Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM. Aripiprazole (OPC-14597) is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole shows a greater anti-inflammatory effect on TNF-α, IL-13, IL-17α and fractalkine.
| Molecular Weight | 448.39 |
| Formula | C23H27Cl2N3O2 |
| CAS Number | 129722-12-9 |
| Solubility (25°C) | DMSO 90 mg/mL DMF 40 mg/mL |
| Storage | 4°C, protect from light |
| 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.
[3] Adrian Preda, et al. A safety evaluation of aripiprazole in the treatment of schizophrenia
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