Synonyms:Acetylcholine esterase;Acetyl b-methylcholinesterase;Acetylcholine acetylhydrolase;Acetylcholineesterase;Acetylcholine hydrolase;Acetylcholinesterase;Acetylthiocholinesterase;E.C. 3.1.1.7;
99%, *data from raw suppliers
Acetylcholinesterase *data from reagent suppliers
B
The research focuses on developing an efficient one-cycle affinity selection method using a T7 phage display pool to identify binding proteins or peptides specific for small molecules. The study employs a cuvette type 27-MHz quartz-crystal microbalance (QCM) apparatus with a self-assembled monolayer (SAM) for immobilizing specific small molecules on the gold electrode surface of a sensor chip. The researchers used this system to screen for proteins or peptides that bind to synthetic ligand for FK506-binding protein (SLF) or the anti-tumor drug irinotecan (Iri, CPT-11). They successfully detected FK506-binding protein 12 (FKBP12)-displaying T7 phage with a short interaction time of 10 minutes, avoiding extensive wash or elution conditions and multiple rounds of selection. Additionally, a random-peptide T7 phage pool was utilized along with RELIC software for bioinformatics analysis, which helped pinpoint specific amino acid residues within the binding site of FKBP12 and regions of the Iri-binding site on known targets, acetylcholinesterase (AChE), and carboxylesterase (CE). The study demonstrates the method's effectiveness and broad applicability for screening small-molecule binding proteins/peptides. Reactants included SLF and Iri derivatives synthesized for forming SAM, natural-protein and random-peptide T7 phage pools, and His-tagged FKBP12. Analyses involved QCM monitoring, agarose gel electrophoresis, DNA sequencing, and bioinformatics tools like RELIC software.
The research presents a study on the development of novel multitarget-directed ligands (MTDLs) for the treatment of Alzheimer's disease. The purpose of the research was to design compounds capable of simultaneously inhibiting acetylcholinesterase (AChE) and acting as agonists of the 5-HT4 receptor, as well as targeting sigma-1 receptors, based on the hypothesis that a pleiotropic intervention is necessary for effective limitation of the progression of Alzheimer's disease. The researchers synthesized a series of indole derivatives, starting from donecopride, which were evaluated for their in vitro activities towards AChE and the σ1 receptor, with selected compounds showing promising results. The crystal structures of the most promising compounds with Torpedo californica AChE were solved to understand their mode of inhibition. The study concluded that some of the synthesized indole derivatives displayed potent nanomolar inhibition of hAChE and affinity for the σ1 receptor, suggesting a potential therapeutic approach for Alzheimer's disease treatment. This was supported by preliminary in vivo experiments where one of the compounds, 6c, showed a protective effect against dizocilpine-induced impairment in the passive avoidance test in mice, correlating with its in vitro σ1 receptor affinity.
The research focuses on the synthesis and pharmacological activity of certain 2,3-dihydroimidazo[1,2-a]benzimidazoles and their intermediates. The purpose of the study was to explore the potential hypotensive and hypoglycemic properties of these compounds, which contain a common nitrogen atom and an imidazoline ring, and have been found to exhibit a broad spectrum of pharmacological activity. The researchers synthesized new derivatives of 9H-2,3-dihydroimidazo[1,2-a]benzimidazole and investigated their pharmacological properties, including their effects on blood sugar levels and arterial pressure in rats, as well as their influence on the enzymatic activity of cyclic AMP phosphodiesterase (cAMP PDE) and acetylcholine esterase (ACE). The chemicals used in the synthesis process included various alkyl- and aralkyl-substituted benzimidazoles, chloroethylaminobenzimidazoles, and methoxyethylaminobenzimidazoles, among others. The conclusions drawn from the study indicated that some of the synthesized imidazo[1,2-a]benzimidazole derivatives showed promising hypoglycemic and hypotensive effects, and certain compounds demonstrated inhibitory activity against cAMP PDE and ACE, suggesting potential therapeutic applications. However, the overall effectiveness of these compounds was found to be less than that of some reference preparations, such as adebite (a quinidine derivative).
The study explores the potential of N-methylpiperidinyl thioesters as surrogate substrates for evaluating corresponding ester compounds as imaging agents for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) in neurological disorders like Alzheimer's disease. The researchers synthesized various N-methylpiperidinyl thioesters and esters, including derivatives from aryl acid chlorides (4-cyanobenzenecarbothioate, 4-fluorobenzenecarbothioate, and 4-iodobenzenecarbothioate) and alkyl acid chlorides (ethanethioate, propanethioate, and butanethioate), as well as their corresponding esters. These compounds were used to conduct enzyme kinetics studies to determine their affinities and hydrolysis rates by AChE and BuChE. The thioesters were also employed in histochemical evaluations to visualize cholinesterase activity in human brain tissue. The results showed that the thioesters had comparable affinities to their ester counterparts and could effectively visualize cholinesterase distribution in brain tissue, suggesting their potential as screening tools for developing imaging agents targeting the cholinergic system.
The research aims to develop a versatile synthetic approach to create analogs of physovenine and physostigmine, which are known acetylcholinesterase (AChE) inhibitors used in treating conditions like myasthenia gravis, glaucoma, and Alzheimer's disease. The study's purpose is to establish structure-activity relationships (SAR) among these analogs to understand their inhibitory activities against human AChE and butyrylcholinesterase (BuChE). The synthesis process involves multiple steps, including radical cyclization to form the spiro-oxindole ring, acetylation, N-alkylation, and reductive radical cyclization. The most potent analogs identified were 21a with an IC50 value of 70 nM against hBuChE and 21g with an IC50 value of 53 nM against hAChE. The study concludes that the size of the substituent at the quaternary carbon center significantly affects the inhibitory activity against hAChE, with smaller alkyl substituents generally yielding more active compounds. Conversely, larger arylalkyl substituents were more effective against hBuChE. This work provides valuable insights into the SAR of physovenine and physostigmine analogs, guiding future drug design efforts.
What can I do for you?
Get Best Price
Total 8 Pictures about this product
