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[CAS NO. 67469-78-7] Vanoxerinedihydrochloride
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-13217 |
| Brand: | MCE |
| CAS: | 67469-78-7 |
Overview
| MDL | MFCD00055193 |
|---|---|
| Molecular Weight | 523.49 |
| Molecular Formula | C28H34Cl2F2N2O |
| SMILES | FC1=CC=C(C(C2=CC=C(F)C=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1.[2HCl] |
2 Publications Citing Use of MCE
Summary
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor ( K i =1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT) [1] .
IC50 & Target
Ki: 1 nM (dopamine reuptake) [1]
In Vitro
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) inhibits the uptake of dopamlne (DA), with an IC
50
in the low nanomolar range, and is several-fold less potent as inhibitors of the uptake of noradrenaline and 5-HT
[2]
.
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is also an oral, mixed ion channel blocker with IKr, INa, and L-type calcium channel activity
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Vanoxerine dihydrochloride (2.5-20 mg/kg; i.p.) significantly increases the ambulatory activity [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male mice (ddY strain at 6 weeks of age) [3] |
| Dosage: | 2.5, 5, 10, 20 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | The ambulatory activity of mice increased in a dose-dependent manner, with a maximal increase at 30 min after the administration. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01691313 | Laguna Pharmaceuticals, Inc. |
Symptomatic Atrial Fibrillation|Atrial Flutter
|
November 2012 | Phase 2 |
| NCT00089687 | National Institute on Drug Abuse (NIDA) |
Cocaine-Related Disorders
|
April 2004 | Phase 1 |
| NCT00100113 | National Institute on Drug Abuse (NIDA) |
Cocaine-Related Disorders
|
June 2004 | Phase 1 |
| NCT00218049 | National Institute on Drug Abuse (NIDA)|University of Texas |
Cocaine Abuse|Cocaine-Related Disorders
|
December 2004 | Phase 1 |
| NCT02454283 | Laguna Pharmaceuticals, Inc. |
Atrial Fibrillation or Flutter
|
September 2015 | Phase 3 |
| NCT00051896 | National Institute on Drug Abuse (NIDA) |
Cocaine-Related Disorders
|
August 2002 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 9.4 mg/mL ( 17.96 mM ; Need ultrasonic and warming)
H 2 O : 1 mg/mL ( 1.91 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9103 mL | 9.5513 mL | 19.1026 mL |
| 5 mM | 0.3821 mL | 1.9103 mL | 3.8205 mL |
| 10 mM | 0.1910 mL | 0.9551 mL | 1.9103 mL |
References
- [1] Rothman RB, et al. Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addiction. Biochem Pharmacol. 2008 Jan 1;75(1):2-16.
- [2] Hirate K, et al. Characteristics of the ambulation-increasing effect of GBR-12909, a selective dopamine uptakeinhibitor, in mice. Jpn J Pharmacol. 1991 Apr;55(4):501-11.
- [3] Andersen PH. The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action. Eur J Pharmacol.
Synonyms
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