Varenicline (CP 526555) is a selective α4β2 nicotinic receptor partial agonist, it stimulates nicotine receptors more weakly than nicotine itself does. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively.
| Cell Experiment | |
|---|---|
| Cell lines | MS/DB neurons |
| Preparation method | In one subset of experiments, bath solution containing nicotine (10 μM) was initially applied followed by a nicotine (10 μM) plus varenicline (10 μM) bath solution. For a second subset of experiments, the order of drug application was reversed with a varenicline (10 μM) containing bath solution applied first followed by a varenicline (10 μM) plus nicotine (10 μM) bath solution. |
| Concentrations | 10 μM |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague–Dawley rats |
| Formulation | saline |
| Dosages | 0.5, 1, 2 and 3 mg/kg |
| Administration | s.c. |
| Molecular Weight | 211.26 |
| Formula | C13H13N3 |
| CAS Number | 249296-44-4 |
| 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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