Search results for "choline"

showing 10 items of 1138 documents

pH-dependent hydrolysis of acetylcholine: Consequences for non-neuronal acetylcholine

2015

Acetylcholine is inactivated by acetylcholinesterase and butyrylcholinesterase and thereby its cellular signalling is stopped. One distinguishing difference between the neuronal and non-neuronal cholinergic system is the high expression level of the esterase activity within the former and a considerably lower level within the latter system. Thus, any situation which limits the activity of both esterases will affect the non-neuronal cholinergic system to a much greater extent than the neuronal one. Both esterases are pH-dependent with an optimum at pH above 7, whereas at pH values below 6 particularly the specific acetylcholinesterase is more or less inactive. Thus, acetylcholine is prevente…

Pharmacologymedicine.medical_specialtyHydrolysisImmunologyMetabolic acidosisHydrogen-Ion Concentrationmedicine.diseaseAcetylcholinesteraseEsteraseAcetylcholinechemistry.chemical_compoundEndocrinologychemistryButyrylcholinesteraseInternal medicineAcetylcholinesterasemedicineExtracellularHumansImmunology and AllergyCholinergicAcetylcholineButyrylcholinesterasemedicine.drugCalcium signalingInternational Immunopharmacology
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The Non-neuronal Cholinergic System

2001

Acetylcholine, one of the most exemplary neurotransmitters, has been detected in bacteria, algae, protozoa, tubellariae and primitive plants, suggesting an extremely early appearance in the evolutionary process and a wide expression in non-neuronal cells. In plants (Urtica dioica), acetylcholine is involved in the regulation of water resorption and photosynthesis. In humans, acetylcholine and/or the synthesizing enzyme, choline acetyltransferase, have been demonstrated in epithelial (airways, alimentary tract, urogenital tract, epidermis), mesothelial (pleura, pericardium), endothelial, muscle and immune cells (granulocytes, lymphocytes, macrophages, mast cells). The widespread expression o…

Pharmacologymedicine.medical_specialtyInflammationBiologyCholine acetyltransferaseCell biologyNicotinic agonistEndocrinologyInternal medicineMuscarinic acetylcholine receptormedicinebiology.proteinSignal transductionmedicine.symptomReceptorAcetylcholinemedicine.drugCholinesteraseJapanese Journal of Pharmacology
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In vivo release of non-neuronal acetylcholine from the human skin as measured by dermal microdialysis: effect of botulinum toxin

2006

1.--Acetylcholine is synthesized in the majority of non-neuronal cells, for example in human skin. In the present experiments, the in vivo release of acetylcholine was measured by dermal microdialysis. 2.--Two microdialysis membranes were inserted intradermally at the medial shank of volunteers. Physiological saline containing 1 muM neostigmine was perfused at a constant rate of 4 microl min(-1) and the effluent was collected in six subsequent 20 min periods. Acetylcholine was measured by high-pressure liquid chromatography (HPLC) combined with bioreactors and electrochemical detection. 3.--Analysis of the effluent by HPLC showed an acetylcholine peak that disappeared, when the analytical c…

Pharmacologymedicine.medical_specialtyMicrodialysisChemistryHuman skinPharmacologyNeostigminechemistry.chemical_compoundEndocrinologyIn vivoInternal medicinemedicineLiberationCarnitineNeurotransmitterAcetylcholinemedicine.drugBritish Journal of Pharmacology
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Formation of N-methylnicotinamide in the brain from a dihydropyridine-type prodrug

1999

The enhancement of brain choline levels is a possible therapeutic option in neurodegenerative diseases; however, brain choline levels are held within narrow limits by homeostatic mechanisms including the rapid clearance of excess choline from the brain. The present study tests whether N-methylnicotinamide (NMN), an inhibitor of the outward transport of choline from the brain, can elevate brain choline levels in vivo. As NMN does not cross the blood-brain barrier, we synthesized and administered the brain-permeable prodrug, 1,4-dihydro-N-methyl-nicotinamide (DNMN), and tested its effect on the levels of NMN and choline in brain extracellular fluid, using the microdialysis procedure. Administ…

Pharmacologymedicine.medical_specialtyMicrodialysisProdrugBlood–brain barrierBiochemistrychemistry.chemical_compoundmedicine.anatomical_structureCerebrospinal fluidEndocrinologychemistryBiochemistryInternal medicineExtracellular fluidBlood plasmamedicineExtracellularCholineBiochemical Pharmacology
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Non-neuronal acetylcholine, a locally acting molecule, widely distributed in biological systems: expression and function in humans.

1998

Acetylcholine acts as a neurotransmitter in the central and peripheral nervous systems in humans. However, recent experiments demonstrate a widespread expression of the cholinergic system in non-neuronal cells in humans. The synthesizing enzyme choline acetyltransferase, the signalling molecule acetylcholine, and the respective receptors (nicotinic or muscarinic) are expressed in epithelial cells (human airways, alimentary tract, epidermis). Acetylcholine is also found in mesothelial, endothelial, glial, and circulating blood cells (platelets, mononuclear cells), as well as in alveolar macrophages. The existence of non-neuronal acetylcholine explains the widespread expression of muscarinic …

Pharmacologymedicine.medical_specialtyMuscarinic acetylcholine receptor M3Muscarinic acetylcholine receptor M2BiologyAcetylcholineCell biologyCholine O-AcetyltransferaseCircadian RhythmEndocrinologyNicotinic agonistInternal medicineMuscarinic acetylcholine receptor M5Muscarinic acetylcholine receptormedicineMuscarinic acetylcholine receptor M4CholinergicHumansPharmacology (medical)Acetylcholinemedicine.drugPharmacologytherapeutics
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Globularia alypumL. extracts reduced histamine and serotonin contractionin vitro

2002

The present study analyses in in vitro models the pharmacological activity of methanol and dichloromethane extracts (1, 10 and 100 microg/mL) obtained from the leaves and stems of Globularia alypum L. Preincubation of the guinea-pig ileum and rat uterus with both extracts produced a dose dependent abolition of the contractile effects of histamine and serotonin, respectively. At the same doses, neither methanol nor dichloromethane extract reduced the contractile effects of acetylcholine on rat duodenum or noradrenaline on rat vas deferens.

Pharmacologymedicine.medical_specialtyVas deferensIleumBiological activityBiologyPharmacognosychemistry.chemical_compoundmedicine.anatomical_structureEndocrinologychemistryInternal medicinemedicineSerotoninSerotonin AntagonistsHistamineAcetylcholinemedicine.drugPhytotherapy Research
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Release of non-neuronal acetylcholine from the isolated human placenta is mediated by organic cation transporters

2001

1. The release of acetylcholine was investigated in the human placenta villus, a useful model for the characterization of the non-neuronal cholinergic system. 2. Quinine, an inhibitor of organic cation transporters (OCT), reduced acetylcholine release in a reversible and concentration-dependent manner with an IC(50) value of 5 microM. The maximal effect, inhibition by 99%, occurred at a concentration of 300 microM. 3. Procaine (100 microM), a sodium channel blocker, and vesamicol (10 microM), an inhibitor of the vesicular acetylcholine transporter, were ineffective. 4. Corticosterone, an inhibitor of OCT subtype 1, 2 and 3 reduced acetylcholine in a concentration-dependent manner with an IC…

Pharmacologymedicine.medical_specialtyVesamicolOrganic cation transport proteinsbiologyAmiloridechemistry.chemical_compoundProcaineEndocrinologychemistryMechanism of actionVesicular acetylcholine transporterInternal medicinemedicinebiology.proteinVerapamilmedicine.symptomAcetylcholinemedicine.drugBritish Journal of Pharmacology
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Modulation of acetylcholine release in the guinea-pig trachea by the nitric oxide donor, S-nitroso-N-acetyl-DL-penicillamine (SNAP)

2000

The effects of the nitric oxide (NO) donor S-nitroso-N-acetyl-DL-penicillamine (SNAP) and the NO synthase inhibitor L-N(G)-nitroarginine (L-NOARG) on the electrically evoked [(3)H]-acetylcholine release were studied in an epithelium-free preparation of guinea-pig trachea that had been preincubated with [(3)H]-choline. SNAP (100 and 300 microM) caused small but significant increases of the electrically evoked [(3)H]-acetylcholine release (121+/-4% and 124+/-10% of control). Resting outflow of [(3)H]-ACh was not affected by SNAP. The increase by SNAP was abolished by the specific inhibitor of soluble guanylyl cyclase, 1H-[1,2,4]oxadiazolo[4,3-alpha]quinoxalin-1-one (ODQ, 1 microM). The facili…

Pharmacologymedicine.medical_specialtybiologySnapNitric oxideNitric oxide synthasechemistry.chemical_compoundNitroarginineEndocrinologychemistryEnzyme inhibitorCapsaicinInternal medicinemedicinebiology.proteinSoluble guanylyl cyclaseAcetylcholinemedicine.drugBritish Journal of Pharmacology
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Hydrolytic action of phospholipase A2 in monolayers in the phase transition region: direct observation of enzyme domain formation using fluorescence …

1990

Phospholipase A2, a ubiquitous lipolytic enzyme highly active in the hydrolysis of organized phospholipid substrates, has been characterized optically in its action against a variety of phospholipid monolayers using fluorescence microscopy. By labeling the enzyme with a fluorescent marker and introducing it into the subphase of a Langmuir film balance, the hydrolysis of lipid monolayers in their liquid-solid phase transition region could be directly observed with the assistance of an epifluorescence microscope. Visual observation of hydrolysis of different phospholipid monolayers in the phase transition region in real-time could differentiate various mechanisms of hydrolytic action against …

Phase transition12-DipalmitoylphosphatidylcholineStereochemistryBiophysicsPhospholipidBiochemistryPhospholipases Achemistry.chemical_compoundPhospholipase A2Phase (matter)MonolayerEnzyme StabilityFluorescence microscopeLipid bilayer phase behaviorParticle SizePhospholipidsFluorescent DyesElapid VenomsPhospholipase ABinding SitesbiologyHydrolysisPhosphatidylethanolaminesCell BiologyImage EnhancementPhospholipases A2chemistryMicroscopy FluorescencePhospholipasesBiophysicsbiology.proteinlipids (amino acids peptides and proteins)DimyristoylphosphatidylcholineBiochimica et biophysica acta
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Phase Transition of Individually Addressable Microstructured Membranes Visualized by Imaging Ellipsometry

2007

The phase transition of individually addressable microstructured lipid bilayers was investigated by means of imaging ellipsometry. Microstructured bilayers were created on silicon substrates by micromolding in capillaries, and the thermotropic behavior of various saturated diacyl phosphatidylcholine (1,2-dipalmitoyl-sn-glycero-3-phosphocholine, 1,2-dipentadecoyl-sn-glycero-3-phosphocholine, and 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC)) bilayers as well as DMPC/cholesterol membranes was determined by measuring the area expansion and thickness of the bilayer as a function of temperature. We found an increase in the main phase transition temperature T(M) of 2-6 degrees C and a substa…

Phase transitionMaterials scienceBilayerVesicleLipid BilayersTemperatureAnalytical chemistryMicroscopy Atomic ForceThermotropic crystalPhase TransitionSurfaces Coatings and FilmsDiffusionchemistry.chemical_compoundMembranechemistryEllipsometryPhosphatidylcholineMaterials ChemistryPhysical and Theoretical ChemistryLipid bilayerThe Journal of Physical Chemistry B
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