Chemical structure of GBR-12909 Dihydrochloride.
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.
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.
Molecular Weight: 523.5 g/mol
Molecular Formula: C28H32F2N2O • 2HCl
Solubility: Soluble in DMSO at 30 mg/ml or water at 10 mg/ml both with slight warming.
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).
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