GBR 12909 dihydrochloride

Catalog # Availability Size / Price Qty
0421/10
0421/50
Dopamine Transporter Inhibitors Small Molecule
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Description: Selective DA uptake inhibitor; also σ ligand

Chemical Name: 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride

Purity: ≥98%

Product Details
Citations (12)
Supplemental Products
Reviews (1)

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citations for GBR 12909 dihydrochloride

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

12 Citations: Showing 1 - 10

  1. Pharmacological Chaperones of the DA Transporter Rescue DA Transporter Deficiency Syndrome Mutations in Heterologous Cells.
    Authors: Beerepoot Et al.
    J Biol Chem  2016;291:22053
  2. Spinal DArgic projections control the transition to pathological pain plasticity via a D1/D5-mediated mechanism.
    Authors: Kim Et al.
    J Neurosci  2015;35:6307
  3. Dysfunctional DArgic neurotransmission in asocial BTBR mice.
    Authors: Squillace Et al.
    Transl Psychiatry  2014;4:e427
  4. Enhanced synthesis and release of DA in transgenic mice with gain-of-function α6* nAChRs.
    Authors: Wang Et al.
    J Neurochem  2014;129:315
  5. 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
  6. Differential regulation of MeCP2 phosphorylation in the CNS by DA and serotonin.
    Authors: Hutchinson Et al.
    J Neurosci  2012;37:321
  7. 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
  8. The plasma membrane-associated GTPase Rin interacts with the DA transporter and is required for protein kinase C-regulated DA transporter trafficking.
    Authors: Navaroli Et al.
    J Neurosci  2011;31:13758
  9. 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
  10. Impact of serotonin 2C receptor null mutation on physiology and behavior associated with nigrostriatal DA pathway function.
    Authors: Abdallah Et al.
    Br J Pharmacol  2009;29:8156

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GBR used as a selective DAT blocker for increasing dopamine release
By Anonymous on 05/15/2018
Species: Mouse

GBR-12909 (300 nM) was used as a DAT blocker in slice voltametry experiments. It's difficult to get into solution. Just use some warming.

PMID: 28115487

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