| Name | Vanoxerine dihydrochloride |
| Description | Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a potent inhibitor of dopamine uptake (IC50: 1-51 nM). |
| In vivo | In 9 SP dogs, 11 episodes each of sustained (>10 minutes) AF and AFL were induced. Electrophysiological studies were performed before and after infusion of vanoxerine, which effectively terminated AF and AFL in 19 of 22 episodes. Simultaneous multisite mapping during 3 AF and 3 AFL episodes demonstrated that termination of each arrhythmia occurred with termination of the driver (a reentrant circuit) following an increase in tachycardia CL. Except for conduction in an area of slow conduction in the driver's reentrant circuit, vanoxerine did not significantly affect intraatrial or atrioventricular conduction time, QRS duration, or QT/QTc intervals. Ventricular refractoriness prolonged minimally during ventricular pacing at 400 and 333 ms (176 +/- 16 ms to 182 +/- 16 ms; 173 +/- 11 ms to 178 +/- 18 ms, respectively). Vanoxerine minimally increased (mean 0.7 mA) atrial stimulus threshold for capture[1].Vanoxerine dihydrochloridealso blocks ligand binding to sigma receptors in rat brain (IC50 = 48 nM)[2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 9.4 mg/mL (17.96 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.91 mM), Sonication is recommended.
|
| Keywords | Vanoxerine dihydrochloride | Vanoxerine | SLC6A3 | Inhibitor | inhibit | I-893 Dihydrochloride | I893 Dihydrochloride | I-893 | I893 | I 893 Dihydrochloride | I 893 | GBR-12909 Dihydrochloride | GBR12909 Dihydrochloride | GBR-12909 | GBR12909 | GBR 12909 Dihydrochloride | GBR 12909 | DopamineReceptor | dopamine uptake | Dopamine Transporter | Dopamine Receptor | DAT |
| Inhibitors Related | Trifluoperazine dihydrochloride | Clozapine N-Oxide | Mirtazapine | Hexamethonium Bromide | Butyrophenone | Octopamine hydrochloride | L-DOPA | Creatine | Dopamine hydrochloride | Oxolinic acid | Mianserin hydrochloride | Doxepin hydrochloride |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Endocrinology-Hormone Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
