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61724
GBR-12909 Dihydrochloride
Activators & Inhibitors
Chemical Modulators

GBR-12909 Dihydrochloride #61724

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Chemical structure of GBR-12909 Dihydrochloride.

Product Usage Information

GBR-12909 Dihydrochloride is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 10 mg of powder in 1.27 ml of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Storage

Store lyophilized at room temperature, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight: 523.5 g/mol

Purity: >98%

Molecular Formula: C28H32F2N2O • 2HCl

CAS: 67469-78-7

Solubility: Soluble in DMSO at 30 mg/ml or water at 10 mg/ml both with slight warming.

Background

GBR-12909 Dihydrochloride is a highly selective synaptosomal dopamine uptake inhibitor (Ki = 1 nM), with a 100-fold stronger affinity for the dopamine uptake carrier protein than noradrenaline and serotonin (1). GBR-12909 Dihydrochloride has also been demonstrated to be a strong sigma receptor ligand in rat brain samples with an IC50 value of 48 nM (2). This small molecule is considered to be a high-affinity, long-acting dopamine transporter (DAT) inhibitor and in vivo models show that intravenous injection of GBR-12909 Dihydrochloride blocks dopamine uptake within 5 seconds, matching the temporal effect of cocaine, with longer-acting and less negative behavioral effects (3). The ability to regulate dopamine uptake makes GBR-12909 Dihydrochloride a compound of interest when studying substance abuse issues like alcohol and cocaine addiction (4,5).

  1. Andersen, P.H. (1989) Eur J Pharmacol 166, 493-504.
  2. Contreras, P.C. et al. (1990) Life Sci 47, PL133-7.
  3. Yorgason, J.T. et al. (2011) Neuroscience 182, 125-32.
  4. Tella, S.R. et al. (1996) J Neurosci 16, 7416-27.
  5. Kamdar, N.K. et al. (2007) Psychopharmacology (Berl) 192, 207-17.
For Research Use Only. Not For Use In Diagnostic Procedures.

Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.

To Purchase # 61724S
Product # Size Price
61724S
10 mg $ 71