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GBR 12783 is a dopamine uptake inhibitor (IC50 = 13 nM in rat striatal synaptosomes).1 It is selective for inhibition of dopamine uptake over norepinephrine or serotonin (5-HT) uptake (IC50s = 230 and 1,100 nM in rat hypothalamic and striatal synaptosomes, respectively). GBR 12783 (10 mg/kg, i.p.) improves learning and memory in the passive avoidance test in rats, an effect that can be blocked by the anticholinergic agent scopolamine.2 It increases locomotor activity, reduces pentobarbital-induced sleep duration, and decreases immobility time in the forced swim test, in mice.3 GBR 12783 (10 mg/kg) inhibits catalepsy induced by the antipsychotic haloperidol (Item No. 12014) in rats.
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1. GBR 12783, a potent and selective inhibitor of dopamine uptake: Biochemical studies in vivo and ex vivo. Eur. J. Pharmacol. 121(2), 199-209 (1986).
2. The specific dopamine uptake inhibitor GBR 12783 improves learning of inhibitory avoidance and increases hippocampal acetylcholine release. Brain Res. Cogn. Brain Res. 7(2), 203-205 (1998).
3. Comparison of the effects of three indirect dopamine agonists, GK 13, GBR 12783 and dexamphetamine on behavioural tests involving central catecholaminergic transmissions. Psychopharmacology (Berl) 101(3), 344-353 (1990).