Donepezil: Difference between revisions
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* Why You Should Care: One of the most effective treatments for teh symptoms of [[Alzheimer's Disease]], although no definitive proof exists as to whether to alters the progression of the disease. | * Why You Should Care: One of the most effective treatments for teh symptoms of [[Alzheimer's Disease]], although no definitive proof exists as to whether to alters the progression of the disease. | ||
* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information | * The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information | ||
===Mechanism of Action=== | ===Mechanism of Action=== | ||
Donepezil is a potent [[Acetylcholinesterase]] inhibitor to the active site of <scene name='Donepezil/Ache/1'>AChE</scene>. It binds along the active-site gorge, extending from the anionic subsite near <scene name='Donepezil/Trp_84/1'>Trp 84</scene> to the peripheral anionic site near <scene name='Donepezil/Trp_279/1'>Trp 279</scene>. 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 w/ AChE nor electrostatic interactions, but rather only interacts via aromatic stacking and solvent mediated interactions. It <scene name='Donepezil/Bound/1'>primarily interacts</scene> 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. | |||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||