Effects of GBR 12909, a selective dopamine uptake inhibitor, on motor activity and operant behavior in the rat
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Modafinil acquires reinforcing effects when combined with citalopram
2022, Pharmacology Biochemistry and BehaviorCitation Excerpt :GBR 12909 is a selective substance that inhibits DAT, so it increases only dopamine levels. It has been described as having fewer reinforcing and differential properties than drugs like cocaine (Kelley and Lang, 1989; Tella et al., 1996; Achterberg et al., 2016). Although GBR 12909 increases MA in a way similar to cocaine (Rothman and Grieg, 1998), it does not produce motor sensitization or tolerance (Melnick et al., 2001), perhaps because the neuroadaptations that it induces in the dopaminergic system are distinct from those of cocaine (Tella et al., 1996).
Electrical high frequency stimulation modulates GABAergic activity in the nucleus accumbens of freely moving rats
2015, Neurochemistry InternationalCitation Excerpt :Behavioral scoring was performed on video recordings of the experiment. Different behavioral patterns were documented as previously described by various authors (Andersen et al., 1987; Kelley and Lang, 1989; Westerink et al., 1987). The behavioral activity was classified in three categories of arbitrary units scored from 0 to 2 (0 = absent, 1 = moderate, 2 = marked).
Contribution of the mGluR7 receptor to antiparkinsonian-like effects in rats: A behavioral study with the selective agonist AMN082
2013, Pharmacological ReportsCitation Excerpt :In contrast, selective DAT inhibitors abolish akinesia in this model [11, 33]; however, since the affinity of Met-1 for DAT is ca. 10 times lower than for SERT, a potential benefit of DAT inhibition may be masked by the effects induced by SERT blockade. Furthermore, DAT inhibitors are known to elevate extracellular DA levels in the striatum and to potentiate locomotion [13, 26]. Since AMN082 is unable to increase either striatal DA release [20] or locomotion (our study), its effect related to DAT inhibition also seems questionable.
Behavioural characterisation of the effects of acute and repeated administration of GBR 12909 in rats: Further evaluation of a potential model of ADHD
2009, NeuropharmacologyCitation Excerpt :The results suggest that acute GBR 12909-induced hyperactivity and increased rearing is possibly due to its' potent ability to selectively block the dopamine transporter and thus inhibit dopamine reuptake resulting in enhanced dopaminergic neuronal transmission at postsynaptic receptors. Indeed this is consistent with previous reports in adult rats (Heikkila and Manzino, 1984; Kelley and Lang, 1989; Hooks et al., 1994) where rats displayed enhanced locomotor responses to acute GBR 12909 sustained for up to 7 weeks following discontinuation of a 14 day treatment regime (Kelley and Lang, 1989). Considering the potency of GBR 12909 to inhibit DAT and the high dose of the drug used, it is probable that this repeated dosing regime caused alterations in the affinity of the drug for the DAT site and indeed it has been reported that GBR 12909 may produce conformational changes in the transporter protein (Stepanov and Järv, 2008).
Altered dopaminergic profiles: Implications for the regulation of voluntary physical activity
2009, Behavioural Brain Research