Cebranopadol is a NOP and opioid receptor agonist that acts on human NOP, MOP, KOP and δ-opioid peptide (DOP) receptors with Ki/EC50 values of 0.9 nM/13 nM and 0.7 nM/1.2 nM, respectively. 2.6 nM/17 nM, 18 nM/110 nM.
| Molecular Weight | 378.48 |
| Formula | C24H27FN2O |
| CAS Number | 863513-91-1 |
| Solubility (25°C) | 10 mM in DMSO |
| 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.
[3] R B Raffa, et al. Cebranopadol: novel dual opioid/NOP receptor agonist analgesic
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