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GBR 12935 is an inhibitor of dopamine uptake that binds to the dopamine transporter (Kd = 27.2 nM).1,2 It is selective for the dopamine transporter over the serotonin and norepinephrine transporters (Kds = 940 and 310 nM, respectively).1 In mice, it increases locomotor activity, but not stereotypic behavior, when administered at a dose of 10 mg/kg but induces gnawing at levels similar to other indirect dopamine agonists with an ED50 value of 17.1 mg/kg.2,3
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1. Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur. J. Pharmacol. 340(2-3), 249-258 (1997).
2. Differential effects of direct and indirect dopamine agonists on the induction of gnawing in C57Bl/6J mice. J. Pharmacol. Exp. Ther. 273(1), 7-15 (1995).
3. Comparison of cocaine and GBR 12935: Effects on locomotor activity and stereotypy in two inbred mouse strains. Pharmacol. Biochem. Behav. 48(3), 733-739 (1994).