GBR 12909 dihydrochloride

Name: GBR 12909 dihydrochloride
Brand: Tocris Bioscience
SKU: 0421
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 0421

(1)

Citations (16)

COA / SDS

Selective DA uptake inhibitor; also σ ligand

Key Product Details

Description:	Selective DA uptake inhibitor; also σ ligand
Chemical Name:	1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	523.49

View Full Technical Details for GBR 12909 dihydrochloride

Technical Data
Citations / Reviews (1)

Biological Activity for GBR 12909 dihydrochloride

GBR 12909 dihydrochloride is a potent, competitive inhibitor of dopamine uptake (K_i = 1 nM for inhibition of striatal dopamine uptake). Has >100-fold lower affinity for the noradrenaline and 5-HT uptake carriers. Also a potent sigma ligand (IC₅₀ = 48 nM). Centrally active following systemic administration.

Compound Libraries for GBR 12909 dihydrochloride

GBR 12909 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GBR 12909 dihydrochloride

M. Wt	523.49
Formula	C₂₈H₃₂F₂N₂O.2HCl
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	67469-78-7
PubChem ID	104920
InChi Key	MIBSKSYCRFWIRU-UHFFFAOYSA-N
Smiles	Cl.Cl.FC1=CC=C(C=C1)C(OCCN1CCN(CCCC2=CC=CC=C2)CC1)C1=CC=C(F)C=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 for GBR 12909 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	2.62	5 with gentle warming
	DMSO	26.17	50

Preparing Stock Solutions for GBR 12909 dihydrochloride

The following data is based on the product molecular weight 523.49.

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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	3.82 mL	19.10 mL	38.21 mL
2.5 mM	0.76 mL	3.82 mL	7.64 mL
5 mM	0.38 mL	1.91 mL	3.82 mL
25 mM	0.08 mL	0.38 mL	0.76 mL

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References for GBR 12909 dihydrochloride

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

Spealman and Melia Pharmacological characterization of the discriminative-stimulus effects of GBR 12909. J.Pharmacol.Exp.Ther. 1991 PMID: 1678014
Contreras GBR-12909 and fluspirilene potently inhibited binding of [³H] (+)3-PPP to sigma receptors in rat brain. Life Sci. 1990 PMID: 1980329
Heikkila and Manzino Behavioral properties of GBR 12909, GBR 13069 and GBR 13098: specific inhibitors of DA uptake. Eur.J.Pharmacol. 1984 PMID: 6237922
Andersen The DA uptake inhibitor GBR12909: selectivity and molecular mechanism of action. Eur.J.Pharmacol. 1989 PMID: 2530094