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GBR-12935
Systematic (IUPAC) name
1-(2-(diphenylmethoxy)ethyl)-4-(3-phenylpropyl)piperazine
Identifiers
CAS number 76778-22-8
ATC code  ?
PubChem 3456
Chemical data
Formula C 28H34N2O 
Mol. mass 414.582 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

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

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. 1985 Jan 2;107(2):289-90. PMID 3979428
  2. ^ Janowsky A, Vocci F, Berger P, Angel I, Zelnik N, Kleinman JE, Skolnick P, Paul SM. [3H]GBR-12935 binding to the dopamine transporter is decreased in the caudate nucleus in Parkinson's disease. Journal of Neurochemistry. 1987 Aug;49(2):617-21. PMID 3598589
  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. 2004 Jan 5;148(1-2):107-17. PMID 14684252
  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 and Memory. 2006 Mar-Apr;13(2):161-7. PMID 16585791
  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. 2008 May 8;51(9):2795-806. PMID 18393401
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