Adrenorphin (Metorphamide) is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with Ki of 12 nM. The binding ratios of Ki for μ-opioid receptor/Ki for δ-opioid receptor is 0.04, and the binding ratios of Ki for μ-opioid receptor/Ki for κ-opioid receptor is 0.46. Adrenorphin potently inhibits catecholamine secretion evoked by 10 μM nicotine in cultured human pheochromocytoma 6 cells, with IC50 of 1.1 μM.
| Molecular Weight | 984.18 |
| Formula | C44H69N15O9S |
| CAS Number | 88377-68-8 |
| Solubility (25°C) | DMSO 48 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.
[2] T Yanase, et al. J Clin Endocrinol Metab. Studies on adrenorphin in pheochromocytoma
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