Donepezil (CAS 120014-06-4)

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Alternate Names: Aricept

Application: Donepezil is shown to increase levels of cortical acetylcholine

CAS Number: 120014-06-4

Purity: ≥99%

Molecular Weight: 379.50

Molecular Formula: C₂₄H₂₉NO₃

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

* Refer to Certificate of Analysis for lot specific data (including water content).

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Donepezil is a noncompetitive acetylcholineesterase inhibitor, which can readily cross the blood brain barrier and increase the concentration of cortical acetylcholine. It is known that Donepezil is a useful tool in the study of Alzheimer's disease. Studies indicate that Donepezil protects the brain against diisopropylfluorophosphate-induced effects. Studies indicate that Donepezil selectively inhibits acetylcholineesterase, whereas it has little effect on butyrylcholinesterase. Alternate studies suggest that Donepezil increases the concentration of extracellular acetylcholine in the cerebral cortex and hippocampus of rats.

References

1. Shintani, E.Y., et al. 1997. Am J Health Syst Pharm. 54: 2805-2810. PMID: 9428950
2. Bryson, H.M. and Benfield, P. 1997. Drugs Aging. 10: 234-240. PMID: 9108896

Physical State :

Solid

Solubility :

Soluble in chloroform (~50 mg/ml), and acetone (~25 mg/ml).

Storage :

Store at -20° C

Melting Point :

206.72° C (Predicted)

Boiling Point :

~527.9° C at 760 mmHg (Predicted)

Density :

~1.1 g/cm³ (Predicted)

Refractive Index :

n²⁰_D 1.58 (Predicted)

IC50 :

Acetylcholinesterase: IC₅₀ = 1.7 nM (rat); AChE: IC₅₀ = 2 nM (human); Acetylcholinesterase: IC₅₀ = 4.2 nM (bovine); Choline acetylase: IC₅₀ = 5.3 nM (rat); Acetylcholinesterase: IC₅₀ = 5.7 nM (mouse)

Ki Data :

Acetylcholinesterase: K_i= 2.9 nM (bovine); AChE: K_i= 7.2 nM (human); Sigma Receptor: K_i= 14.6 nM (human); Acetylcholinesterase: K_i= 56 nM (electric eel); Butyrylcholinesterase: K_i= 640 nM (horse)

pK Values :

pK_b: 8.84 (Predicted)

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

PubChem CID :

3152

Merck Index :

14: 3419

MDL Number :

MFCD00912833

EC Number :

601-651-9

Beilstein Registry :

7081955

SMILES :

COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC

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Certificate of Analysis

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Donepezil (CAS 120014-06-4) Product Citations

See how others have used Donepezil (CAS 120014-06-4). Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 25498859 Chae, YJ. et al. 2015. Brain Res. 1597: 77-85.

PMID: # 32221697 Psychopharmacology (Berl.).

Citations 1 to 2 of 2 total

Rated 5 out of 5 by NZ from Bryson et al Bryson et al. (PubMed ID 9108896) found that Donepezil inhibited acetylcholinerase activity in human red blood cells and increased acetylcholine in the cerebral cortex and hippocampus of rats. It was also used to improve cognitive function in patients with Alzheimer s disease. -SCBT Publication Review

Date published: 2015-03-31

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