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.
|Animal models||Male Lister Hooded rats|
|Formulation||0.9% w:v NaCl (saline)|
|Administration||Administered via i.p. or p.o.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||Water 25 mg/mL|
|Related AChR/AChE Products|
|Scopolamine hydrobromide trihydrate
Scopolamine hydrobromide trihydrate is a competitive muscarinic acetylcholine receptor with an IC50 of 55.3 ± 4.3 nM.
Choline Glycerophosphate is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue.
MK-7622 is a cholinesterase inhibitor, it is also a muscarinic M1 receptor positive allosteric modulator.
Acotiamide is a potent, selective and reversible inhibitor of human and canine stomach-derived acetylcholinesterase (AChE).
Huperzine A is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor extracted from traditional Chinese herb.
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