Medetomidine is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.
 |
Source | BMC Vet Res (2013). Figure 2. Medetomidine |
| Method | anaesthetic treatments | |
| Cell Lines | C57BL/6N mice | |
| Concentrations | 1 mg/kg | |
| Incubation Time | 48 h | |
| Results | Loss of the tail-pinch reflex occurred by 12 minutes post-injection and did not significantly differ between MK and DK |
 |
Source | BMC Vet Res (2013). Figure 1. Medetomidine |
| Method | anaesthetic treatments | |
| Cell Lines | C57BL/6N mice | |
| Concentrations | 1 mg/kg | |
| Incubation Time | 48 h | |
| Results | The time until LORR was not significantly affected by drug (glm, F = 1.14, P = 0.29), administration route (glm, F = 0.14, P = 0.71; Figure 1), or individual bodyweight (glm, F = 3.30, P = 0.078). |
| Cell Experiment | |
|---|---|
| Cell lines | A549 human alveolar epithelial cells |
| Preparation method | Cells were challenged with 500 μM H2O2 in fresh RPMI 1640 medium without FBS for 24 hours in the control group, while, in the treatment groups, the cells were pretreated with 1 nM medetomidine for 15 minutes, in the presence or absence of 10 nM atipamezole, a synthetic α 2-adrenergic antagonist and then exposed to 500 μM H2O2 for additional 24 hours. |
| Concentrations | 1 nM |
| Incubation time | 15 min |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6N mice |
| Formulation | physiological saline solution |
| Dosages | 1 mg/kg |
| Administration | i.p. |
| Molecular Weight | 236.74 |
| Formula | C13H16N2.HCl |
| CAS Number | 86347-15-1 |
| Solubility (25°C) | DMSO 10 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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