACC. The selective NE uptake blocker desipramine (10 mg/kg IP) increased NE but also 5-HT in the VTA and NACC; the DA level was persistently enhanced in the VTA, whereas in the NACC it initially rose and then fell below baseline value. The selective 5-HT uptake blocker citalopram (15 mg/kg IP) was generally more effective in elevating dialysate level of 5-HT than that of other amines in both regions. Cocaine (20 mg/kg IP) was non-selective in enhancing all three amines in both regions. There is considerable crosstalk between monoamine systems occurring upon systemic administration of uptake blockers, and the VTA and NACC are notably different in the time course of the DA effect (long-lasting versus transient).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/s002130050454
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    Paper (German National Licenses)
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