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The muscarinic agonist arecoline suppresses motor circuit hyperactivity in C. elegans.

Katherine A McCulloch, Yishi Jin,

MicroPubl Biol (microPublication biology)
[2020, 2020:]

Cited: 1 time

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Novel actions of arecoline in the C. elegans motor circuit.

Katherine A McCulloch, Yishi Jin,

MicroPubl Biol (microPublication biology)
[2020, 2020:]

Cited: 0 times

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Kavain suppresses human Aβ-induced paralysis in C. elegans.

Manish Chamoli, Shankar J Chinta, Julie K Andersen, Gordon J Lithgow,

MicroPubl Biol (microPublication biology)
[2020, 2020:]

Cited: 0 times

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Interspecific comparison of sensitivity to paralytic compounds.

Vivian Vy Le, Bryan Sanchez, Ray Hong,

MicroPubl Biol (microPublication biology)
[2019, 2019:]

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nu444 is a novel allele of pkc-1 in C. elegans.

Han Wang, Derek Sieburth,

MicroPubl Biol (microPublication biology)
[2017, 2017:]

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Enzyme-digested Colla Corii Asini (E'jiao) prevents hydrogen peroxide-induced cell death and accelerates amyloid beta clearance in neuronal-like PC12 cells.

Li Xiao, Feng Liao, Ryoji Ide, Tetsuro Horie, Yumei Fan, Chikako Saiki, Nobuhiko Miwa,

As an aging-associated degenerative disease, Alzheimer's disease is characterized by the deposition of amyloid beta (Aβ), oxidative stress, inflammation, dysfunction and loss of cholinergic neurons. Colla Corii Asini (CCA) is a traditional Chinese medicine which has been used for feebleness-related diseases and anti-aging. CCA might delay aging-induced degenerative changes in ... Read more >>

Neural Regen Res (Neural regeneration research)
[2020, 15(12):2270-2272]

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Calcium and potassium channels are involved in curcumin relaxant effect on tracheal smooth muscles.

Bahman Emami, Farzaneh Shakeri, Zahra Gholamnezhad, Saeideh Saadat, Marzie Boskabady, Vahab Azmounfar, Hamed Sadatfaraji, Mohammad Hossein Boskabady,

Context: Curcumin, the active component of Curcuma longa L. (Zingiberaceae), exhibits a wide variety of biological activities including vasodilation and anti-inflammation.Objective: The relaxant effect of curcumin in tracheal smooth muscle (TSM) was not examined so far, thus, this study was designed to assess the relaxant effect of curcumin on rat ... Read more >>

Pharm Biol (Pharmaceutical biology)
[2020, 58(1):257-264]

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Design, synthesis and cholinesterase inhibitory properties of new oxazole benzylamine derivatives.

Ivana Šagud, Nikolina Maček Hrvat, Ana Grgičević, Tena Čadež, Josipa Hodak, Milena Dragojević, Kornelija Lasić, Zrinka Kovarik, Irena Škorić,

The enzymes acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are primary targets in attenuating the symptoms of neurodegenerative diseases. Their inhibition results in elevated concentrations of the neurotransmitter acetylcholine which supports communication among nerve cells. It was previously shown for trans-4/5-arylethenyloxazole compounds to have moderate AChE and BChE inhibitory properties. A preliminary ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):460-467]

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Polygala tenuifolia: a source for anti-Alzheimer's disease drugs.

Xinxin Deng, Shipeng Zhao, Xinqi Liu, Lu Han, Ruizhou Wang, Huifeng Hao, Yanna Jiao, Shuyan Han, Changcai Bai,

Context: Alzheimer's disease (AD) is a chronic neurodegenerative disease that originates from central nervous system lesions or recessions. Current estimates suggest that this disease affects over 35 million people worldwide. However, lacking effective drugs is the biggest handicap in treating AD. In traditional Chinese medicine (TCM), Polygala tenuifolia Willd. (Polygalaceae) ... Read more >>

Pharm Biol (Pharmaceutical biology)
[2020, 58(1):410-416]

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Synthesis of calix[4]azacrown substituted sulphonamides with antioxidant, acetylcholinesterase, butyrylcholinesterase, tyrosinase and carbonic anhydrase inhibitory action.

Mehmet Oguz, Erbay Kalay, Suleyman Akocak, Alessio Nocentini, Nebih Lolak, Mehmet Boga, Mustafa Yilmaz, Claudiu T Supuran,

A series of novel calix[4]azacrown substituted sulphonamide Schiff bases was synthesised by the reaction of calix[4]azacrown aldehydes with different substituted primary and secondary sulphonamides. The obtained novel compounds were investigated as inhibitors of six human (h) isoforms of carbonic anhydrases (CA, EC 4.2.1.1). Their antioxidant profile was assayed by various ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):1215-1223]

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Novel tacrine-benzofuran hybrids as potential multi-target drug candidates for the treatment of Alzheimer's Disease.

Gaia Fancellu, Karam Chand, Daniel Tomás, Elisabetta Orlandini, Luca Piemontese, Diana F Silva, Sandra M Cardoso, Sílvia Chaves, M Amélia Santos,

Pursuing the widespread interest on multi-target drugs to combat Alzheimer´s disease (AD), a new series of hybrids was designed and developed based on the repositioning of the well-known acetylcholinesterase (AChE) inhibitor, tacrine (TAC), by its coupling to benzofuran (BF) derivatives. The BF framework aims to endow the conjugate molecules with ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):211-226]

Cited: 1 time

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Sulphonamides incorporating 1,3,5-triazine structural motifs show antioxidant, acetylcholinesterase, butyrylcholinesterase, and tyrosinase inhibitory profile.

Nabih Lolak, Mehmet Boga, Muhammed Tuneg, Gulcin Karakoc, Suleyman Akocak, Claudiu T Supuran,

A series of 16 novel benzenesulfonamides incorporating 1,3,5-triazine moieties substituted with aromatic amines, dimethylamine, morpholine and piperidine were investigated. These compounds were assayed for antioxidant properties by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay, 2,2`-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical decolarisation assay and metal chelating methods. They were also investigated as inhibitors of ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):424-431]

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1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy.

Barbara Kaproń, Robert Czarnomysy, Mariusz Wysokiński, Rudolf Andrys, Kamil Musilek, Andrea Angeli, Claudiu T Supuran, Tomasz Plech,

There are numerous studies supporting the contribution of oxidative stress to the pathogenesis of epilepsy. Prolonged oxidative stress is associated with the overexpression of ATP-binding cassette transporters, which results in antiepileptic drugs resistance. During our studies, three 1,2,4-triazole-3-thione derivatives were evaluated for the antioxidant activity and anticonvulsant effect in the ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):993-1002]

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Synthesis of thiazolidin-4-ones and thiazinan-4-ones from 1-(2-aminoethyl)pyrrolidine as acetylcholinesterase inhibitors.

Adriana M das Neves, Gabriele A Berwaldt, Cinara T Avila, Taís B Goulart, Bruna C Moreira, Taís P Ferreira, Mayara S P Soares, Nathalia S Pedra, Luiza Spohr, Anita A A dE Souza, Roselia M Spanevello, Wilson Cunico,

The present study describes the synthesis of a novel series of thiazolidin-4-one and thiazinan-4-one using 1-(2-aminoethyl)pyrrolidine as amine precursor. All compounds were synthesised by one-pot three component cyclocondensation reaction from the amine, a substituted benzaldehyde and a mercaptocarboxylic acid. The compounds were obtained in moderate to good yields and were ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):31-41]

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Development of potent reversible selective inhibitors of butyrylcholinesterase as fluorescent probes.

Stane Pajk, Damijan Knez, Urban Košak, Maja Zorović, Xavier Brazzolotto, Nicolas Coquelle, Florian Nachon, Jacques-Philippe Colletier, Marko Živin, Jure Stojan, Stanislav Gobec,

Brain butyrylcholinesterase (BChE) is an attractive target for drugs designed for the treatment of Alzheimer's disease (AD) in its advanced stages. It also potentially represents a biomarker for progression of this disease. Based on the crystal structure of previously described highly potent, reversible, and selective BChE inhibitors, we have developed ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):498-505]

Cited: 1 time

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Advances in phytochemical and modern pharmacological research of Rhizoma Corydalis.

Bing Tian, Ming Tian, Shu-Ming Huang,

ABSRACTContext: Rhizoma Corydalis (RC) is the dried tubers of Corydalis yanhusuo (Y. H. Chou and Chun C. Hsu) W. T. Wang ex Z. Y. Su and C. Y. Wu (Papaveraceae). Traditionally, RC is used to alleviate pain such as headache, abdominal pain, and epigastric pain. Modern medicine shows that it ... Read more >>

Pharm Biol (Pharmaceutical biology)
[2020, 58(1):265-275]

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Synthesis, in vitro screening and molecular docking of isoquinolinium-5-carbaldoximes as acetylcholinesterase and butyrylcholinesterase reactivators.

David Malinak, Rafael Dolezal, Rafael Dolezal, Vendula Hepnarova, Miroslava Hozova, Rudolf Andrys, Petr Bzonek, Veronika Racakova, Jan Korabecny, Lukas Gorecki, Eva Mezeiova, Miroslav Psotka, Daniel Jun, Kamil Kuca, Kamil Musilek,

The series of symmetrical and unsymmetrical isoquinolinium-5-carbaldoximes was designed and prepared for cholinesterase reactivation purposes. The novel compounds were evaluated for intrinsic acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) inhibition, when the majority of novel compounds resulted with high inhibition of both enzymes and only weak inhibitors were selected for reactivation experiments ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):478-488]

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Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer's disease agents.

Jie Yang, Yinling Yun, Yuhang Miao, Jie Sun, Xiaojing Wang,

Multi-target drugs can better address the cascade of events involved in oxidative stress and the reduction in cholinergic transmission that occur in Alzheimer's disease than cholinesterase inhibitors alone. We synthesised a series of 3-arylbenzofuranone derivatives and evaluated their antioxidant activity, cholinesterase inhibitory activity, and monoamine oxidase inhibitory activity. 3-Arylbenzofuranone compounds ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):805-814]

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Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases.

Mustafa Durgun, Cüneyt Türkeş, Mesut Işık, Yeliz Demir, Ali Saklı, Ali Kuru, Abdussamat Güzel, Şükrü Beydemir, Suleyman Akocak, Sameh M Osman, Zeid AlOthman, Claudiu T Supuran,

Sulphonamides are biologically important compounds with low toxicity, many bioactivities and cost-effectiveness. Eight sulphonamide derivatives were synthesised and characterised by FT-IR, 13C NMR, 1H NMR, LC-MS and elemental analysis. Their inhibitory effect on AChE, and carbonic anhydrase I and II enzyme activities was investigated. Their antioxidant activity was determined using ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):950-962]

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Carbonic anhydrase modulation of emotional memory. Implications for the treatment of cognitive disorders.

Patrizio Blandina, Gustavo Provensi, Maria Beatrice Passsani, Clemente Capasso, Claudiu T Supuran,

Carbonic anhydrases (CAs, EC 4.2.1.1) are metalloenzymes which use CO2 as substrate, catalysing its interconversion to bicarbonate and a proton. In humans 15 CAs are expressed, 12 of which are catalytically active: the cytosolic CA I-III, VII, XIII, the membrane-bound CA IV, the mitochondrial CA VA and VB, the secreted ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):1206-1214]

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LC-QTOF-MS analysis of xanthone content in different parts of Garcinia mangostana and its influence on cholinesterase inhibition.

Kooi Yeong Khaw, Chun Wie Chong, Vikneswaran Murugaiyah,

Mangosteen is one of the best tasting tropical fruit widely cultivated in Southeast Asia. This study aimed to quantify xanthone content in different parts of Garcinia mangostana by LC-QTOF-MS and determine its influence on their cholinesterase inhibitory activities. The total xanthone content in G. mangostana was in the following order: ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):1433-1441]

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Design, synthesis and evaluation of quinolinone derivatives containing dithiocarbamate moiety as multifunctional AChE inhibitors for the treatment of Alzheimer's disease.

Jie Fu, Fengqi Bao, Min Gu, Jing Liu, Zhipeng Zhang, Jiaoli Ding, Sai-Sai Xie, Jinsong Ding,

A series of novel quinolinone derivatives bearing dithiocarbamate moiety were designed and synthesised as multifunctional AChE inhibitors for the treatment of AD. Most of these compounds exhibited strong and clearly selective inhibition to eeAChE. Among them, compound 4c was identified as the most potent inhibitor to both eeAChE and hAChE ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):118-128]

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Stability of motor endplates is greater in the biceps than in the interossei in a rat model of obstetric brachial plexus palsy.

Bo Li, Liang Chen, Yu-Dong Gu,

The time window for repair of the lower trunk is shorter than that of the upper trunk in patients with obstetric brachial plexus palsy. The denervated intrinsic muscles of the hand become irreversibly atrophic much faster than the denervated biceps. However, it is unclear whether the motor endplates of the ... Read more >>

Neural Regen Res (Neural regeneration research)
[2020, 15(9):1678-1685]

Cited: 0 times

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Mechanism of calcium potentiation of the α7 nicotinic acetylcholine receptor.

Kathiresan Natarajan, Nuriya Mukhtasimova, Jeremías Corradi, Matías Lasala, Cecilia Bouzat, Steven M Sine,

The α7 nicotinic acetylcholine receptor (nAChR) is among the most abundant types of nAChR in the brain, yet the ability of nerve-released ACh to activate α7 remains enigmatic. In particular, a major population of α7 resides in extra-synaptic regions where the ACh concentration is reduced, owing to dilution and enzymatic ... Read more >>

J. Gen. Physiol. (The Journal of general physiology)
[2020, 152(9):]

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Design, synthesis, in vitro and in vivo evaluation of benzylpiperidine-linked 1,3-dimethylbenzimidazolinones as cholinesterase inhibitors against Alzheimer's disease.

Jun Mo, Tingkai Chen, Hongyu Yang, Yan Guo, Qi Li, Yuting Qiao, Hongzhi Lin, Feng Feng, Wenyuan Liu, Yao Chen, Zongliang Liu, Haopeng Sun,

Cholinesterase inhibitor plays an important role in the treatment of patients with Alzheimer's disease (AD). Herein, we report the medicinal chemistry efforts leading to a new series of 1,3-dimethylbenzimidazolinone derivatives. Among the synthesised compounds, 15b and 15j showed submicromolar IC50 values (15b, eeAChE IC50 = 0.39 ± 0.11 µM; 15j, eqBChE IC50 = 0.16 ± 0.04 µM) towards acetylcholinesterase (AChE) ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2020, 35(1):330-343]

Cited: 1 time

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