GBR 12909 dihydrochloride

Catalog #: 0421
12 Citations Datasheet / COA / SDS

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0421/10
0421/50

GBR 12909 dihydrochloride | CAS No. 67469-78-7 | Dopamine Transporter Inhibitors

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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%

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Product Details

Citations (12)

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Biological Activity

GBR 12909 dihydrochloride is a potent, competitive inhibitor of dopamine uptake (K_i = 1 nM for inhibition of striatal dopamine uptake). Has >100-fold lower affinity for the noradrenaline 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.

Background References

A New Glucocerebrosidase Chaperone Reduces ?-Synuclein and Glycolipid Levels in iPSC-Derived Dopaminergic Neurons from Patients with Gaucher Disease and Parkinsonism

J Neurosci, 2016;36(28):7441-52.
High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
Sources contributing to the average extracellular concentration of dopamine in the nucleus accumbens.
Owesson-White CA, Roitman MF, Sombers LA, Belle AM, Keithley RB, Peele JL, Carelli RM, Wightman RM
J. Neurochem., 2012;121(2):252-62.
The DA uptake inhibitor GBR12909: selectivity and molecular mechanism of action.
Andersen
Eur.J.Pharmacol., 1989;166:493
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
Behavioral properties of GBR 12909, GBR 13069 and GBR 13098: specific inhibitors of DA uptake.
Heikkila and Manzino
Eur.J.Pharmacol., 1984;103:241
Pharmacological characterization of the discriminative-stimulus effects of GBR 12909.
Spealman and Melia
J.Pharmacol.Exp.Ther., 1991;258:626

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

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

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
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
Dysfunctional DArgic neurotransmission in asocial BTBR mice.
Authors: Squillace Et al.
Transl Psychiatry 2014;4:e427
Enhanced synthesis and release of DA in transgenic mice with gain-of-function α6* nAChRs.
Authors: Wang Et al.
J Neurochem 2014;129:315
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
Differential regulation of MeCP2 phosphorylation in the CNS by DA and serotonin.
Authors: Hutchinson Et al.
J Neurosci 2012;37:321
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
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
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
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

Electrophysiology and pharmacology of striatal neuronal dysfunction induced by mitochondrial complex I inhibition.
Authors: Costa Et al.
J Neurosci 2008;28:8040

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

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