Catalog Number: 0421
Chemical Name: 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride
Biological Activity
Potent, competitive inhibitor of dopamine uptake (Ki = 1 nM for inhibition of striatal dopamine uptake). Has > 100-fold lower affinity for the noradrenalin and 5-HT uptake carriers. Also a potent sigma ligand (IC50 = 48 nM). Centrally active following systemic administration.
Technical Data
  • M.Wt:
    523.49
  • Formula:
    C28H32F2N2O.2HCl
  • Solubility:
    Soluble to 5 mM in water with gentle warming and to 50 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    67469-78-7
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. The dopamine uptake inhibitor GBR12909: selectivity and molecular mechanism of action.
    Andersen
    Eur.J.Pharmacol., 1989;166:493
  2. GBR-12909 and fluspirilene potently inhibited binding of [3H] (+)3-PPP to sigma receptors in rat brain.
    Contreras et al.
    Life Sci., 1990;47:PL133
  3. Pharmacological characterization of the discriminative-stimulus effects of GBR 12909.
    Spealman and Melia
    J.Pharmacol.Exp.Ther., 1991;258:626
  4. Behavioral properties of GBR 12909, GBR 13069 and GBR 13098: specific inhibitors of dopamine uptake.
    Heikkila and Manzino
    Eur.J.Pharmacol., 1984;103:241
Citations:

The citations listed below are publications that use Tocris products. Selected citations for GBR 12909 dihydrochloride include:

11 Citations: Showing 1 - 10
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  1. Spinal dopaminergic projections control the transition to pathological pain plasticity via a D1/D5-mediated mechanism.
    Authors: Kim Et al.
    J Neurosci 2015;35:6307
  2. Dysfunctional dopaminergic neurotransmission in asocial BTBR mice.
    Authors: Squillace Et al.
    Transl Psychiatry 2014;4:e427
  3. Enhanced synthesis and release of dopamine in transgenic mice with gain-of-function α6* nAChRs.
    Authors: Wang Et al.
    J Neurochem 2014;129:315
  4. Soluble interleukin-6 receptor induces motor stereotypies and co-localizes with gp130 in regions linked to cortico-striato-thalamo-cortical circuits.
    Authors: Patel Et al.
    PLoS One 2012;7:e41623
  5. Differential regulation of MeCP2 phosphorylation in the CNS by dopamine and serotonin.
    Authors: Hutchinson Et al.
    J Neurosci 2012;37:321
  6. Progressive neurodegeneration or endogenous compensation in an animal model of Parkinson's disease produced by decreasing doses of alpha-synuclein.
    Authors: Koprich Et al.
    PLoS One 2011;6:e17698
  7. The plasma membrane-associated GTPase Rin interacts with the dopamine transporter and is required for protein kinase C-regulated dopamine transporter trafficking.
    Authors: Navaroli Et al.
    J Neurosci 2011;31:13758
  8. Expression of human A53T alpha-synuclein in the rat substantia nigra using a novel AAV1/2 vector produces a rapidly evolving pathology with protein aggregation, dystrophic neurite architecture and nigrostriatal degeneration with potential to model the pat
    Authors: Koprich Et al.
    Mol Neurodegener 2010;5:43
  9. Impact of serotonin 2C receptor null mutation on physiology and behavior associated with nigrostriatal dopamine pathway function.
    Authors: Abdallah Et al.
    Br J Pharmacol 2009;29:8156
  10. Electrophysiology and pharmacology of striatal neuronal dysfunction induced by mitochondrial complex I inhibition.
    Authors: Costa Et al.
    J Neurosci 2008;28:8040
  11. PYM50028, a novel, orally active, nonpeptide neurotrophic factor inducer, prevents and reverses neuronal damage induced by MPP+ in mesencephalic neurons and by MPTP in a mouse model of Parkinson's disease.
    Authors: Visanji Et al.
    FASEB J 2008;22:2488
Expand to show all 11 Citations

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