GBR 12909 dihydrochloride
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.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|water||2.62||5mM with gentle warming|
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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.91 mL||9.55 mL||19.1 mL|
|5 mM||0.38 mL||1.91 mL||3.82 mL|
|10 mM||0.19 mL||0.96 mL||1.91 mL|
|50 mM||0.04 mL||0.19 mL||0.38 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Andersen (1989) The dopamine 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 dopamine 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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Keywords: Potent σ sigma ligand DA uptake inhibitors inhibits Selective General Receptors DAT Dopamine Transporters Monoamine Neurotransmitter GBR12909 dihydrochloride Dopamine Transporters
11 Citations for GBR 12909 dihydrochloride
Citations are publications that use Tocris products. Selected citations for GBR 12909 dihydrochloride include:
Hutchinson et al (2012) Differential regulation of MeCP2 phosphorylation in the CNS by dopamine and serotonin. J Neurosci 37 321 PMID: 21956448
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 pat Mol Neurodegener 5 43 PMID: 21029459
Abdallah et al (2009) Impact of serotonin 2C receptor null mutation on physiology and behavior associated with nigrostriatal dopamine 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
Kim et al (2015) Spinal dopaminergic projections control the transition to pathological pain plasticity via a D1/D5-mediated mechanism. J Neurosci 35 6307 PMID: 25904784
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
Squillace et al (2014) Dysfunctional dopaminergic neurotransmission in asocial BTBR mice. Transl Psychiatry 4 e427 PMID: 25136890
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
Do you know of a great paper that uses GBR 12909 dihydrochloride from Tocris? If so please let us know.
Literature in this Area
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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