Structure of Donepezil
CAS No.: 120014-06-4
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Donepezil is a centrally acting reversible AchE inhibitor with IC50 of 8.12 nM and 11.6 nM for bAChE and hAChE, respectively, a medication used to treat Alzheimer's disease.
Synonyms: E2020 free base; Aricept; HSDB 7743
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Petzer, Anél ; Petzer, Jacobus P ; Cloete, Stephanus J ;
Abstract: Acetylcholinesterase (AChE) is present in the venom of Elapid snakes, except the Mambas. Although the physiological role of AChE in snake venom is uncertain, it may contribute to acute neuromuscular paralysis following envenomation. With the aim of repurposing clinically used drugs for snakebite envenoming, this study investigated the inhibition of AChE from snake species of Southern Africa. Hemachatus haemachatus and Naja nivea venom presented with high AChE activity, which was inhibited by tacrine, galantamine and donepezil with IC50 values ranging from 0.49 to 3.73 μM.
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| CAS No. : | 120014-06-4 |
| Formula : | C24H29NO3 |
| M.W : | 379.49 |
| SMILES Code : | C1=C2C(=CC(=C1OC)OC)CC(C2=O)CC4CCN(CC3=CC=CC=C3)CC4 |
| Synonyms : |
E2020 free base; Aricept; HSDB 7743
|
| MDL No. : | MFCD00912833 |
| InChI Key : | ADEBPBSSDYVVLD-UHFFFAOYSA-N |
| Pubchem ID : | 3152 |
| GHS Pictogram: |
|
| Signal Word: | Warning |
| Hazard Statements: | H315-H319-H335 |
| Precautionary Statements: | P261-P305+P351+P338 |
| Target |
|
In Vitro:
| Concentration | Treated Time | Description | References |
| OPC-DRG neuron co-culture | 10 μM | 9 days | Donepezil promotes myelination in OPC-DRG neuron co-culture. | Acta Pharmacol Sin. 2019 Nov;40(11):1386-1393. |
| Primary OPCs | 2.5–20 μM | 4 days | Donepezil significantly increases the percentage of MBP+ OLs generated from primary OPCs. | Acta Pharmacol Sin. 2019 Nov;40(11):1386-1393. |
| Mouse 6-3 microglial cells | 5 μM | 12 hours | Pretreatment with donepezil suppressed the TNFα-induced sustained intracellular Ca2+ elevation | J Neuroinflammation. 2017 Dec 22;14(1):258. |
| Mouse primary microglial cells | 5 μM | 12 hours | Pretreatment with donepezil suppressed the TNFα-induced sustained intracellular Ca2+ elevation | J Neuroinflammation. 2017 Dec 22;14(1):258. |
| Rat HAPI microglial cells | 5 μM | 12 hours | Pretreatment with donepezil suppressed the TNFα-induced sustained intracellular Ca2+ elevation | J Neuroinflammation. 2017 Dec 22;14(1):258. |
| APPsw-SY5Y cells | 10 μmol/L | 2 hours | To evaluate the inhibitory effect of donepezil on copper-induced Aβ1-42 production, results showed that donepezil significantly reduced Aβ1-42 production | Acta Pharmacol Sin. 2016 Nov;37(11):1401-1412. |
| Th17 cells | 5 μM | 48 hours | To evaluate the effect of Donepezil on Th17 cell differentiation. Results showed that Donepezil significantly reduced the expression of IL17A in Th17 cells and inhibited the activation of the JAK2-STAT3 signaling pathway. | Theranostics. 2023 Mar 21;13(6):1826-1842. |
| NPC-derived OPCs | 20 μM | 4.5 days | Donepezil significantly promotes OPC to OL differentiation, increasing the percentage of MBP+ cells. | Acta Pharmacol Sin. 2019 Nov;40(11):1386-1393. |
In Vivo:
| Administration | Dosage | Frequency | Description | References |
| Rat | Passive avoidance test model | Oral | 0.1 mg/kg | Single dose | Evaluate the effect of Donepezil in the passive avoidance test model | Cell. 2021 Nov 24;184(24):5886-5901.e22 |
| C57BL/6 mice | BLM-induced lung fibrosis mouse model | Intraperitoneal injection | 1 mg/kg | Once daily for 21 days | To evaluate the effect of Donepezil on BLM-induced lung fibrosis and pulmonary hypertension. Results showed that Donepezil significantly improved pulmonary artery and RV remodeling, reduced lung fibrosis, and inhibited Th17 cell infiltration and activation. | Theranostics. 2023 Mar 21;13(6):1826-1842. |
| Male mice | VGLUT3T8I/T8I mutant mice | Intraperitoneal injection | 0.3 mg/kg | Daily throughout the entire ABA paradigm | To evaluate the effect of donepezil on reversing the self-starvation phenotype in VGLUT3T8I/T8I mice, showing that donepezil effectively reversed the self-starvation behavior in mutant mice. | Nat Commun. 2024 Jul 7;15(1):5691 |
| Mice | VAChTcKO mice | Intraperitoneal injection | 0.3 mg/kg | Chronic treatment | Increasing cholinergic signaling by AChE inhibition was fully effective to treat the anorexia-like phenotype in VAChTcKO mice. | J Clin Invest. 2020 Dec 1;130(12):6616-6630 |
| Mice | Scopolamine-induced memory-deficient mouse model | Intracalvariosseous administration | 5 mg/kg | Single administration, lasting four weeks | To evaluate the long-term cognitive improvement effect of DPZ@LAM, results showed that a single ICO of DPZ@LAM significantly recovered cognitive function in scopolamine-induced memory-deficient mice, along with decreased acetylcholinesterase activity and increased brain-derived neurotrophic factor. | Theranostics. 2024 Oct 14;14(17):6708-6725 |
| Mouse | Drd1a-tdTomato/Drd2-mVenus double transgenic mice | Subcutaneous injection | 0.4 mg/kg | Single dose | To investigate the enhancement of aversive learning by donepezil through M1R-PKC-PAK signaling | Mol Psychiatry. 2022 Aug;27(8):3479-3492. |
| Mice | Chronic stress model | Intraperitoneal injection | 1.0 mg/kg | Single administration | Investigated the effects of Donepezil on cognitive and emotional deficits in chronically stressed mice. Results showed Donepezil alone improved cognitive deficits but exacerbated anxiety-like behaviors, while combined with vHPC M1 receptor blockade rescued both phenotypes. | Sci Adv. 2024 Nov 8;10(45):eado1508 |
| C57BL/6 mice | Cuprizone-induced demyelination model | Intraperitoneal injection | 1.5 and 5 mg/kg | Daily for 1–3 weeks | Donepezil significantly promotes remyelination in vivo, reducing demyelination area and increasing myelin formation. | Acta Pharmacol Sin. 2019 Nov;40(11):1386-1393. |
| Mice | 3xTg and 5xFAD mouse models | Intraperitoneal injection | 1.0 and 2.0 mg/kg | Daily for 4 weeks | Low-dose donepezil significantly ameliorated MS-hTau-induced spatial memory deficits and reduced tau accumulation, with more prominent effects than high dose. | Clin Transl Med. 2021 Jun;11(6):e428 |
| C57BL6/J mice | AlCl3-induced Alzheimer's disease model | Nasal administration | 30 mg/kg | Once daily for 7 weeks | To evaluate the improvement of cognitive function and memory ability in AlCl3-induced AD mice by GH/CeO2NPs, results showed significant improvement. | Int J Mol Sci. 2024 Apr 11;25(8):4262 |
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| Bio Calculators | ||||
| Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.64mL 0.53mL 0.26mL |
13.18mL 2.64mL 1.32mL |
26.35mL 5.27mL 2.64mL |
|
| Dissolving Methods |
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:
in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
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