GBR 12909 dihydrochloride

Cat. No. 0421

GBR 12909 dihydrochloride C28H32F2N2O.2HCl [67469-78-7]

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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.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

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

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.

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

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

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

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

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

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 (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 dopamine transporter and is required for protein kinase C-regulated dopamine transporter trafficking. J Neurosci 31 13758. PMID: 21957239.

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 pathology of Parkinson's disease. Mol Neurodegener 5 43. PMID: 21029459.

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.

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Keywords: GBR 12909 dihydrochloride, supplier, Potent, σ, sigma, ligand, DA, uptake, inhibitors, inhibits, Selective, General, Receptors, DAT, Dopamine, Transporters, Monoamine, Neurotransmitter, GBR12909, dihydrochloride, Tocris Bioscience, Dopamine Transporter Inhibitor products

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