GBR 12935 dihydrochloride (CAS 67469-81-2)

GBR 12935 dihydrochloride inhibits DAT (dopamine transporter) (K_i = 21.5 nM) and SLC6A2 (norepinephrine transporter) (K_i = 225 nM). GBR 12935 does not inhibit the serotonin transporter (K_i = 6.5 μM). GBR 12935 binds to a nondopaminergic piperazine site in blood platelets and brain that has been identified as cytochrome P450.

References

Andersen et al (1987) Biochemical and pharmacological characterization of [3H]GBR 12935 binding in vitro to rat striatal membranes: labelling of the dopamine uptake complex. J.Neurochem. 48 1887. Reith et al (1992) Evidence for mutually exclusive binding of cocaine, BTCP, GBR 12935, and dopamine to the dopamine transporter. Eur.J.Pharmacol.Mol.Pharmacol.Sect. 227 417. Reith et al (1994) GBR 12909 and 12935 block dopamine uptake into brain synaptic vesicles as well as nerve endings. Eur.J.Pharmacol. 253 175.