GBR 12935 is a potent, and selectivedopaminereuptake inhibitor, with the binding constant (K_d) of 1.08 nM in COS-7 cells. GBR 12935 stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 also prevents the d-Fenfluramine-induced head-twitch response in mice^[1][2][3][4].

GBR 12909 (10-100 nM) also shows a high affinity for CYP2D6 with the K_dvalue of 42.2 nM, lower than the affinity for dopamine transporter. The binding effect can be reduced byQuinidine(HY-B1751) andQuinine(HY-D0143), which are the specific and potent inhibitors of CYPZD enzymatic activities^[1].
GBR 12935 (10 nM; 2 min) increases the extracellular levels of dopamine to approximately 400% of basal during the application in the nucleus accumbens^[2].
GBR 12935 (100 μM; 60 min) increases extracellular levels of dopamine compared with levels for artificial cerebrospinal fluid (ACSF) by local perfusion for 60 min^[2].
GBR 12935 (1-9 nM) dose-dependently inhibits active uptake of [³H]dopamine in homogenates of the nucleus accumbens^[2].
Co-perfusion of 100 μM GBR 12935 with either 100 μMSulpiride(HY-B1019) orRaclopride(HY-103414) produces a significant reduction in the GBR 12935 induced increase in the extracellular levels of dopamine to basal levels^[2].

GBR 12935 (1-32 mg/kg; repeat injection; 7 d) elevates locomotion activity to a greater extent in C57BL/6J mice than DBA/2J mice, and (10 mg/kg; injection; 7 d) results few mice sensitized to cocaine-induced stereotypy with repeated injections^[3].

414.58

C₂₈H₃₄N₂O

76778-22-8

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