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.
Cell Experiment | |
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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 | |
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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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