Donepezil hydrochloride monohydrate

Manufactured by Merck Group

Sourced in United States

Donepezil hydrochloride monohydrate is a chemical compound used as a pharmaceutical ingredient. It is a white crystalline powder that is soluble in water. The compound is typically used in the production of medications, but its core function is not to be interpreted or extrapolated upon.

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Donepezil hydrochloride Donepezil Hydrochlorides

10 protocols using donepezil hydrochloride monohydrate

Electrochemical Acetylcholinesterase Inhibition Assay

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Donepezil hydrochloride monohydrate (≥98%), berberine chloride dihydrate (≥98%), AChE from electric eel (EC 3.1.1.7, 518 U mg⁻¹), ATCh, poly(lactic acid), thionine acetate (3,7-diamino-5-phenothiazinium acetate), Methylene blue (MB, 3,7-bis(dimethylamino)phenazathionium chloride), N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide chloride (EDC), N-hydroxysuccinimide (NHS), pralidoxime (2-pyridine aldoxime methiodide, 2-PAM), and carbofuran (2,3-dihydro-2,2-dimethylbenzofuran-7-yl methylcarbamate) were purchased from Sigma-Aldrich (St. Louis, MO, USA). Unsubstituted P[5]A was synthesized at the Organic Chemistry Department of Kazan Federal University by the modified Ogoshi method [42 (link)]. Carbon black N 220 (CB, >99.95% C) was purchased from Imerys Graphite&Carbon (Willebroek, Belgium). All the working solutions were prepared using Millipore Q^® water (Simplicity^® water purification system, Merck-Millipore, Molsheim, France). Other reagents were of analytical grade.
Artificial urine contained 10 mM CaCl₂, 6 mM MgCl₂, 6 mM Na₂SO₄, 2 mM potassium citrate, 20 mM KH₂PO₄, 21 mM KCl, 18 mM NH₄Cl, 9 mM creatinine and 416 mM urea.
Electrochemical measurements were performed in a 0.1 M phosphate buffer containing 0.1 M KCl.

Ivanov A., Stoikov D., Shafigullina I., Shurpik D., Stoikov I, & Evtugyn G. (2022). Flow-Through Acetylcholinesterase Sensor with Replaceable Enzyme Reactor. Biosensors, 12(9), 676.

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Spinosin-Mediated Neuroprotection in Alzheimer's

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Spinosin was provided by one of the authors (D.S. Jang) and the purity of this sample was greater than 99%. The Aβ_1–42 protein fragment and donepezil hydrochloride monohydrate were purchased from Sigma Chemical Co. (St. Louis, MO, USA). Rabbit polyclonal anti-glial fibrillary acidic protein (GFAP) antibody was purchased from Invitrogen Co. (Carlsbad, CA, USA). Rat polyclonal anti-OX-42 and goat polyclonal anti-ChAT antibodies were purchased from Chemicon (Temecula, CA, USA). All other materials were of the highest grade commercially available.

Ko S.Y., Lee H.E., Park S.J., Jeon S.J., Kim B., Gao Q., Jang D.S, & Ryu J.H. (2015). Spinosin, a C-Glucosylflavone, from Zizyphus jujuba var. spinosa Ameliorates Aβ1–42 Oligomer-Induced Memory Impairment in Mice. Biomolecules & Therapeutics, 23(2), 156-164.

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Pharmacological Compound Acquisition

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Carrageenan, dexamethasone, scopolamine hydrobromide, and donepezil hydrochloride monohydrate were purchased from Sigma—Aldrich Co. (St. Louis, MO, USA). All chemical reagents and solvents used were of analytical grade (Vetec, Rio de Janeiro, Brazil).

Formagio A.S., Vilegas W., Kassuya C.A., De Almeida V.P., Manfron J., Konkiewitz E.C., Ziff E.B., Faoro J.A., Dos Santos J.M., Cecatto A.J., Sarragiotto M.H, & Mussury R.M. (2024). A Comprehensive Description of the Anatomy and Histochemistry of Psychotria capillacea (Müll. Arg.) Standl. and an Investigation into Its Anti-Inflammatory Effects in Mice and Role in Scopolamine-Induced Memory Impairment. Pharmaceuticals, 17(5), 564.

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Scopolamine Hydrobromide Neuroprotective Effects

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Scopolamine hydrobromide, demethoxycurcumin (DMC), and donepezil hydrochloride monohydrate (DNP) were purchased from Sigma (St. Louis, MO, USA). DMC (10 mg/kg) or DNP (2 mg/kg) as a positive control were dissolved in corn oil and orally administered once a day for 28 consecutive days. The normal group was administered the vehicle solution (1 mL/kg, p.o.) using the same schedule of administration. On day 28, the mice were exposed to the behavioral experiments 1 h after the administration.

Lim D.W., Son H.J., Um M.Y., Kim I.H., Han D., Cho S, & Lee C.H. (2016). Enhanced Cognitive Effects of Demethoxycurcumin, a Natural Derivative of Curcumin on Scopolamine-Induced Memory Impairment in Mice. Molecules, 21(8), 1022.

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Biflorin Neuroprotective Effects Protocol

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Biflorin was provided by one of the authors (D.S. Jang) and suspended in 10% Tween 80 solution. Donepezil hydrochloride monohydrate, scopolamine hydrobromide, and dizocilpine (MK-801) were purchased from Sigma-Aldrich (St Louis, MO, USA). Antibodies against calcium/calmodulin-dependent protein kinase II (CaMKII), protein kinase C-ζ (PKC-ζ), phosphorylated PKC-ζ at Thr 410, cAMP response element-binding protein (CREB) at Ser 133, extracellular signal-regulated kinase (ERK), and phosphorylated ERK at Thr202/Tyr204 antibodies were purchased from Santa Cruz Biotechnology, Inc. (Santa Cruz, CA, USA). Antibody against phosphorylated CaMKII at Thr 286 (pCaMKII) was purchased from Abcam (Cambridge, UK). All other materials were obtained from normal commercial sources and were of the highest grade available. All drugs were freshly made on the day of testing. Donepezil, a positive control, and scopolamine were dissolved in a 0.9% saline solution.

Jeon S.J., Kim B., Ryu B., Kim E., Lee S., Jang D.S, & Ryu J.H. (2016). Biflorin Ameliorates Memory Impairments Induced by Cholinergic Blockade in Mice. Biomolecules & Therapeutics, 25(3), 249-258.

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Nicotine and Donepezil Interaction in Fear Conditioning

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Nicotine hydrogen tartrate salt (Sigma, N5260) and donepezil hydrochloride monohydrate (Sigma, D6821) were dissolved in 0.9% sterile saline. For the dose response experiment, donepezil (0.015, 0.05, 0.15, 0.5, 1.5 mg/kg, doses based on previous research (Geerts et al., 2005 (link))) or saline was administered s.c. 30 mins prior to fear conditioning training and testing. For the withdrawal study, chronic nicotine (12.6 mg/kg/day, dose based on previous research (André, Gulick, Portugal, & Gould, 2008 (link))) or saline was administered s.c. via osmotic-mini pumps for 12 days; mice were then trained 24 hours after cessation of nicotine administration.

Poole R.L., Connor D.A, & Gould T.J. (2014). Donepezil reverses nicotine withdrawal-induced deficits in contextual fear conditioning in C57BL/6J mice. Behavioral neuroscience, 128(5), 588-593.

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Quantification of Insoluble Amyloid-Beta

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4-(2-hydroxyethyl)-1-piperazinepropanesulfonic acid (EPPS), donepezil hydrochloride monohydrate, thioflavin-S, and protease inhibitor cocktail were from Sigma-Aldrich (St. Louis, MO). Deionized water was generated by a Milli-Q plus from Millipore (Bedford, MA). A RIPA buffer and phosphate buffered saline (PBS buffer) were purchased from ThermoFisher. (Roxkford, IL). Immunoassay kits for insoluble fraction of Aβ quantifications were used from Invitrogen (KHB3442, Camarillo, CA).

Kim H.Y., Kim H.V., Lee D.K., Yang S.H, & Kim Y. (2016). Rapid and sustained cognitive recovery in APP/PS1 transgenic mice by co-administration of EPPS and donepezil. Scientific Reports, 6, 34165.

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Acetylcholine and BDNF Assay Protocol

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Donepezil hydrochloride monohydrate and scopolamine hydrobromide were purchased from Sigma Chemical Co. (St. Louis, MO, USA). Acetylcholine ELISA kit and acetylcholinesterase ELISA kit were purchased from Elabscience Biotechnology Co. (Houston, TX, USA). Anti-β-actin antibody was purchased from Sigma Chemical Co. Anti-BDNF antibodies were purchased from Abcam (Cambridge, UK). All other materials were obtained from normal commercial sources and were of the highest grade available.

Kim S.K., Kwon D.A., Kim Y.S., Lee H.S., Kim H.K, & Kim W.K. (2021). Standardized Extract (HemoHIM) Protects against Scopolamine-Induced Amnesia in a Murine Model. Evidence-based Complementary and Alternative Medicine : eCAM, 2021, 8884243.

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Pharmacological Interventions in Cognitive Impairment

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Galangin (Alfa Aesar) were dissolved in distilled water: DMSO (5:1 ratio) and administered intraperitoneally. Donepezil hydrochloride monohydrate (Sigma-Aldrich) and mecamylamine hydrochloride (Santa Cruz Biotechnology) were dissolved in saline and injected subcutaneously. Scopolamine hydrobromide trihydrate (Acros Organics) were dissolved in saline and given intraperitoneally.

Kilic F.S., Kaygisiz B., Aydin S., Yildirim E., Oner S, & Erol K. (2019). The effects and mechanisms of the action of galangin on spatial memory in rats. Bratislavske lekarske listy, 120(12).

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Pharmacological administration protocols for cognitive studies

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Donepezil hydrochloride monohydrate (Sigma, UK) was dissolved in 0.5% carboxymethylcellulose and given in a volume of 1 ml/kg via the intraperitoneal (i.p.) route.
Risperidone (Sigma, UK) was dissolved in a minimum volume of acetic acid, made up to volume with distilled water and pH adjusted to 6 with 0.1M NaOH. Risperidone was administered in a volume of 1 ml/kg via the i.p. route. PNU-282987 (Tocris, UK) was dissolved in isotonic water and given in a volume of 1 ml/kg via the sub-cutaneous (s.c.) route. RJR-2403 oxalate (Tocris, UK) was dissolved in 0.9% saline and given in a volume of 1 ml/kg via the s.c. route. All drug doses were calculated as base equivalent weight and were administered 30 min before the acquisition trial, with the exception of PNU-282987 which was administered 60 min before the acquisition trial. In experiment 3 all drugs were given 30 min before the retention trial, except PNU-282987 which was administered 60 min before the retention trial.

McLean S.L., Grayson B., Marsh S., Zarroug S.H., Harte M.K, & Neill J.C. (2016). Nicotinic α7 and α4β2 agonists enhance the formation and retrieval of recognition memory: Potential mechanisms for cognitive performance enhancement in neurological and psychiatric disorders. Behavioural brain research, 302.

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