Search results for "cholinesterase inhibitor"

Inhibitory and excitatory muscarinic receptors modulating the release of acetylcholine from the postganglionic parasympathetic neuron of the chicken …

1992

The effects of muscarinic receptor antagonists on ACh release were studied in the absence or presence of cholinesterase (ChE) inhibition using the isolated perfused chicken heart. Presynaptic inhibitory muscarinic autoreceptor were characterized by determining the potency of various antagonists to enhance [3H]-ACh release evoked by field stimulation (3 Hz, 1 min). The order of potencies was: (±)-telenzepine > atropine > 4-DAMP > silahexocyclium > pirenzepine > hexahydro-siladifenidol > AF-DX 116. The comparison with known pA2 values for M1-, M2- and M3-receptors revealed that the presynaptic autoreceptor meets the criteria of an M1-receptor. Basal, not electrically evoked overflow of unlabe…

Amyloid precursor protein in platelets of patients with Alzheimer disease: effect of acetylcholinesterase inhibitor treatment.

2001

BACKGROUND:Amyloid precursor protein (APP) forms with apparent molecular weights of 130, 110, and 106 kd are present in human platelets. It has been demonstrated that Alzheimer disease (AD) is specifically associated with a decreased APP forms ratio in platelets. OBJECTIVE:To investigate whether acetylcholinesterase (AChE) inhibitor treatment modifies the ratio of platelet APP forms in patients with AD. PATIENTS AND METHODS:From a large sample of patients with probable AD, 30 with mild to moderate AD were selected. Each patient underwent a clinical evaluation including the Mini-Mental State Examination (MMSE) and platelet APP forms analysis at baseline and after 30 days. During this interva…

Release of non-neuronal acetylcholine from the human placenta: difference to neuronal acetylcholine

2001

The synthesis and release of non-neuronal acetylcholine, a widely expressed signaling molecule, were investigated in the human placenta. This tissue is free of cholinergic neurons, i.e. a contamination of neuronal acetylcholine can be excluded. The villus showed a choline acetyltransferase (ChAT) activity of 0.65 nmol/mg protein per h and contained 500 nmol acetylcholine/g dry weight. In the absence of cholinesterase inhibitors the release of acetylcholine from isolated villus pieces amounted to 1.3 nmol/g wet weight per 10 min corresponding to a fractional release rate of 0.13% per min. The following substances did not significantly modify the release of acetylcholine: oxotremorine (1 micr…

Alterations on AChE Activity of the Fish Anguilla anguilla as Response to Herbicide-Contaminated Water

2000

Abstract The inhibition of both total and specific acetylcholinesterase activities was measured in the whole eyes of the yellow eel Anguilla anguilla after exposure to the carbamate thiobencarb. In vivo assays were conducted under a constant flow-through system of thiobencarb-contaminated water (1/60 LC50 96 h=0.22 ppm for 96 h) followed by a recovery period in clean water (192 h more). The results indicated a measurable level of AChE activity on eyes of control eels, which resulted in a sensitive indicator of the presence of thiobencarb in the water. The pesticide induced significant inhibitory effects on AChE activity ranging from 35% in total AChE activity to 75% in specific AChE activit…

Cholinesterase Activity and Hematological Parameters as Biomarkers of Sublethal Molinate Exposure in Anguilla anguilla

2000

Cholinesterase (ChE) activity was measured in plasma, whole blood [using 5,5'-dithiobis(2-nitrobenzoic acid) and 2-PDS as chromophores], brain, and whole eyes of Anguilla anguilla exposed to a sublethal concentration of 11.15 mg/L (one-third of the 96-h LC(50)) of the carbamate herbicide molinate. ChE activity was evaluated after 6, 24, 48, 72, and 96 h of pesticide exposure. Results indicated that ChE activity in eel tissues decreased as time of exposure increased, especially in eel blood. Eels exposed to molinate were transferred to a pesticide-free water for a recovery period of 4 days and ChE activity was also evaluated. Results indicated that ChE activity for those animals with preexpo…

Methodological matters on an Alzheimer's dementia trial: is a double-blind randomized controlled study design sufficient to draw strong conclusions o…

2007

Use of atropine-treated Daphnia magna survival for detection of environmental contamination by acetylcholinesterase inhibitors.

2003

The toxicity of cholinesterase-inhibiting compounds (e.g., carbamates and organophosphates) is due to a decrease in acetylcholine metabolism, which results in a continuous stimulation of cholinergic receptors (muscarinic and nicotinic) that can be fatal. The goal of this study was to evaluate the protective effect of atropine (muscarinic receptor antagonist) against paraoxon-induced toxicity to Daphnia magna using its survival rate for the detection of environmental contamination by cholinesterase-inhibiting compounds. As expected, paraoxon was lethal to D. magna in a concentration-dependent manner. Noteworthy, the pretreatment of these organisms with atropine dramatically increased their s…

Toxicity of Dimethoate to Some Soil Animal Species in Different Soil Types

1996

Toxicity of dimethoate (insecticide) to an earthworm (Aporrectodea caliginosa tuberculata), a collembola (Folsomia candida), and an enchytraeid worm (Enchytraeus crypticus/variatus) was studied in three different soil types (artificial soil, clayey soil, and humus sandy soil). Parameters measured were survival and biomass change of the earthworms and survival and reproduction of the collembolas and enchytraeids. The degradation of dimethoate was analyzed too. Toxic effects were observed at the concentrations of some mg/kg dry soil. The biomass reduction of the earthworms occurred at lower concentrations than reduction in survival. The collembolas were more susceptible to dimethoate than the…

Cardiovascular Outcomes of Cholinesterase Inhibitors in Individuals with Dementia: A Meta-Analysis and Systematic Review

2018

Objectives: To evaluate the cardiovascular (CV) effects of acetylcholinesterase inhibitors (AChEIs) in individuals with dementia. Design: Systematic review and meta-analysis. Setting: Two authors independently searched major electronic databases from inception until June 17, 2017, for longitudinal (without a control group) and cohort (with a control group) studies reporting CV outcomes in relation to AChEIs. Randomized controlled trials were excluded because they included relatively healthy subjects. Participants: Individuals with dementia and controls. Measurements: Changes in CV parameters were summarized using standardized mean differences (SMDs) with 95% confidence intervals (CIs). Even…

Evaluation of Galantamine transbuccal absorption by reconstituted human oral epithelium and porcine tissue as buccal mucosa models: Part I

2008

Over the last decade, interest in delivering drugs through buccal mucosa has increased. As a major limitation in buccal drug delivery could be the low permeability of the epithelium, the aim of this study was to evaluate the aptitude of galantamine, useful in Alzheimer's disease, to penetrate the buccal mucosa. The evaluation of the ability of galantamine to permeate through the buccal epithelium was investigated using two permeation models. Firstly, in vitro permeation experiments were carried out using reconstituted human oral non-keratinised epithelium and Transwell diffusion cells system. Results were validated by ex vivo experiments using porcine buccal mucosa as membrane and Franz typ…