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Vanoxerine dihydrochloride

Product Name
Vanoxerine dihydrochloride
CAS No.
67469-78-7
Chemical Name
Vanoxerine dihydrochloride
Synonyms
I-893;GBR 12909;Vanoxerine;Boxeprazine;GBR129092HCl;Vanoxerine 2HCl;vanoxerine-GBR-12909;I893 dihydrochloride;GBR 12909 DIHYDROCHLORIDE;GBR 12909 (hydrochloride)
CBNumber
CB9398144
Molecular Formula
C28H33ClF2N2O
Formula Weight
487.03
MOL File
67469-78-7.mol
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Vanoxerine dihydrochloride Property

Melting point:
221 °C
storage temp. 
Sealed in dry,Room Temperature
solubility 
DMSO: >5 mg/mL Solutions freshly prepared daily
form 
solid
color 
white
Water Solubility 
Soluble in DMSO to 50mM. Soluble to 5mM in water with warming.
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month.
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Safety

WGK Germany 
3
HS Code 
2933.59.5300
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
D052
Product name
GBR 12909 dihydrochloride
Purity
solid, ≥98% (HPLC)
Packaging
25mg
Price
$293
Updated
2024/03/01
Sigma-Aldrich
Product number
D052
Product name
GBR 12909 dihydrochloride
Purity
solid, ≥98% (HPLC)
Packaging
100mg
Price
$732
Updated
2024/03/01
Sigma-Aldrich
Product number
5.05732
Product name
GBR 12909 Dihydrochloride - CAS 67469-78-7 - Calbiochem
Packaging
10mg
Price
$111
Updated
2024/03/01
TCI Chemical
Product number
G0541
Product name
GBR 12909 Dihydrochloride
Packaging
50MG
Price
$178
Updated
2024/03/01
TCI Chemical
Product number
G0541
Product name
GBR 12909 Dihydrochloride
Packaging
250MG
Price
$600
Updated
2024/03/01
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Vanoxerine dihydrochloride Chemical Properties,Usage,Production

Description

Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a potent inhibitor that blocks dopamine uptake (IC50 = 1-51 nM). It is more than 100-fold less effective at blocking serotonin or noradrenaline uptake. GBR 12909 effectively inhibits dopamine uptake in vivo, leading to consequent stimulation of dopamine receptors. GBR 12909 also inhibits pyrilamine binding to the histamine H1 receptor (IC50 = 18 nM) but poorly inhibits ligand binding to dopamine, adrenergic, acetylcholine, serotonin, and γ-aminobutyric acid receptors. It also blocks ligand binding to sigma receptors in rat brain (IC50 = 48 nM).

Uses

Vanoxerine dihydrochloride is a Dopamine reuptake inhibitor that is developed for treatment of Parkinson's disease and depression but has no effect on these diseases.

Definition

ChEBI: Vanoxerine dihydrochloride is a hydrochloride salt that is obtained by reaction of vanoxerine with two equivalents of hydrogen chloride. Potent, competitive inhibitor of dopamine uptake (Ki = 1 nM for inhibition of striatal dopamine uptake). Has > 100-fold lower affinity for the noradrenalin and 5-HT uptake carriers. Also a potent sigma ligand (IC50 = 48 nM). Centrally active following systemic administration. It has a role as a dopamine uptake inhibitor. It contains a vanoxerine(2+).

General Description

Vanoxerine dihydrochloride is a potent inhibitor of dopamine active transporter (DAT, Ki = 1 nM, IC50 = 40 and 51 nM) with >100 fold selectivity over noradrenalin and 5-HT re-uptake transporter. Shown to produce behavioral profile in mice for bipolar mania disease model and ADHD disease models.

Hazard

A poison.

Biological Activity

Potent, competitive inhibitor of dopamine uptake (K i = 1 nM for inhibition of striatal dopamine uptake). Has > 100-fold lower affinity for the noradrenalin and 5-HT uptake carriers. Also a potent sigma ligand (IC 50 = 48 nM). Centrally active following systemic administration.

Biochem/physiol Actions

Highly selective dopamine reuptake inhibitor with behavioral effects similar to cocaine.

storage

Room temperature (desiccate)

References

1) Andersen?et al. (1989),?The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action; Eur. J. Pharmacol.,?166?493
2) Contreras?et al. (1990),?GBR-12909 and fluspirilene potently inhibited binding of [3H] (+)3-PPP to sigma receptors in rat brain; Life Sci.,?47?PL133
3) Yorgason?et al. (2011),?Low and high affinity dopamine transporter inhibitors block dopamine uptake within 5 sec of intravenous injection; Neuroscience,?182?125

Vanoxerine dihydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Vanoxerine dihydrochloride manufacturers

Shaanxi Dideu Medichem Co. Ltd
Product
Vanoxerine dihydrochloride 67469-78-7
Price
US $0.00-0.00/KG
Min. Order
1g
Purity
99%
Supply Ability
2000tons
Release date
2019-12-31
Career Henan Chemical Co
Product
Vanoxerine dihydrochloride 67469-78-7
Price
US $1.00/g
Min. Order
1g
Purity
99.99%
Supply Ability
2tons
Release date
2019-12-19

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