Donepezil hydrochloride (Aricept) 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 5 mg/mL|
|Related AChE Products|
Donepezil(E 2020) is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM, respectively.
|Neostigmine methyl sulfate
Neostigmine methyl sulfate is a reversible inhibitor of acetylcholinesterase, can not cross the blood-brain barrier.
Malathion is an organophosphate parasympathomimetic which binds irreversibly to cholinesterase, is an insecticide of relatively low human toxicity.
Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|Atropine Sulfate Monohydrate
Atropine sulfate monohydrate is a competitive antagonist for the muscarinic acetylcholine receptor, used to decrease the production of saliva and secretions of the airway prior to surgery.
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