Vortioxetine hydrobromide is a novel multimodal antidepressant and a 5-HT transporter (5-HTT) inhibitor in vitro. Vortioxetine (Lu AA21004) inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. Vortioxetine significantly increased cell proliferation and cell survival and stimulated maturation of immature granule cells in the subgranular zone of the dentate gyrus of the hippocampus after 21 days of treatment. Vortioxetine enhances contextual and episodic memory in rat behavioral models. Vortioxetine (Lu AA21004) displays an antidepressant and anxiolytic profile following repeated administration associated with increased neurogenesis at several stages.
| Molecular Weight | 379.36 |
| Formula | C18H22N2S.HBr |
| CAS Number | 960203-27-4 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
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