OBJECTIVE To study the long-term dual inhibitory effects of rivastigmine on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) in patients with AD. METHODS Eleven patients with mild AD received rivastigmine for 12 months. Cholinesterase (ChE) activities in the CSF and plasma were assessed colorimetrically. Immunoblot analysis was used to evaluate AChE isoforms. Neuropsychiatric tes...

The effect of transient cerebral ischemia on acetylcholinesterase (AChE) synthesis was studied in rats by a modified pharmacohistochemical method. The procedure involved in vivo irreversible inhibition of AChE by administration of the inhibitor diisopropyl fluorophosphate (DFP; 1.2 mg/kg b.w., i.m.) 1 h before 30 min forebrain ischemia (the four-vessel occlusion model). At the onset of ischemia...

To determine if donepezil, an acetylcholinesterase (AChE) inhibitor, improved the assimilation of cognitive training by older adults with memory complaints, we gave 168 nondemented, community-dwelling volunteers with memory complaints either 5 mg of donepezil (Aricept) or placebo daily for 6 weeks in a randomized, double-blind, placebo-controlled trial. The dosage rose to 10 mg daily for anothe...

Acetylcholinesterase (AChE), an important component of cholinergic synapses, colocalizes with amyloid-beta peptide (A beta) deposits of Alzheimer's brain. We report here that bovine brain AChE, as well as the human and mouse recombinant enzyme, accelerates amyloid formation from wild-type A beta and a mutant A beta peptide, which alone produces few amyloid-like fibrils. The action of AChE was i...

Tacrine (THA), the first clinically effective acetylcholinesterase (AChE) inhibitor and the first approved drug for the treatment of Alzheimer's disease (AD), was withdrawn from the market due to its side effects, particularly its hepatotoxicity. Nowadays, THA serves as a valuable scaffold for the design of novel agents potentially applicable for AD treatment. One such compound, namely 7-methox...

Balanced dopaminergic cholinergic interactions are crucial for proper basal ganglia function. This is dramatically demonstrated by the worsening of Parkinson's disease symptoms following acetylcholinesterase (AChE) inhibition. Typically, in the brain, the synapse-anchored synaptic AChE (AChE-S) variant is prevalent whereas the soluble readthrough AChE (AChE-R) variant is induced in response to ...

Alzheimer merupakan penyakit neurodegeneratif yang disebabkan oleh penurunan sintesis asetilkolin akibat pemecahan menjadi kolin dan asetat enzim asetilkolinesterase (AChE). Senyawa dengan aktivitas inhibitor AChE diketahui kandidat obat menjanjikan untuk mengobati ini. Pada penelitian ini, dilakukan studi in-silico terhadap senyawa dalam Daun Sirih (Piper betle L.) sebagai anti-alzheimer mengg...

Alzheimer’s disease (AD) is a neurodegenerative age-related brain which diminishes learning and memory. Two main cholinesterases (ChEs), first acetylcholinesterase (AChE) second one butyrylcholinesterase (BChE) are the major targets to treat this disease. In current study, six novel pyrazolo-benzothiazole analogues were systematically planned, synthesized, biological tested for their ChEs activ...

Nine compounds (MO1–MO9) containing the morpholine moiety were assessed for their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE). Most of potently inhibited MAO-B; MO1 most with an IC50 value 0.030 µM, followed by MO7 (0.25 µM). MO5 AChE (IC50 = 6.1 µM), MO9 12.01 µM) MAO-A 7.1 was a reversible mixed-type inhibitor MAO-B (Ki 0.018 µM); reversibly competi...

UNLABELLED We investigated the effects of rivastigmine (a cholinesterase inhibitor) and selegiline ((-)deprenyl, an irreversible inhibitor of monoamineoxidase-B), alone and in combination, on brain acetylcholinesterase (AChE), (Na(+), K(+))-, Mg(2+)-ATPase activities, total antioxidant status (TAS), and learning performance, after long-term drug administration in aged male rats. The possible re...