Vanoxerine dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Vanoxerine (GBR-12909, I-893) 是一种高效的体外多巴胺摄取抑制剂，在从大鼠新纹状体获得的组织切片中，IC50 为 40-50 nM。

Vanoxerine (GBR-12909, I-893) 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(In Vitro):Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) 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 dihydrochloride (GBR-12909 dihydrochloride) is also an oral, mixed ion channel blocker with IKr, INa, and L-type calcium channel activity.(In Vivo):Vanoxerine dihydrochloride (2.5-20 mg/kg; i.p.) significantly increases the ambulatory activity.

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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

Membrane Transporter/Ion Channel

Monoamine Transporter

Monoamine Transporter

Cardiovascular Disease

Heart Arrhythmia

67469-78-7

450.5633

C28H32F2N2O

>98% (HPLC)

DMSO: 9.4 mg/mL

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

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

(-20℃)

With Ice Pack

≥ 2 years