GBR 12783 dihydrochloride

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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 (1)
Literature (3)

Biological Activity for GBR 12783 dihydrochloride

GBR 12783 dihydrochloride is 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 for GBR 12783 dihydrochloride

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GBR 12783 dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 24.27 50

Preparing Stock Solutions for GBR 12783 dihydrochloride

The following data is based on the product molecular weight 485.5. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.12 mL 20.6 mL 41.19 mL
2.5 mM 0.82 mL 4.12 mL 8.24 mL
5 mM 0.41 mL 2.06 mL 4.12 mL
25 mM 0.08 mL 0.41 mL 0.82 mL

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Product Datasheets for GBR 12783 dihydrochloride

Certificate of Analysis / Product Datasheet
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References for GBR 12783 dihydrochloride

References are publications that support the biological activity of the product.

Bonnet and Constentin (1986) GBR 12783, a potent and selective inhibitor of DA 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 DA. J.Neurochem. 72 396 PMID: 9886093

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

Vaugeois et al (1992) In vivo labelling of the neuronal DA 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:

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

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

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

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


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Reviews for GBR 12783 dihydrochloride

Average Rating: 4 (Based on 1 Review.)

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Inhibition of Synaptic Transmission in the VP.
By Anonymous on 02/02/2020
Assay Type: In Vivo
Species: Mouse

DAT blocker GBR12783 (1 μΜ)

PMID: 29949769
review image

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Dopamine Receptors Scientific Review

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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