| Bioactivity | Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator. Radafaxine hydrochloride (GW-353162A) is a potent metabolite of bupropion and selective for inhibiting the reuptake of norepinephrine over dopamine[1][2][3]. |
| Invitro | The relatively low potency of Radafaxine hydrochloride (GW-353162A) in blocking DAT and its slow blockade suggests that it is unlikely to have reinforcing effects[3]. |
| Name | Radafaxine hydrochloride |
| CAS | 106083-71-0 |
| Formula | C13H19Cl2NO2 |
| Molar Mass | 292.20 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Xu H, et al. Stereoselective analysis of hydroxybupropion and application to drug interaction studies. Chirality. 2007 Mar;19(3):163-70. [2]. Volkow ND, et al. The slow and long-lasting blockade of dopamine transporters in human brain induced by the new antidepressant drug radafaxine predict poor reinforcing effects. Biol Psychiatry. 2005 Mar 15;57(6):640-6. [3]. Bondarev ML, et al. Behavioral and biochemical investigations of bupropion metabolites. Eur J Pharmacol. 2003 Aug 1;474(1):85-93. |