Donepezil hydrochloride is a centrally acting reversible acetylcholinesterase inhibitor (AChEI) with an IC50 of 12.3 nM. Its main therapeutic use is in the treatment of Alzheimer’s disease where it is used to increase levels of cortical acetylcholine. It has an oral bioavailability of 100% and easily crosses the blood-brain barrier.
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Animal Experiment | |
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Animal models | Male Lister Hooded rats |
Formulation | 0.9% w:v NaCl (saline) |
Dosages | 18 μM/kg |
Administration | Administered via i.p. or p.o. |
Molecular Weight | 416 |
Formula | C24H29NO3.HCl |
CAS Number | 120011-70-3 |
Solubility (25°C) | Water 25 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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