Vanoxerine dihydroChloride - CAS 67469-78-7
Catalog number: 67469-78-7
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Dopamine Reuptake Inhibitor
Vanoxerine is a is a potent and selective DRI acts to block cardiac ion channels.
White solid
GBR 12909 Dihydrochloride; GBR12909 Dihydrochloride; GBR-12909 Dihydrochloride; 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine;dihydrochloride;
Soluble in DMSO
Store at -20 °C
DAT1 antagonist
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
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1.Negative interaction of dopamine D2 receptor antagonists and GBR 12909 and GBR 12935 dopamine uptake inhibitors in the nucleus accumbens.
Rahman S1, Engleman E, Simon J, McBride WJ. Eur J Pharmacol. 2001 Feb 23;414(1):37-44.
The objective of this study was to examine the interaction of dopamine D2 receptor antagonists and dopamine uptake inhibitors on the regulation of extracellular dopamine release in the nucleus accumbens of Wistar rats employing in vivo microdialysis and in vitro dopamine uptake studies. Application of the D2 receptor antagonists raclopride (100 microm) or sulpiride (100 microm) alone through the microdialysis probe in the nucleus accumbens for 60 min increased the extracellular levels of dopamine in the nucleus accumbens to 150% and 200% of basal, respectively. Perfusion of the nucleus accumbens for 60 min with the dopamine uptake inhibitors, 1-[2-[bis(4-Fluorophenyl)methoxy]ethyl]-4-[3-phenylpropyl]piperazine dihydrochloride (GBR 12909; 100 microm) or 1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)-piperazine dihydrochloride (GBR 12935; 100 microm) alone, increased the extracellular levels of dopamine in the nucleus accumbens to 400% and 350% of basal, respectively.
2.Methylphenidate restores ventral tegmental area dopamine neuron activity in prenatal ethanol-exposed rats by augmenting dopamine neurotransmission.
Choong KC1, Shen RY. J Pharmacol Exp Ther. 2004 May;309(2):444-51. Epub 2004 Jan 14.
Altered neurotransmission in the mesolimbic dopamine (DA) system has been suggested to be the underlying cause of attention problems commonly observed in children with fetal alcohol spectrum disorder (FASD). Methylphenidate is effective in treating attention problems in children with FASD. However, the underlying mechanism is currently unknown. We have shown previously that reduced ventral tegmental area (VTA) DA neuron activity in prenatal ethanol-exposed animals can be normalized by DA agonist treatment. In the present study, we investigated the possibility that similar mechanism mediates the effect of methylphenidate using the in vivo extracellular single-unit recording technique in anesthetized animals. We observed that reduced VTA DA neuron activity in prenatal ethanol-exposed animals was normalized by methylphenidate. The effect of methylphenidate was mediated by increased extracellular levels of DA instead of norepinephrine because this effect was not altered by the coadministration of prazosin, an alpha(1) receptor antagonist, and was mimicked by the application of DA transporter blockers, nomifensine and 1-2(-[bis(4-flurophenyl)methoxy]ethyl)-4-(3-phenyl)piperazine dihydrochloride (GBR 12909).
3.A simple probe measures the pharmacokinetics of[125I]RTI-55 in mouse brain in vivo.
Mochizuki T1, Villemagne VL, Scheffel U, Liu X, Musachio JL, Dannals RF, Wagner HN Jr. Eur J Pharmacol. 1997 Oct 29;338(1):17-23.
A simple external radiation detector system was used to assess brain dopamine and serotonin transporters in mice in vivo using [125I]RTI-55. The results were compared to ex vivo dissection data. Methyl 3beta-(4-iodophenyl) tropane-2beta-carboxic acid methyl ester (RTI-55 or beta-CIT), a high-affinity cocaine antagonist, binds to presynaptic dopamine and serotonin transporters in the brain. Radiotracer accumulation increased for the first 150 min after intravenous injection and then remained constant. When unlabeled RTI-55 was injected, either before or 60 min after radiotracer administration, a significant decrease in tracer accumulation was observed. [125I]RTI-55 binding was also displaced by blocking doses of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-[3-phenylpropyl]piperazine dihydrochloride (GBR 12909) and paroxetine. The results were similar to the ex vivo dissection data. The results demonstrate the feasibility of using the probe detector system to study the presynaptic transporter system in vivo in the mouse brain.
4.A novel modulatory mechanism of sodium currents: frequency-dependence without state-dependent binding.
Mike A1, Karoly R, Vizi ES, Kiss JP. Neuroscience. 2004;125(4):1019-28.
We have previously found that the dopamine uptake inhibitor 1-(2-[bis(4-fluorophenyl)methoxy]ethyl)-4-(3-phenylpropyl)piperazine dihydrochloride (GBR 12909) inhibits neuronal sodium channels. The inhibition was profoundly dependent on the voltage protocol, suggesting that the effect is determined by the activity pattern of individual neurons. Our present study was aimed to understand more thoroughly the mechanism of this inhibition. The effect of GBR 12909 on sodium currents was investigated using whole-cell patch clamp recordings on cultured hippocampal neurons. Repetitive trains of depolarizations revealed two distinct components of inhibition: a frequency-dependent, transient and a frequency-independent, sustained component. Frequency-dependent inhibition can reflect dynamic equilibrium of binding or gating. In order to decide which is the dominant mechanism in the case of GBR 12909, we studied the rates of association and dissociation.
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Chemical Structure

CAS 67469-78-7 Vanoxerine dihydroChloride

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