Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a piperazine derivative which is a potent and selective DRI (dopamine reuptake inhibitor). GBR-12909 binds to the target site on the DAT ~ 500 times more strongly than cocaine, but simultaneously inhibits the release of dopamine. This combined effect only slightly elevates dopamine levels, giving vanoxerine only mild stimulant effects. Vanoxerine has been researched for use in treating cocaine dependence both as a substitute for cocaine and to block the rewarding effects.
| Molecular Weight | 523.49 |
| Formula | C28H32F2N2O.2HCl |
| CAS Number | 67469-78-7 |
| Solubility (25°C) | DMSO 8 mg/mL |
| Storage | 4°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] Antonio E Lacerda, et al. Vanoxerine: cellular mechanism of a new antiarrhythmic
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