Milnacipran inhibits both norepinephrine transporter (NET) and norepinephrine transporter (SERT) with IC50 of 77 nM and 420 nM, respectively. Milnacipran inhibits the reuptake of serotonin and norepinephrine in an approximately 1:3 ratio, respectively; in practical use this means a relatively balanced action upon bothneurotransmitters.
| Molecular Weight | 282.81 |
| Formula | C15H22N2O.HCl |
| CAS Number | 101152-94-7 |
| Form | Solid |
| Solubility (25°C) | DMSO 38 mg/mL Water 30 mg/mL |
| Storage | 2-8°C |
| 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.
[1] Harshit Gupta, et al. Milnacipran for the Treatment of Fibromyalgia
[3] Patrick Welsch, et al. Serotonin and noradrenaline reuptake inhibitors (SNRIs) for fibromyalgia
[4] No authors listed. Aust Prescr. Milnacipran hydrochloride
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