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Cholinesterase inhibitors

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https://www.readbyqxmd.com/read/29332579/alzheimer-s-disease-a-systemic-review-of-substantial-therapeutic-targets-and-the-leading-multi-functional-molecules
#1
Tarana Umar, Nasimul Hoda
Alzheimer's disease (AD) is a fatal neurodegenerative disorder, having a complex aetiology with numerous possible drug targets. There are targets that have been known for years while more new targets and theories have also emerged. Beta amyloid and cholinesterases are the most significant biological targets for finding curative treatment of AD. The major class of drugs used for AD till now has been the Cholinesterase (ChE) inhibitors. Other prevailing models of molecular pathogenesis in AD include neurofibrillary tangles (NFTs) and amyloid deposition, tryptophan degradation pathway, kinase and phosphatase activity imbalance and neuroinflammation...
January 12, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29321572/specific-inhibition-of-acetylcholinesterase-as-an-approach-to-decrease-muscarinic-side-effects-during-myasthenia-gravis-treatment
#2
Konstantin A Petrov, Alexandra D Kharlamova, Oksana A Lenina, Ayrat R Nurtdinov, Marina E Sitdykova, Victor I Ilyin, Irina V Zueva, Evgeny E Nikolsky
Non-selective inhibitors of cholinesterases (ChEs) are clinically used for treatment of myasthenia gravis (MG). While being generally safe, they cause numerous adverse effects including induction of hyperactivity of urinary bladder and intestines affecting quality of patients life. In this study we have compared two ChEs inhibitors, a newly synthesized compound C547 and clinically used pyridostigmine bromide, by their efficiency to reduce muscle weakness symptoms and ability to activate contractions of urinary bladder in a rat model of autoimmune MG...
January 10, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29318278/effect-of-idalopirdine-as-adjunct-to-cholinesterase-inhibitors-on-change-in-cognition-in-patients-with-alzheimer-disease-three-randomized-clinical-trials
#3
Alireza Atri, Lutz Frölich, Clive Ballard, Pierre N Tariot, José Luis Molinuevo, Neli Boneva, Kristian Windfeld, Lars L Raket, Jeffrey L Cummings
Importance: New therapeutic approaches for Alzheimer disease (AD) are needed. Objective: To assess whether idalopirdine, a selective 5-hydroxytryptamine-6 receptor antagonist, is effective for symptomatic treatment of mild to moderate AD. Design, Setting, and Participants: Three randomized clinical trials that included 2525 patients aged 50 years or older with mild to moderate AD (study 1: n = 933 patients at 119 sites; study 2: n = 858 at 158 sites; and study 3: n = 734 at 126 sites)...
January 9, 2018: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/29317084/-reversal-of-neuromuscular-block-with-sugammadex-in-five-heart-transplant-pediatric-recipients
#4
Ricardo Vieira Carlos, Marcelo Luis Abramides Torres, Hans Donald de Boer
Heart transplantation is a frequent procedure in the treatment of end-stage cardiac dysfunction. Therefore, these patient populations will also be more frequent exposed to other more common surgical procedures after their transplantation. Anesthesiologist should be aware in their assessment of these patients, especially regarding some specific issues related to patients with a history of heart transplantation, like reversal of neuromuscular block. Several reports described that cholinesterase inhibitors drugs, like neostigmine, may produce a dose-dependent life-threatening bradycardia in heart transplant recipients while other publication described the safe use of neostigmine...
January 6, 2018: Revista Brasileira de Anestesiologia
https://www.readbyqxmd.com/read/29297118/novel-conjugates-of-tacrine-with-1-2-4-thiadiazole-as-highly-effective-cholinesterase-inhibitors-blockers-of-nmda-receptors-and-antioxidants
#5
G F Makhaeva, V V Grigoriev, A N Proshin, N V Kovaleva, E V Rudakova, N P Boltneva, I V Serkov, S O Bachurin
Conjugates of tacrine with 1,2,4-thiadiazole derivatives were synthesized for the first time. Their esterase profile and effects on the key NMDA receptor-binding sites as well as antioxidant activity were investigated. The obtained compounds effectively inhibited cholinesterases (with a predominant effect on butyrylcholinesterase), simultaneously blocked two NMDA receptor-binding sites (allosteric and intrachannel sites, and exhibited a high radical-scavenging activity. Our study shows that the obtained compounds are promising to design drugs for the treatment of Alzheimer's disease and other multifactorial neurodegenerative diseases...
November 2017: Doklady. Biochemistry and Biophysics
https://www.readbyqxmd.com/read/29296045/current-pharmacological-and-surgical-treatment-of-underactive-bladder
#6
REVIEW
Yuan-Hong Jiang, Cheng-Ling Lee, Jia-Fong Jhang, Hann-Chorng Kuo
Underactive bladder (UAB) or detrusor underactivity (DU) is a common yet still poorly understood urological problem. In addition to true detrusor failure and neuropathy, the inhibitory effects of detrusor contraction by the striated urethral sphincter and the bladder neck through alpha-adrenergic activity may also play a role in the development of UAB or DU. Treatment of UAB or DU aims to reduce the postvoid residual (PVR) urine volume and increase voiding efficiency, either by spontaneous voiding or abdominal straining...
October 2017: Ci Ji Yi Xue za Zhi, Tzu-chi Medical Journal
https://www.readbyqxmd.com/read/29283428/structure-related-inhibition-of-enzyme-systems-in-cholinesterases-and-bace1-in-vitro-by-naturally-occurring-naphthopyrone-and-its-glycosides-isolated-from-cassia-obtusifolia
#7
Srijan Shrestha, Su Hui Seong, Pradeep Paudel, Hyun Ah Jung, Jae Sue Choi
Cassia obtusifolia Linn. have been used to improve vision, inflammatory diseases, and as hepatoprotective agents and to promote urination from ancient times. In the present study, we investigated the influence of glycosylation of components of C. obtusifolia and structure-activity relationships (SARs) with respect to the inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein (APP)-cleaving enzyme 1 (BACE1), which are related to Alzheimer's disease (AD)...
December 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29282327/practice-guideline-update-summary-mild-cognitive-impairment-report-of-the-guideline-development-dissemination-and-implementation-subcommittee-of-the-american-academy-of-neurology
#8
Ronald C Petersen, Oscar Lopez, Melissa J Armstrong, Thomas S D Getchius, Mary Ganguli, David Gloss, Gary S Gronseth, Daniel Marson, Tamara Pringsheim, Gregory S Day, Mark Sager, James Stevens, Alexander Rae-Grant
OBJECTIVE: To update the 2001 American Academy of Neurology (AAN) guideline on mild cognitive impairment (MCI). METHODS: The guideline panel systematically reviewed MCI prevalence, prognosis, and treatment articles according to AAN evidence classification criteria, and based recommendations on evidence and modified Delphi consensus. RESULTS: MCI prevalence was 6.7% for ages 60-64, 8.4% for 65-69, 10.1% for 70-74, 14.8% for 75-79, and 25.2% for 80-84...
December 27, 2017: Neurology
https://www.readbyqxmd.com/read/29278947/synthesis-and-bioevaluation-of-new-tacrine-cinnamic-acid-hybrids-as-cholinesterase-inhibitors-against-alzheimer-s-disease
#9
Yao Chen, Jie Zhu, Jun Mo, Hongyu Yang, Xueyang Jiang, Hongzhi Lin, Kai Gu, Yuqiong Pei, Liang Wu, Renxiang Tan, Jing Hou, Jingyi Chen, Yang Lv, Yaoyao Bian, Haopeng Sun
Small molecule cholinesterases inhibitor (ChEI) provides an effective therapeutic strategy to treat Alzheimer's disease (AD). Currently, the discovery of new ChEI with multi-target effect is still of great importance. Herein, we report the synthesis, structure-activity relationship study and biological evaluation of a series of tacrine-cinnamic acid hybrids as new ChEIs. All target compounds are evaluated for their in vitro cholinesterase inhibitory activities. The representatives which show potent activity on cholinesterase, are evaluated for the amyloid β-protein self-aggregation inhibition and in vivo assays...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29277489/c-547-a-6-methyluracil-derivative-with-long-lasting-binding-and-rebinding-on-acetylcholinesterase-pharmacokinetic-and-pharmacodynamic-studies
#10
Konstantin Petrov, Irina Zueva, Irina Kovyazina, Igor Sedov, Sofya Lushchekina, Alexandra Kharlamova, Oksana Lenina, Sergei Koshkin, Yurii Shtyrlin, Evgeny Nikolsky, Patrick Masson
C-547, a potent slow-binding inhibitor of acetylcholinesterase (AChE) was intravenously administered to rat (0.05 mg/kg). Pharmacokinetic profiles were determined in blood and different organs: extensor digitorum longus muscle, heart, liver, lungs and kidneys as a function of time. Pharmacokinetics (PK) was studied using non-compartmental and compartmental analyses. A 3-compartment model describes PK in blood. Most of injected C-547 binds to albumin in the bloodstream. The steady-state volume of distribution (3800 ml/kg) is 15 times larger than the distribution volume, indicating a good tissue distribution...
December 22, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29260798/potential-for-intermittent-stimulation-of-nucleus-basalis-of-meynert-to-impact-treatment-of-alzheimer-s-disease
#11
David T Blake, Alvin V Terry, Marc Plagenhoef, Christos Constantinidis, Ruifeng Liu
The brain's cholinergic arousal pathways decline in parallel with the brain's executive functions in aging and Alzheimer's Disease. The frontline and currently most effective approach to treating Alzheimer's disease is the administration of cholinesterase inhibitors, which, in a dose dependent manner, improve the symptoms of cognitive decline over the first months of treatment before further decline occurs. We recently showed that intermittent deep brain stimulation of the nucleus basalis of Meynert improves working memory function in young adult monkeys, and that this improvement depended on cholinergic function...
2017: Communicative & Integrative Biology
https://www.readbyqxmd.com/read/29260408/practical-treatment-of-lewy-body-disease-in-the-clinic-patient-and-physician-perspectives
#12
Elisabet Londos
This article describes the practical considerations in the clinical medical treatment in dementia with Lewy body (DLB) patients. It is illustrated with the voice of a DLB sufferer and his wife. According to our experience, emanating from a 15 year collaboration between a doctor and a nurse at a memory clinic, there are several possible therapeutical entrances. However, the order in which the medication is introduced is of great importance to avoid aggravation of other DLB symptoms. We start the treatment with cholinesterase inhibitor and memantine, and; thereafter, we treat the most disturbing symptom...
December 19, 2017: Neurology and Therapy
https://www.readbyqxmd.com/read/29259546/neither-cholinergic-nor-dopaminergic-enhancement-improve-spatial-working-memory-precision-in-humans
#13
Adeola N Harewood Smith, Jnana Aditya Challa, Michael A Silver
Acetylcholine and dopamine are neurotransmitters that play multiple important roles in perception and cognition. Pharmacological cholinergic enhancement reduces excitatory receptive field size of neurons in marmoset primary visual cortex and sharpens the spatial tuning of visual perception and visual cortical fMRI responses in humans. Moreover, previous studies show that manipulation of cholinergic or dopaminergic signaling alters the spatial tuning of macaque prefrontal cortical neurons during the delay period of a spatial working memory (SWM) task and can improve SWM performance in macaque monkeys and human subjects...
2017: Frontiers in Neural Circuits
https://www.readbyqxmd.com/read/29248451/features-and-outcomes-of-drugs-for-combination-therapy-as-multi-targets-strategy-to-combat-alzheimer-s-disease
#14
REVIEW
Atish Kumar Sahoo, Jagnehswar Dandapat, Umesh Chandra Dash, Satish Kanhar
ETHNOPHARMACOLOGICAL RELEVANCE: Alzheimer's disease (AD), a deleterious neurodegenerative disorder that impairs memory, cognitive functions and may lead to dementia in late stage of life. The pathogenic cause of AD remains incompletely understood and FDA approved drugs are partial inhibitors rather than curative. Most of drugs are synthetic or natural products as galanthamine is an alkaloid obtained from Galanthus spp. Huperzine A, an alkaloid found in Huperzia spp., gingkolides a diterpenoids from Gingko biloba and many ethnobotanicals like Withania somnifera (L...
December 14, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29247294/rcbf-and-cognitive-impairment-changes-assessed-by-spect-and-adas-cog-in-late-onset-alzheimer-s-disease-after-18%C3%A2-months-of-treatment-with-the-cholinesterase-inhibitors-donepezil-or-galantamine
#15
Yukihiko Shirayama, Michio Takahashi, Yasunori Oda, Kouhei Yoshino, Koichi Sato, Toshiyuki Okubo, Masaomi Iyo
Late-onset Alzheimer's disease (AD) differs substantially from early-onset AD. In this cross sectional study we investigated brain perfusion changes after 18 months of treatment with cholinesterase inhibitors (ChEIs) donepezil or galantamine. Twenty-five drug-naïve late-onset AD patients were recruited from outpatient clinics. We examined brain perfusion using single photon emission computed tomography (SPECT) and used three-dimensional stereotactic surface projection (3D-SSP) and the stereotactic extraction estimation method (SEE) level 3 to analyze classified gyrus level segments...
December 15, 2017: Brain Imaging and Behavior
https://www.readbyqxmd.com/read/29243208/plasma-cholinesterase-activity-in-female-green-turtles-chelonia-mydas-nesting-in-laguna-de-terminos-mexico-related-to-organochlorine-pesticides-in-their-eggs
#16
Gerardo Rivas-Hernández, Yaneli May-Uc, Elsa Noreña-Barroso, Víctor Cobos-Gasca, Gabriela Rodríguez-Fuentes
The inhibition of cholinesterase (ChE) activity has been used as a biomarker of exposure to organophosphate and carbamate insecticides. ChE of nesting female green turtles (Chelonia mydas) were biochemically characterized using two substrates, acetylthiocholine iodide and butyrylthiocholine iodide, and three ChE inhibitors (eserine sulfate, BW284C51 and iso-OMPA). The results indicated that BChE is the predominant plasma ChE in female C. mydas, but with atypical properties that differ from those found in human BChE...
December 14, 2017: Bulletin of Environmental Contamination and Toxicology
https://www.readbyqxmd.com/read/29243034/application-of-pyridostigmine-in-pediatric-gastrointestinal-motility-disorders-a-case-series
#17
Mhd Louai Manini, Michael Camilleri, Rayna Grothe, Carlo Di Lorenzo
BACKGROUND: Gastrointestinal (GI) motility disorders are common in children. Treatment is challenging with limited medical and surgical options. Pyridostigmine, an acetyl cholinesterase inhibitor, increases acetylcholine at the neuromuscular junction promoting intestinal contractions. Little is known about the role and dosing of pyridostigmine in pediatric GI motility disorders. METHODS: We present a case series of children with GI dysmotility managed with oral pyridostigmine...
December 14, 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/29231138/cholinesterase-inhibitor-6-chlorotacrine-in-vivo-toxicological-profile-and-behavioural-effects
#18
Jan Misik, Eugenie Nepovimova, Jaroslav Pejchal, Jiri Kassa, Jan Korabecny, Ondrej Soukup
BACKGROUND: 6-chlorotacrine is a cholinesterase inhibitor showing good inhibitory potential, even better than parent compound tacrine, in vitro. Despite tacrine scaffold is broadly used for design and synthesis of novel compounds with anti-Alzheimer's potential, no in vivo effects have been investigated so far. Thus, basic toxicological and behavioural evaluation has been carried out throughout this study. METHODS: Maximum tolerated dose (MTD) and median lethal dose (LD50) were assessed in BALB/c mice and Wistar rats...
December 11, 2017: Current Alzheimer Research
https://www.readbyqxmd.com/read/29222591/dementia-with-lewy-bodies-and-parkinson-s-disease-dementia-current-concepts-and-controversies
#19
REVIEW
Kurt A Jellinger
Dementia with Lewy bodies (DLB) and Parkinson's disease-dementia (PDD), although sharing many clinical, neurochemical and morphological features, according to DSM-5, are two entities of major neurocognitive disorders with Lewy bodies of unknown etiology. Despite considerable clinical overlap, their diagnosis is based on an arbitrary distinction between the time of onset of motor and cognitive symptoms: dementia often preceding parkinsonism in DLB and onset of cognitive impairment after onset of motor symptoms in PDD...
December 8, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29210284/can-persistence-with-cholinesterase-inhibitor-treatment-lower-mortality-and-health-care-costs-among-patients-with-alzheimer-s-disease-a-population-based-study-in-taiwan
#20
Li-Jung Elizabeth Ku, Chung-Yi Li, Yu Sun
Although cholinesterase inhibitors (ChEIs) have been proved to help reduce cognitive deterioration in patients with Alzheimer's disease (AD), their effects on survival remain inconclusive. This study aims to assess the effects of the persistent use of ChEIs on the risk of mortality in patients with AD. This population-based cohort study included 8614 patients having AD with ChEI prescription from 2002 to 2006 and followed until 2010. Kaplan-Meier curves and hazard ratios (HRs) of mortality were estimated in association with ChEI treatment duration and adherence...
January 1, 2017: American Journal of Alzheimer's Disease and Other Dementias
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