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Vanoxerine

Chemical Structure : Vanoxerine

CAS No.: 67469-69-6

Vanoxerine (Boxeprazine;GBR-12909;GBR12909;GBR 12909;I893;I-893;I 893)

Catalog No.: PC-43400Not For Human Use, Lab Use Only.

Vanoxerine (GBR-12909, I-893, Boxeprazine) is a highly potent inhibitor of dopamine uptake in vitro in tissue slices obtained from rat neostriatum with IC50 of 40-50 nM, also inhibits norepinephrine uptake with IC50 of 560-2600 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Vanoxerine (GBR-12909, I-893, Boxeprazine) is a highly potent inhibitor of dopamine uptake in vitro in tissue slices obtained from rat neostriatum with IC50 of 40-50 nM, also inhibits norepinephrine uptake with IC50 of 560-2600 nM; Vanoxerine also is a potent hK(v)11.1 blocker, and at submicromolar concentrations, it blocks Ca and Na currents in a strongly frequency-dependent manner possesses anticonvulsant activity in zebrafish and rodent models of generalized epilepsy but with cardiac ion channel effects.

Heart Arrhythmia

Phase 3 Discontinued

Physicochemical Properties

M.Wt 450.5633
Formula C28H32F2N2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Piperazine, 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)-

References

1. Teicher MH, et al. Brain Res. 1986 Nov;395(1):124-8.

2. Heikkila RE, et al. Eur J Pharmacol. 1984 Aug 17;103(3-4):241-8.

3. Lacerda AE, et al. J Cardiovasc Electrophysiol. 2010 Mar;21(3):301-10.

4. Goldsmith P, et al. Pharmacology. 2007;79(4):250-8.

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