GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor. It was originally developed in its 3Hradiolabelled form for the purpose of mapping the distribution of dopaminergic neurons in the brain by selective labelling of dopamine transporter proteins.[1] This has led to potential clinical uses in the diagnosis of Parkinson's disease,[2] although selective radioligands such as Ioflupane (123I) are now available for this application. GBR-12935 is now widely used in animal research into Parkinson's disease and the dopamine pathways in the brain.[3][4][5]
^Berger P, Janowsky A, Vocci F, Skolnick P, Schweri MM, Paul SM (January 1985). "[3H]GBR-12935: a specific high affinity ligand for labeling the dopamine transport complex". European Journal of Pharmacology. 107 (2): 289–90. doi:10.1016/0014-2999(85)90075-5. PMID3979428.
^Janowsky A, Vocci F, Berger P, Angel I, Zelnik N, Kleinman JE, et al. (August 1987). "[3H]GBR-12935 binding to the dopamine transporter is decreased in the caudate nucleus in Parkinson's disease". Journal of Neurochemistry. 49 (2): 617–21. doi:10.1111/j.1471-4159.1987.tb02908.x. PMID3598589. S2CID25654981.
^Zhu J, Green T, Bardo MT, Dwoskin LP (January 2004). "Environmental enrichment enhances sensitization to GBR 12935-induced activity and decreases dopamine transporter function in the medial prefrontal cortex". Behavioural Brain Research. 148 (1–2): 107–17. doi:10.1016/s0166-4328(03)00190-6. PMID14684252. S2CID20382190.