GBR 12909 dihydrochloride
Cat. No. 0421
Chemical Name: 1-[2-[Bis-(4-fluorophenyl)methoxy]e
Biological ActivityPotent, 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.
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 / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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:
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.
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.
Hutchinson et al (2012) Differential regulation of MeCP2 phosphorylation in the CNS by dopamine and serotonin. J Neurosci 37 321. PMID: 21956448.
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.
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.
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