Donepezil
Donepezil
Better Known as: Aricept
Mechanism of ActionDonepezil is a potent Acetylcholinesterase (AChE) inhibitor to the active site of AChE. By inhibiting AChE, the important neurotransmitter, acetylcholine, is degraded at a slower rate, helping reverse the marked decrease in neuronal function evident in Alzheimer's Disease patients. Donepezil binds along the active-site gorge, extending from the anionic subsite near Trp 84 to the peripheral anionic site near Trp 279. Interestingly, it does not directly interact with the catalytic triad of acetylcholinesterase nor the oxyanion hole. Further, donepezil does not form any direct hydrogen bonds with AChE nor electrostatic interactions, but rather only interacts via aromatic stacking and solvent mediated interactions. It primarily interacts with Glu 199, His 440, Phe 330, Trp 84, Tyr 334, Tyr 121, Phe 331, Phe 288, Ser 286, Phe 290, Arg 289, Trp 279, & Leu 282 to tightly bind to AChE[2]. More details can be seen at Aricept_Complexed_with_Acetylcholinesterase. Pharmacokinetics
References
| ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
