Vanoxerine

Research use only, not for human use.

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.

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.

Vanoxerine (GBR-12909) inhibits the uptake of dopamlne (DA), with an IC50 in the low nanomolar range, and is several-fold less potent as inhibitors of the uptake of noradrenaline and 5-HT. Vanoxerine (GBR-12909) is also an oral, mixed ion channel blocker with IKr, INa, and L-type calcium channel activity.

Vanoxerine (GBR-12909) (2.5-20 mg/kg; i.p.) significantly increases the ambulatory activity. Animal Model:Male mice(ddY strain at 6 weeks of age)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.

Boxeprazine | GBR-12909 | GBR12909 | GBR 12909 | I893

Membrane Transporter/Ion Channel

Monoamine Transporter

Monoamine Transporter

Cardiovascular Disease

Heart Arrhythmia

67469-69-6

450.5633

C28H32F2N2O

>98% (HPLC)

10 mM in DMSO

C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F

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

(-20℃)

With Ice Pack

≥ 2 years