Search results for "Cholines"

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…

A biochemical study of the effects of tributyltin on unfertilized eggs, embryos and larvae of the sea squirt Ciona intestinalis

2009

We have used unfertilized eggs, embryos and larvae of the sea squirt Ciona intestinalis (Ascidiacea, Urochordata) to study the effects of tributyltin (TBT) on acetylcholine esterase (AChE) activity. Our results showed an increase of AChE enzyme activity levels after TBT exposure in both unfertilized eggs and embryos. The effects of TBT were more pronounced during the gastrula stage, while no differences between exposed larvae and controls were observed. A mechanism of TBT action on enzyme activity during ascidian embryonic development and the possibility of employing AChE in C. intestinalis as a biomarker of TBT exposure are suggested and discussed.

BODIPY dyes functionalized with 2-(2-dimethylaminophenyl)ethanol moieties as selective OFF–ON fluorescent chemodosimeters for the nerve agent mimics …

2014

[EN] Two OFF-ON fluorescent chemodosimeters based on a BODIPY core for the detection of nerve agent mimics have been synthesized. Their reactivity towards diethylcyanophosphonate (DCNP) and diisopropylfluorophosphate (DFP) has been tested in organic and aqueous phase. These chemodosimeters selectively detect the nerve agent mimics with good LODs. The chemodosimeters hold their sensing properties on solid supports, allowing the preparation of a hand held sensing kit. The sensing in solid-liquid phase has been demonstrated. The X-ray structure of compound 2 has been resolved.

Chapter 17: The cholinesterases: a discussion of some unanswered questions

1993

Publisher Summary During the past three decades, a vast body of specificity and kinetic data relating to the cholinesterases has accumulated, which must now be explained by the extremely interesting new sequence and X-ray crystallographic results presented by MassouliC et al. As this chapter shows, the cholinesterases are remarkable among enzymes in having a broad specificity embracing both charged and uncharged substrates but with a clearly expressed preference, at any rate in the aliphatic series, for the acylcholine configuration: a classical example of the principle of complementariness between substrate and active site as the basis for enzyme action. It is well known that AChE exists i…

Choline is a Selective Agonist of α7 Nicotinic Acetylcholine Receptors in the Rat Brain Neurons

1998

In the present study, we demonstrate that choline, a precursor of acetylcholine (ACh) and a product of acetylcholine hydrolysis by acetylcholinesterase (AChE), acts as an efficient and relatively selective agonist of alpha7-containing nicotinic acetylcholine receptors (nAChR) in neurons cultured from the rat hippocampus, olfactory bulb and thalamus as well as in PC12 cells. Choline was able to activate postsynaptic and presynaptic alpha7 nAChRs, with the latter action resulting in the release of other neurotransmitters. Although choline was approximately one order of magnitude less potent than ACh (EC50 of 1.6 mM for choline and 0.13 mM for ACh), it acted as a full agonist at alpha7 nAChRs.…

Elimination of Parathion by Hemoperfusion in Severe E 605 ForteR Intoxication in Vivo

1978

Severe parathion (P) intoxication results in complete inhibition of cholinesterase activity and toxic accumulation of acetylcholine. Besides these well known biochemical changes, there is evidence of direct toxic effects on the cardio-vascular system which may prove fatal due to an excess of P.

Coiled-Coil Lipopeptides Mimicking the Prehairpin Intermediate of Glycoprotein gp41

2009

Tin compounds interaction with membranes of egg lecithin liposomes.

2007

This work is a continuation of earlier research concerning the influence of tin compounds on the dynamic properties of liposome membranes produced with lecithin hen egg yolks (EYL). The experiments were carried out at room temperature (about 25 ∞C). Four tin compounds were chosen, including three organic ones, (CH3)4Sn, (C2H5)4Sn and (C3H7)3SnCl, and one inorganic, SnCl2. The investigated compounds were admixed to water dispersions of liposomes. The content of the admixture changed within the range 0 mol-% to 11mol-% in proportion to EYL. Two spin probes were used in the experiment: 2,2,6,6-tetramethylpiperidine- 1-oxyl (TEMPO) and 2-ethyl-2-(15-methoxy-15-oxopentadecyl)-4,4-dimethyl-3-oxaz…

Efficient, non-toxic anion transport by synthetic carriers in cells and epithelia.

2016

Transmembrane anion transporters (anionophores) have potential for new modes of biological activity, including therapeutic applications. In particular they might replace the activity of defective anion channels in conditions such as cystic fibrosis. However, data on the biological effects of anionophores are scarce, and it remains uncertain whether such molecules are fundamentally toxic. Here, we report a biological study of an extensive series of powerful anion carriers. Fifteen anionophores were assayed in single cells by monitoring anion transport in real time through fluorescence emission from halide-sensitive yellow fluorescent protein. A bis-(p-nitrophenyl)ureidodecalin shows especial…

Drug‐refractory myasthenia gravis: Clinical characteristics, treatments, and outcome

2022

[Objective] To describe the clinical characteristics and outcomes in patients with refractory myasthenia gravis (MG) and to determine the effectiveness and side effects of the drugs used for their treatment.