GBR 12909 dihydrochloride

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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% (HPLC)
Citations (12)
Reviews (1)
Literature (3)

Biological Activity for GBR 12909 dihydrochloride

GBR 12909 dihydrochloride is a potent, competitive inhibitor of dopamine uptake (Ki = 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.

Compound Libraries for GBR 12909 dihydrochloride

GBR 12909 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GBR 12909 dihydrochloride

M. Wt 523.49
Formula C28H32F2N2O.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 67469-78-7
PubChem ID 104920

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.

Solubility Data for GBR 12909 dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 2.62 5 with gentle warming
DMSO 26.17 50

Preparing Stock Solutions for GBR 12909 dihydrochloride

The following data is based on the product molecular weight 523.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 3.82 mL 19.1 mL 38.21 mL
2.5 mM 0.76 mL 3.82 mL 7.64 mL
5 mM 0.38 mL 1.91 mL 3.82 mL
25 mM 0.08 mL 0.38 mL 0.76 mL

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Product Datasheets for GBR 12909 dihydrochloride

Certificate of Analysis / Product Datasheet
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References for GBR 12909 dihydrochloride

References are publications that support the biological activity of the product.

Andersen (1989) The DA uptake inhibitor GBR12909: selectivity and molecular mechanism of action. Eur.J.Pharmacol. 166 493 PMID: 2530094

Contreras et al (1990) GBR-12909 and fluspirilene potently inhibited binding of [3H] (+)3-PPP to sigma receptors in rat brain. Life Sci. 47 PL133 PMID: 1980329

Heikkila and Manzino (1984) Behavioral properties of GBR 12909, GBR 13069 and GBR 13098: specific inhibitors of DA uptake. Eur.J.Pharmacol. 103 241 PMID: 6237922

Spealman and Melia (1991) Pharmacological characterization of the discriminative-stimulus effects of GBR 12909. J.Pharmacol.Exp.Ther. 258 626 PMID: 1678014

If you know of a relevant reference for GBR 12909 dihydrochloride, please let us know.

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12 Citations for GBR 12909 dihydrochloride

Citations are publications that use Tocris products. Selected citations for GBR 12909 dihydrochloride include:

Patel et al (2012) Soluble interleukin-6 receptor induces motor stereotypies and co-localizes with gp130 in regions linked to cortico-striato-thalamo-cortical circuits. PLoS One 7 e41623 PMID: 22911828

Koprich et al (2010) 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 Mol Neurodegener 5 43 PMID: 21029459

Hutchinson et al (2012) Differential regulation of MeCP2 phosphorylation in the CNS by DA and serotonin. J Neurosci 37 321 PMID: 21956448

Beerepoot et al (2016) Pharmacological Chaperones of the DA Transporter Rescue DA Transporter Deficiency Syndrome Mutations in Heterologous Cells. J Biol Chem 291 22053 PMID: 27555326

Do you know of a great paper that uses GBR 12909 dihydrochloride from Tocris? Please let us know.

Reviews for GBR 12909 dihydrochloride

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GBR used as a selective DAT blocker for increasing dopamine release.
By Anonymous on 05/15/2018
Assay Type: Ex Vivo
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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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Dopamine Receptors Scientific Review

Dopamine Receptors Scientific Review

Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.

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