GBR 12909 dihydrochloride

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Cat.No. 0421 - GBR 12909 dihydrochloride | C28H32F2N2O.2HCl | CAS No. 67469-78-7
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)
Datasheet
Citations (12)
Reviews (1)
Literature

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.

Compound Libraries

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

Technical Data

M. Wt 523.49
Formula C28H32F2N2O.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 67469-78-7
PubChem ID 104920
InChI Key MIBSKSYCRFWIRU-UHFFFAOYSA-N
Smiles Cl.Cl.FC1=CC=C(C=C1)C(OCCN1CCN(CCCC2=CC=CC=C2)CC1)C1=CC=C(F)C=C1

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

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

Preparing Stock Solutions

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.

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

Certificate of Analysis / Product Datasheet
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References

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


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View all Dopamine Transporter Inhibitors

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12 Citations for GBR 12909 dihydrochloride

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

Wang et al (2014) Enhanced synthesis and release of DA in transgenic mice with gain-of-function α6* nAChRs. J Neurochem 129 315 PMID: 24266758

Squillace et al (2014) Dysfunctional DArgic neurotransmission in asocial BTBR mice. Transl Psychiatry 4 e427 PMID: 25136890

Abdallah et al (2009) Impact of serotonin 2C receptor null mutation on physiology and behavior associated with nigrostriatal DA pathway function. Br J Pharmacol 29 8156 PMID: 19553455

Costa et al (2008) Electrophysiology and pharmacology of striatal neuronal dysfunction induced by mitochondrial complex I inhibition. J Neurosci 28 8040 PMID: 18685029

Visanji et al (2008) 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. FASEB J 22 2488 PMID: 18364399

Koprich et al (2011) Progressive neurodegeneration or endogenous compensation in an animal model of Parkinson's disease produced by decreasing doses of alpha-synuclein. PLoS One 6 e17698 PMID: 21408191

Navaroli et al (2011) The plasma membrane-associated GTPase Rin interacts with the DA transporter and is required for protein kinase C-regulated DA transporter trafficking. J Neurosci 31 13758 PMID: 21957239

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

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

Kim et al (2015) Spinal DArgic projections control the transition to pathological pain plasticity via a D1/D5-mediated mechanism. J Neurosci 35 6307 PMID: 25904784

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


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Reviews for GBR 12909 dihydrochloride

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GBR used as a selective DAT blocker for increasing dopamine release: Excellent publishable, performed ideally.
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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