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Biological Data
Biological description
Potent, competitive dopamine uptake inhibitor (Ki = 1 nM). Also a potent Kv 11.1, and Na+ and Ca+ channel blocker (IC50 values are 0.8, 320 and 830 nM at hKv 11.1, hICa,L and hNav 1.5 respectively and σ receptor blocker). Shows variety of biological actions. Active in vivo .
Solubility & Handling
Storage instructions
Room temperature (desiccate)
Solubility overview
Soluble in water (25 mM, gentle warming) and in DMSO (50 mM)
Important
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
Chemical Data
Chemical name
1-[2-[Bis -(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride
Chemical structure
Molecular Formula
C28 H32 F2 N2 O.2HCl
PubChem identifier
104920
SMILES
C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F.Cl.Cl
InChi
InChI=1S/C28H32F2N2O.2ClH/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;2*1H
InChiKey
MIBSKSYCRFWIRU-UHFFFAOYSA-N
References for GBR 12909 dihydrochloride
References are publications that support the biological activity of the product
Vanoxerine: cellular mechanism of a new antiarrhythmic.
Lacerda AE et al (2010)
J Cardiovasc Electrophysiol 21(3) : 301-10.
Short-acting cocaine and long-acting GBR-12909 both elicit rapid dopamine uptake inhibition following intravenous delivery.
Espaã±a RA et al (2008)
Neuroscience 155(1) : 250-7.
The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action.
Andersen PH (1989)
Eur J Pharmacol 166(3) : 493-504.
Publications
These publications cite the use of GBR 12909 dihydrochloride purchased from Hello Bio:
A dynamic role for dopamine receptors in the control of mammalian spinal networks
Sharples et al (2020)
Sci Rep. : 10(1)
Dopaminergic control of postnatal mammalian spinal network function is predominantly inhibitory
Sharples et al (2019)
bioRxiv : https://doi.org/10.1101/715326
State-dependent neuromodulation of mammalian spinal networks
Sharples et al (2018)
University of Calgary : Thesis
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Potent, competitive dopamine uptake inhibitor