Donepezil HCl(Aricept) is a selective and effective AChE inhibitor for bAChE and hAChE (IC50: 8.12/11.6 nM).

AChE (human):11.6 nM, AChE (bovine):8.12 nM

Donepezil以浓度依赖的方式抑制人类SHSY5Y神经母细胞系中carbachol诱导的细胞内Ca2+浓度增加，表明Donepezil具有抗胆碱能活性。[2] 最近的研究表明，Donepezil能够保护人类脐静脉内皮细胞(HUVECs)免受Water2引起的细胞损伤。这对于心血管和脑血管疾病中的氧化应激潜在治疗具有重要意义。[3]

大鼠腹腔内注射Donepezil导致剂量依赖性的增加唾液分泌和震颤，这些是明显的 Choline 能行为表现，其ED50为6μmol/kg。口服给药后，Donepezil的效力略低，ED50为50μmol/kg。[2]。在体内单独给药时，5-HT(4)受体诱导剂RS67333（0.3及1 mg/kg）和Donepezil（1 mg/kg）比生理盐水处理的小鼠改善了识别性能，而RS67333（0.1 mg/kg）和Donepezil（0.3 mg/kg）的低活性剂量联合给药可以改善记忆。然而，如果同时给予5-HT(4)R拮抗剂（GR125487，10 mg/kg），这种改善会被阻止。[4]

[3H]-Pyrilamine binding to histamine (H1) receptors in guinea pig cerebellum membranes.: Antagonists are incubated with guinea pig cerebellum membranes (0.6 mg/ml) and [3H]-pyrilamine (1.2 nM) in 0.5 ml 50 mM PBS, pH 7.5, for 30 min at 25 ℃. The incubation is ended by the addition of 5 ml of ice-cold PBS containing 2 μM pyrilamine and the collection of membranes on Whatman GF/B filters. Then the filters are washed with 3 × 5 ml of ice-cold PBS plus 2 μM pyrilamine and transferred to counting vials. The radioactivity retained by each filter is measured by liquid scintillation counting in 3 ml of HiSafe 3. Specific binding is determined from the difference between the [3H]-pyrilamine bound in the absence and in the presence of a large molar excess (10 μM) of unlabeled promethazine.