GBR 12935 CAS NO.67469-81-2

gbr 12935 2hcl is a potent, and selective dopamine reuptake inhibitor.
ic50 value:
target: dopamine reuptake inhibitor
in vitro: the calculated kd of [3h]gbr-12935 binding to cyp2d6 was 42.2 nm, indicating that gbr-12935 has a high affinity for cyp2d6. the binding of [3h]gbr-12935 to cyp2d6 was decreased partially by substrates or inhibitors of cyp2d isoforms (quinine, quinidine, propranolol, bufuralol, imipramine, and desipramine) [1]. co-perfusion of 100 microm gbr 12909 or gbr 12935 with either 100 microm sulpiride or raclopride produced a significant reduction in the gbr 12909 or gbr 12935 induced increase in the extracellular levels of dopamine to basal levels. in vitro, gbr 12909 (1-9 nm) dose-dependently inhibited active uptake of [3h]dopamine in homogenates of the nucleus accumbens [2].
in vivo: gbr 12935 elevated locomotion to a greater extent in c57bl/6j mice at the maximally active dose of 10 mg/kg. locomotor stimulation by gbr 12935 remained consistent in both strains with repeated injections. dba/2j mice became sensitized to cocaine-induced stereotypy with repeated injections. cocaine induced no stereotypy in c57bl/6j mice on any test day. no stereotypies were induced by gbr 12935 in either strain on any test day [3].