Short communicationGBR 12909 and 12935 block dopamine uptake into brain synaptic vesicles as well as nerve endings
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Cited by (27)
Prolonged dopamine D<inf>3</inf> receptor stimulation promotes dopamine transporter ubiquitination and degradation through a PKC-dependent mechanism
2021, Pharmacological ResearchCitation Excerpt :A range of temperatures (25−35 °C), incubation times (5−30 min) and striatal protein concentrations (0.2−3 μg/μl) were checked in order to establish the working parameters in the linear ascending segment of the uptake curve. Fifty microliters of synaptosomal suspension (0.5 μg total protein/μl in striatal samples, 1 μg total protein/μl in cells) were preincubated in assay buffer with or without the selective DAT inhibitor GBR 12,935 [42] (10 μM, 30 °C, 5 min; #G9659; Sigma;). Subsequently, 20 nM [3H]-DA (final concentration; #NET131250UC; PerkinElmer, Waltham, MA) was added to each tube.
N-phenylpropyl-N′-substituted piperazines occupy sigma receptors and alter methamphetamine-induced hyperactivity in mice
2016, Pharmacology Biochemistry and BehaviorCitation Excerpt :To measure occupancy of DAT, groups of mice (n = 4–5 mice/group) received saline or test ligand (10 μmol/kg) injection (i.p.) 1 min prior to [125I]RTI-121. A separate group was administered the DAT inhibitor GBR-12909 (10 μmol/kg, i.p.) as a positive control condition (Reith et al., 1994). In both studies, groups of mice were euthanized 30 min after radioligand administration.
Olfactory Stimulation Selectively Modulates the OFF Pathway in the Retina of Zebrafish
2013, NeuronCitation Excerpt :To test further the idea that activation of the ORC acts by decreasing dopamine level in the retina, we attempted to prevent these changes without interfering with the activity of dopamine receptors. Our strategy was to inject vanoxerine (GBR 12909; 2 μM), a potent and specific blocker of the transporters involved in dopamine reuptake from extracellular space and into secretory vesicles (Reith et al., 1994; Singh, 2000). Vanoxerine administration has been reported to result in a small but steady increase in extracellular dopamine concentration, followed by a persistent “clamp” once both uptake and release are blocked (Rothman et al., 1991; Lima et al., 1994; Reith et al., 1994; Schlicker et al., 1996; Kubrusly et al., 2008).
Effect of daily dosing duration of direct and indirect dopamine receptor agonists: Cocaine cross-tolerance following chronic regimens
2002, European NeuropsychopharmacologyDopamine induces ERK activation in renal epithelial cells through H<inf>2</inf>O<inf>2</inf> produced by monoamine oxidase
2001, Kidney InternationalCitation Excerpt :After a 48-hour period to allow attachment, cells were made quiescent by incubation for an additional 24-hour period in serum-free medium (DME/Ham's F-12 medium for rat proximal tubule cells and DMEM for HEK 293 cells). Cells were pretreated with or without appropriate compounds [the monoamine oxidase inhibitor pargyline, the antioxydant N-acetylcysteine (NAC)15, the MEKK inhibitor PD 9805929, and the specific DA uptake inhibitor GBR 12909]30,31 for 30 minutes and treated with DA or tyramine in the presence of 1 μCi/mL of [3H]thymidine for 24 hours. Cells were then washed twice with 1 mL HBSS to remove unincorporated [3H]thymidine and were subjected to ice-cold 5% trichloracetic acid (wt/vol) for 15 minutes.
Specificity and ion dependence of binding of GBR analogs
1998, Methods in Enzymology