Donepezil hydrochloride

Biological Activity

Donepezil hydrochloride is a potent and selective acetylcholinesterase inhibitor (IC₅₀ = 5.7 nM). In animal models of Alzheimer's disease, Donepezil reduces brain tissue Aβ protein and plaque deposition, restores normal glucose metabolism, reduces neuroinflammation and rescues cognitive dysfunction and memory deficits. The pro-cognitive effects are potentiated by combination with Mefloquine (Cat. No. 6819). In vitro Donepezil reduces LPS-induced inflammation and protects against mitochondrial membrane potential damage.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.
   Sugimoto et al.
   J.Med.Chem., 1995;38:4821
2. Structure of acetylcholinesterase complexed with E2020 (Aricept): implications for the design of new anti-Alzheimer drugs.
   Kryger et al.
   Structure, 1999;7:297
3. Donepezil hydrochloride (E2020) and other acetylcholinesterase inhibitors.
   Sugimoto et al.
   Curr.Med.Chem., 2000;7:303

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