GBR-12909 | B3043

GBR-12909 is a potent and selective inhibitor of dopamine uptake (Ki = 1 nM). It inhibits dopamine uptake in tissue slices obtained from rat neostriatum at nanomolar concentrations. GBR-12909 (10 mg/kg IP) produces a dose-dependent decrease in the binding of cocaine to the dopamine transporter in rats. It antagonizes the ability of cocaine to elevate extracellular dopamine. It is also a potent blocker of cardiac hERG, sodium and calcium channels and shows cardiac antiarrhythmic properties. It is a potent ligand for sigma receptor. Regulators of sigma receptors are suggested to show activity against COVID-19, based on viral assay screens

GBR-12909 is a potent and selective inhibitor of dopamine uptake (Ki = 1 nM). It inhibits dopamine uptake in tissue slices obtained from rat neostriatum at nanomolar concentrations. GBR-12909 (10 mg/kg IP) produces a dose-dependent decrease in the binding of cocaine to the dopamine transporter in rats. It antagonizes the ability of cocaine to elevate extracellular dopamine. It is also a potent blocker of cardiac hERG, sodium and calcium channels and shows cardiac antiarrhythmic properties. It is a potent ligand for sigma receptor. Regulators of sigma receptors are suggested to show activity against COVID-19, based on viral assay screens

B3043 | GBR-12909 DataSheet

Alternate Name/Synonyms: Vanorexine; Vanoxerin; 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine; Vanoxerina; Vanoxerinum

Appearance: Solid powder

Formulation:

CAS Number: 67469-69-6

Structure Available?: TRUE

Peptide sequence:

Salt Form: FALSE

Molecular Formula: C₂₈H₃₂F₂N₂O

Molecular Weight: 450.56

Cell-Permeable?: TRUE

Purity: ≥98%

Solubilities: Soluble in DMSO

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A potent and selective inhibitor of dopamine uptake

MDL Number: MFCD00600385

PubChem CID: 3455

SMILES: C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F

InChi: InChI=1S/C28H32F2N2O/c29-26-12-8-24(9-13-26)28(25-10-14-27(30)15-11-25)33-22-21-32-19-17-31(18-20-32)16-4-7-23-5-2-1-3-6-23/h1-3,5-6,8-15,28H,4,7,16-22H2

InChi Key: NAUWTFJOPJWYOT-UHFFFAOYSA-N