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 AChR/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.
Competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors.
Varenicline Tartrate is a nicotinic AChR partial agonist, used to treat nicotine addiction.
TD-4208 is a novel and potent muscarinic receptor antagonist that has a high affinity and long residence time at the M3 receptor, and demonstrates in vitro kinetic selectivity for M3 over M2 muscarinic receptor subtype and no meaningful off-target activity.
Tropicamide is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM.
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