GBR 12783 dihydrochloride

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Cat.No. 0513 - GBR 12783 dihydrochloride | C28H32N2O.2HCl | CAS No. 67469-75-4
Description: Potent and selective DA uptake inhibitor
Chemical Name: 1-(2-Diphenylmethoxyethyl)-4-(3-phenyl-2-propenyl)-piperazine dihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (4)
Reviews
Literature

Biological Activity

A very potent and selective inhibitor of dopamine uptake (IC50 for inhibition of [3H]-dopamine uptake in rat striatal synaptosomes is 1.8 nM).

Technical Data

M. Wt 485.5
Formula C28H32N2O.2HCl
Storage Desiccate at -20°C
Purity ≥99% (HPLC)
CAS Number 67469-75-4
PubChem ID 24744862
InChI Key HJDXBLLTRMCYNC-JFXLULTRSA-N
Smiles Cl[H].Cl[H].C(CN1CCN(C\C=C\C2=CC=CC=C2)CC1)OC(C1=CC=CC=C1)C1=CC=CC=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 4.86 10 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 485.5. 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
0.1 mM 20.6 mL 102.99 mL 205.97 mL
0.5 mM 4.12 mL 20.6 mL 41.19 mL
1 mM 2.06 mL 10.3 mL 20.6 mL
5 mM 0.41 mL 2.06 mL 4.12 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.

Bonnet and Constentin (1986) GBR 12783, a potent and selective inhibitor of dopamine uptake: biochemical studies in vivo and ex vivo. Eur.J.Pharmacol. 121 199 PMID: 3754516

Do-Rego et al (1999) Evidence for the sequential formation of two complexes between an uptake inhibitor, GBR 12783 [1-[2-(diphenylmethoxy)ethyl]-4-(3-phenyl-2-propenyl)piperazine], and the neuronal transporter of dopamine. J.Neurochem. 72 396 PMID: 9886093

Giros et al (1992) Cloning, pharmacological characterization and chromosome assignment of the human dopamine transporter. Mol.Pharmacol. 42 383 PMID: 1406597

Vaugeois et al (1992) In vivo labelling of the neuronal dopamine uptake complex in the mouse striatum by [3H]GBR 12783. Eur.J.Pharmacol. 210 77 PMID: 1350989


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4 Citations for GBR 12783 dihydrochloride

Citations are publications that use Tocris products. Selected citations for GBR 12783 dihydrochloride include:

Matsui and Alvarez (2018) Cocaine Inhibition of Synaptic Transmission in the Ventral Pallidum Is Pathway-Specific and Mediated by Serotonin. Cell Rep 23 3852 PMID: 29949769

Ferreira et al (2012) Presynaptic CB(1) cannabinoid receptors control frontocortical serotonin and glutamate release--species differences. J Pharmacol Exp Ther 61 219 PMID: 22609378

Ferraro et al (2012) A novel mechanism of cocaine to enhance dopamine d2-like receptor mediated neurochemical and behavioral effects. An in vivo and in vitro study. Neuropsychopharmacology 37 1856 PMID: 22453136

Masi et al (2013) MPP(+) -dependent inhibition of Ih reduces spontaneous activity and enhances EPSP summation in nigral dopamine neurons. Br J Pharmacol 169 130 PMID: 23323755


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