Rotigotine is a potent dopamine receptor agonist with Ki values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor.
 |
Source | Bioanalysis (2014). Figure 3. Rotigotine |
| Method | competition binding assays | |
| Cell Lines | LMtk cells | |
| Concentrations | 10 μM | |
| Incubation Time | ||
| Results | There was a good correlation between functional potency of the agonists examined (Table 4) and their binding affinity versus [3H]rotigotine (Table 5) at the three dopamine receptors |
 |
Source | Bioanalysis (2014). Figure 2. Rotigotine |
| Method | competition binding assays | |
| Cell Lines | CHO cells | |
| Concentrations | 10 μM | |
| Incubation Time | ||
| Results | Equilibrium saturation assays were performed in triplicate with [3H]rotigotine and with the radiolabelled antagonist [3H]SCH23390 for D1 and D5, [3H]raclopride for D2 and [3H]spiperone for D3 and D4 receptors |
| Cell Experiment | |
|---|---|
| Cell lines | primary mesencephalic cell |
| Preparation method | To investigate the effect of rotigotine (UCB, Belgium) on the survival of THir neurons, primary mesencephalic cell cultures were treated with different concentrations of rotigotine (0.01, 0.1, 1 and 10 µM) from the 6th DIV for 8 consecutive days. Rotigotine was added with each change of the culture medium every second day from a fresh stock solution (10 mM) prepared in DMSO (0.1% final concentration). To investigate the effect of rotigotine against MPP+ or rotenone-induced cell death, rotigotine was added from the 6th DIV until the 14th DIV as described above and MPP+ (10 µM) or rotenone (20 nM) were co-administered on the 12th DIV for 48 h. |
| Concentrations | 0.01, 0.1, 1 and 10 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | Sprague-Dawley rats |
| Formulation | 1:10 ratio of dimethyl sulfoxide (DMSO) and 5% dextrose |
| Dosages | 0.5 or 3 mg/kg |
| Administration | s.c. |
| Molecular Weight | 315.47 |
| Formula | C19H25NOS |
| CAS Number | 99755-59-6 |
| Solubility (25°C) | DMSO ≥ 40 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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