GBR-12935 explained

GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor. It was originally developed in its ³H radiolabelled 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]}

See also

• Vanoxerine
• GBR-12783
• GBR-13069
• GBR-13098
• DBL-583

Notes and References

1. Berger P, Janowsky A, Vocci F, Skolnick P, Schweri MM, Paul SM . [3H]GBR-12935: a specific high affinity ligand for labeling the dopamine transport complex . European Journal of Pharmacology . 107 . 2 . 289–90 . January 1985 . 3979428 . 10.1016/0014-2999(85)90075-5 .
2. Janowsky A, Vocci F, Berger P, Angel I, Zelnik N, Kleinman JE, Skolnick P, Paul SM . 6 . [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 . August 1987 . 3598589 . 10.1111/j.1471-4159.1987.tb02908.x . 25654981 .
3. Zhu J, Green T, Bardo MT, Dwoskin LP . 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 . January 2004 . 14684252 . 10.1016/s0166-4328(03)00190-6 . 20382190 .
4. Swant J, Wagner JJ . Dopamine transporter blockade increases LTP in the CA1 region of the rat hippocampus via activation of the D3 dopamine receptor . Learning & Memory . 13 . 2 . 161–7 . 16585791 . 1409827 . 10.1101/lm.63806 . 2006 .
5. Hsin LW, Chang LT, Rothman RB, Dersch CM, Jacobson AE, Rice KC . Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: role of amino, fluoro, hydroxyl, methoxyl, methyl, methylene, and oxo substituents on affinity for the dopamine and serotonin transporters . Journal of Medicinal Chemistry . 51 . 9 . 2795–806 . May 2008 . 18393401 . 5548119 . 10.1021/jm701270n .