Donepezil-d₅ hydrochloride  (Synonyms: E2020-d₅)

Donepezil-d₅ (hydrochloride) is deuterium labeled Donepezil (Hydrochloride). Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

420.98

C₂₄H₂₅D₅ClNO₃

1883548-90-0

120011-70-3

Solid

White to off-white

O=C1C(CC2=CC(OC)=C(C=C21)OC)CC3CCN(CC3)CC4=C(C([2H])=C(C([2H])=C4[2H])[2H])[2H].Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. H Ogura, et al. Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase in vitro. Methods Find Exp Clin Pharmacol. 2000 Oct;22(8):609-13.  [Content Brief]

  [3]. Min-Young Noh,et al. Neuroprotective effects of donepezil through inhibition of GSK-3 activity in amyloid-beta-induced neuronal cell death. J Neurochem. 2009 Mar;108(5):1116-25.  [Content Brief]

  [4]. Chang Yell Shin, et al. The Effects of Donepezil, an Acetylcholinesterase Inhibitor, on Impaired Learning and Memory in Rodents. Biomol Ther (Seoul). 2018 May 1;26(3):274-281.  [Content Brief]