Home Neuronal Signaling AChR inhibitor Donepezil For research use only.

Donepezil

Synonyms: Aricept, Donepezilo

Donepezil (Aricept, Donepezilo) is a piperidine based, potent, specific, non-competitive and reversible inhibitor of acetylcholinesterase (AChE) used for the treatment of mild to moderate dementia of the Alzheimer's type.

Donepezil Chemical Structure

Donepezil Chemical Structure

CAS: 120014-06-4

Selleck's Donepezil has been cited by 4 publications

Purity & Quality Control

Batch: S507301 DMSO] 75 mg/mL] false] ] ] false] ] ] false Purity: 99.96%
99.96

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Biological Activity

Description Donepezil (Aricept, Donepezilo) is a piperidine based, potent, specific, non-competitive and reversible inhibitor of acetylcholinesterase (AChE) used for the treatment of mild to moderate dementia of the Alzheimer's type.
Targets
AChE [1]
6.7 nM
In vitro
In vitro Donepezil has reversible and noncompetitive inhibition effects on AChE. It has 500-1000-fold more selective for AChE over butyrylcholinesterase (BuChE). Short- and long-exposure of SH-SY5Y human neuroblastoma cells to donepezil induces a concentration-dependent inhibition of cell proliferation unrelated to muscarinic or nicotinic receptor blockade or apoptosis. Donepezil reduces the number of cells in the S-G2/M phases of the cell cycle, increases the G0/G1 population, and reduces the expression of two cyclins of the G1/S and G2/M transitions, cyclin E and cyclin B, in parallel with an increase in the expression of the cell cycle inhibitor p21. In addition, donepezil increases action potential-dependent dopamine release and modulates nicotinic receptors of substantia nigra dopaminergic neurons[1].
Cell Research Cell lines retinal ganglion cells (RGCs)
Concentrations 100 nM-10 μM
Incubation Time 3 days
Method

RGC survival after exposure to each reagent (glutamate, donepezil, tacrine, galanthamine, and HA14-1) is measured by calcein-AM staining after 3 days in culture, Briefly, cells are incubated in 1 μM calcein-AM in PBS for 15 minutes at 37℃. After the medium is replaced with fresh PBS, cells are examined under a fluorescence microscope using a fluorescein filter. The total number of surviving RGCs defined as cells with a calcein-AM stained cell body and a process extending at least two cell diameters from the cell body is counted in each well. The number of surviving RGCs without any drug served as a control.
In Vivo
In vivo Donepezil is slowly absorbed from the gastrointestinal tract and has a terminal elimination half-life of 50-70 hours in young volunteers (>100 hours in elderly subjects). After extensive metabolization in the liver, the parent compound is 93% bound to plasma proteins. Donepezil is metabolized in the liver via the cytochrome P450 system (CYP1A2-, CYP2D6-, CYP3A4-related enzymes). In animals, donepezil is found unchanged in brain, and no metabolites are detected in the nervous tissue. In plasma, urine, and bile, most donepezil metabolites are O-glucuronides. After oral ingestion, peak plasma concentrations are achieved in 3-5 hours and its absortion is not affected by food. Donepezil has linear pharmacokinetics over a dose range of 1-10 mg/day. 96% of circulating donepezil is protein bound[1].
Animal Research Animal Models Age-matched (10-12 weeks old, 21–24 g) male C57BL/6 wild-type and CGRP(−/−) mice
Dosages 1.5 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05345509 Recruiting Alzheimer Disease Inventage Lab. Inc. April 1 2023 Phase 1|Phase 2
NCT04308304 Completed Alzheimer''s Disease Merck Sharp & Dohme LLC February 16 2021 Phase 1
NCT04617782 Completed Healthy Subjects Corium Inc. December 8 2020 Phase 1
NCT03905096 Completed Healthy Boehringer Ingelheim April 12 2019 Phase 1

Chemical lnformation & Solubility

Molecular Weight 379.49 Formula

C24H29NO3
CAS No. 120014-06-4 SDF --
Smiles COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (197.63 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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