Search results for "choline"

showing 10 items of 1138 documents

Two types of receptors for 5-hydroxytryptamine on the cholinergic nerves of the guinea-pig myenteric plexus

1985

Abstract The effects of 5-hydroxytryptamine (5-HT) on spontaneous and electrically-evoked release of [3H]-acetylcholine (ACh) from guinea-pig myenteric plexus preparations preincubated with [3H]-choline have been investigated in the absence of cholinesterase inhibitors. 5-HT caused a transient increase in spontaneous release and an inhibition of the electrically-evoked release of [3H]-ACh. The 5-HT-induced contractions of the longitudinal muscle were clearly related to the increase in spontaneous release. The inhibitory effect was not due to activation of alpha-adrenoceptors since it was also observed in the presence of tolazoline and on strips from reserpine-pretreated guinea-pigs. After d…

MaleSerotoninmedicine.medical_specialtyKetanserinMetoclopramideMethiothepinGuinea PigsMethysergideMyenteric PlexusBiologyTachyphylaxisInhibitory postsynaptic potentialBinding Competitivechemistry.chemical_compoundCocainePiperidinesInternal medicinemedicineAnimalsReceptorNeurotransmitterMyenteric plexusPharmacologyMethysergideAcetylcholineElectric StimulationEndocrinologychemistryReceptors SerotoninAutoreceptorFemaleKetanserinSerotonin AntagonistsResearch ArticleMuscle ContractionTropanesmedicine.drugBritish Journal of Pharmacology
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Histamine and serotonin released from the rat perfused heart by compound 48/80 or by allergen challenge influence noradrenaline or acetylcholine exoc…

1994

Terminal nerve fibres of the autonomic nervous system closely approach mast cells in peripheral organs, and mutual influences between release of neurotransmitters or mast cell mediators may cause neuro-immunological interactions. We have studied the influence of mast cell degranulation on the release of endogenous noradrenaline and newly incorporated acetylcholine (such as 14C-choline/acetylcholine overflow) evoked by stimulation of extrinsic postganglionic sympathetic or preganglionic vagal nerves in the rat Langendorff heart perfused with Tyrode solution. Compound 48/80 perfused in normal hearts, or ovalbumin infused into hearts from rats sensitized to ovalbumin, enhanced the overflow of …

MaleSerotoninmedicine.medical_specialtyLangendorff heartSerotonergicHistamine ReleaseExocytosisNorepinephrinechemistry.chemical_compoundInternal medicinemedicineAnimalsp-Methoxy-N-methylphenethylaminePharmacology (medical)Mast CellsRats WistarNeurotransmitterPharmacologyThioperamideChemistryMyocardiumAllergensCompound 48/80AcetylcholineRatsPerfusionEndocrinologyHistamine H3 receptorAcetylcholineHistaminemedicine.drugFundamental & Clinical Pharmacology
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Adrenoceptor- and cholinoceptor-mediated mechanisms in the regulation of 5-hydroxytryptamine release from isolated tracheae of newborn rabbits

1996

Abstract 1. Isolated tracheae of newborn rabbits were incubated in vitro and the outflow of 5-hydroxytryptamine (5-HT) was determined by h.p.l.c. with electrochemical detection. Evidence has previously been provided that this 5-HT outflow derives from neuroendocrine epithelial (NEE) cells of the airway mucosa. 2. Phenylephrine (1, 10 and 30 microM) enhanced the outflow of 5-HT by 80, 290 and 205%, respectively. 5-HT outflow evoked by 10 microM phenylephrine was not affected by the presence of the neurotoxin tetrodotoxin (1 microM). 3. Rauwolscine, ARC 239 (an alpha(2B)-adrenoceptor preferring antagonist), yohimbine and prazosin antagonized the effect of 10 microM phenylephrine in a concentr…

MaleSerotoninmedicine.medical_specialtyRauwolscineIn Vitro TechniquesMuscarinic Agonistschemistry.chemical_compoundIsoprenalineInternal medicineReceptors Adrenergic betaCyclic AMPmedicinePrazosinAnimalsReceptors CholinergicPhenylephrinePharmacologyForskolinMuscarineHydroxyindoleacetic AcidReceptors AdrenergicYohimbineTracheaEndocrinologyAnimals NewbornchemistryFemaleHexamethoniumRabbitsResearch Articlemedicine.drugBritish Journal of Pharmacology
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Amplifying effect of serotonin on contractile responses in rat aorta and depletion of intracellular Ca-stores

1993

1. Serotonin, 1 microM, induces a contractile response in isolated rat aorta in the presence or absence of extracellular Ca. 2. In Ca-free media, the fast phasic contraction is lower in magnitude and further addition of serotonin evokes no response. 3. Recovery of the contractile response in Ca-free medium is obtained by a 40 min incubation in Ca-containing solution. 4. In Ca, Mg-free medium, the response to serotonin is significantly higher than that obtained in the presence of Mg. 5. An amplifying effect of serotonin on the contractile responses induced by serotonin itself or by noradrenaline was observed in Ca-containing but not in Ca-free solution.

MaleSerotoninmedicine.medical_specialtychemistry.chemical_elementAorta ThoracicIn Vitro TechniquesCalciumBiologyMuscle Smooth VascularNorepinephrine (medication)NorepinephrineInternal medicinemedicine.arterymedicineExtracellularAnimalsMagnesiumRats WistarPharmacologyCalcium metabolismAortaAcetylcholineRatsEndocrinologychemistryCatecholamineCalciumSerotoninmedicine.symptomMuscle Contractionmedicine.drugMuscle contractionGeneral Pharmacology: The Vascular System
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Cisplatin increases the release of 5-hydroxytryptamine (5-HT) from the isolated vascularly perfused small intestine of the guinea-pig: Involvement of…

1991

Isolated segments of the guinea-pig small intestine were vascularly perfused and the release of 5-hydroxytryptamine (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) into the portal venous effluent determined by high pressure liquid chromatography with electrochemical detection. Release of acetylcholine from isolated superfused intestinal segments was determined as outflow of [3H]radioactivity from preparations preincubated with [3H]choline. Cisplatin (3 microM) increased the outflow of 5-HT and 5-HIAA by about 90%. At 30 and 100 microM cisplatin decreased the outflow of 5-HT and its metabolite by 40%-50%. The stimulatory effect of cisplatin was consistently observed only when the bicarbonate-…

MaleSerotoninmedicine.medical_specialtymedicine.drug_classMetaboliteGuinea PigsTetrodotoxinIn Vitro Techniqueschemistry.chemical_compoundInternal medicineIntestine SmallEnterochromaffin CellsmedicineAnimalsReceptor5-HT receptorPharmacologyCisplatinDose-Response Relationship DrugImidazolesGeneral MedicineHydroxyindoleacetic AcidReceptor antagonistOndansetronAcetylcholineSmall intestinePerfusionEndocrinologymedicine.anatomical_structurechemistryReceptors SerotoninFemaleHexamethoniumCisplatinAcetylcholinemedicine.drugNaunyn-Schmiedeberg's Archives of Pharmacology
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The effects of racemic bethanechol and its (R)- and (S)-enantiomers on pre- and postjunctional muscarine receptors in the guinea-pig ileum

1985

The effect of racemic bethanechol and its (R)- and (S)-enantiomers on smooth muscle contraction and outflow of [3H]-acetylcholine were studied in the guinea-pig myenteric plexus-longitudinal muscle preparation that had been preincubated with [3H]-choline. (S)-, racemic, and (R)-bethanechol caused concentration-dependent contractions of the longitudinal muscle. The potency ratio of the strong isomer (S) to the weak one (R) was 915. Racemic and (S)-bethanechol concentration-dependently inhibited the evoked outflow of [3H]-acetylcholine. Racemic bethanechol was more potent than (S)-bethanechol. (R)-bethanechol up to a concentration of 1 mM did no affect the evoked outflow of [3H]-acetylcholine…

MaleStereochemistryGuinea PigsMyenteric PlexusBethanecholchemistry.chemical_compoundBethanechol CompoundsIleumMuscarinic acetylcholine receptormedicineAnimalsPharmacologyMuscarineChemistryMuscle SmoothStereoisomerismGeneral MedicineSmooth muscle contractionBethanecholReceptors MuscarinicRacemic mixtureFemaleCholinesterase InhibitorsEnantiomermedicine.symptomAcetylcholineMuscle Contractionmedicine.drugMuscle contractionNaunyn-Schmiedeberg's Archives of Pharmacology
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Modulation of hippocampal theta oscillations and spatial memory by relaxin-3 neurons of the nucleus incertus.

2009

Hippocampal theta rhythm is thought to underlie learning and memory, and it is well established that “pacemaker” neurons in medial septum (MS) modulate theta activity. Recent studies in the rat demonstrated that brainstem-generated theta rhythm occurs through a multisynaptic pathway via the nucleus incertus (NI), which is the primary source of the neuropeptide relaxin-3 (RLN3). Therefore, this study examined the possible contribution of RLN3 to MS activity, and associated hippocampal theta activity and spatial memory. In anesthetized and conscious rats, we identified the ability of intraseptal RLN3 signaling to modulate neuronal activity in the MS and hippocampus and promote hippocampal the…

MaleStilbamidinesCognitive NeuroscienceMutant Chimeric ProteinsPresynaptic TerminalsHippocampusNeuropeptideBiotinNerve Tissue ProteinsHippocampal formationNeuropsychological TestsHippocampusRats Sprague-DawleyCellular and Molecular NeuroscienceMicroscopy Electron TransmissionMemoryPonsNeural PathwaysPremovement neuronal activityAnimalsInsulinTheta RhythmNeuronsAnalysis of VarianceBehavior AnimalRhodaminesSpectrum AnalysisRelaxinProteinsDextransSpontaneous alternationNucleus IncertusRatsNeuropsychology and Physiological Psychologynervous systemSpace PerceptionExploratory BehaviorCholinergicSeptum of BrainRelaxin-3PsychologyPeptidesNeuroscienceProto-Oncogene Proteins c-fosLearningmemory (Cold Spring Harbor, N.Y.)
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Distribution and targets of the relaxin-3 innervation of the septal area in the rat.

2012

Neural tracing studies have revealed that the rat medial and lateral septum are targeted by ascending projections from the nucleus incertus, a population of tegmental GABA neurons. These neurons express the relaxin-family peptide, relaxin-3, and pharmacological modulation of relaxin-3 receptors in medial septum alters hippocampal theta rhythm and spatial memory. In an effort to better understand the basis of these interactions, we have characterized the distribution of relaxin-3 fibers/terminals in relation to different septal neuron populations identified using established protein markers. Dense relaxin-3 fiber plexuses were observed in regions of medial septum containing hippocampal-proje…

MaleStilbamidinesPopulationHippocampusNerve Tissue ProteinsNitric Oxide Synthase Type IBiologyHippocampal formationCholine O-AcetyltransferaseRats Sprague-DawleyRelaxin-3 like-immunoreactivityMicroscopy Electron TransmissionNeural PathwaysmedicineAnimalseducationNeuronseducation.field_of_studyBrain MappingGlutamate DecarboxylaseGeneral NeuroscienceHippocampal theta rhythmRelaxinSeptal nucleiAnatomyNucleus IncertusCholine acetyltransferaseRatsSeptohippocampal systemmedicine.anatomical_structureParvalbuminsnervous systemStress and emotionSeptum of BrainNeuronNucleus incertusNucleusNeurosciencehormones hormone substitutes and hormone antagonistsThe Journal of comparative neurology
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Distribution of origin of nitric oxide synthase-immunoreactive nerve fibers in the rat epididymis.

1996

Abstract Distribution of neuronal nitric oxide synthase-immunoreactive (nNOS-IR) nerve fibers and somata in the rat epididymis and major pelvic ganglia was studied by immunohistochemical methods. In the epididymis, the supply of nNOS-IR fibers was highest in the cauda and became progressively fewer toward the caput. In the cauda and corpus, nNOS-IR fibers were distributed throughout the subepithelial tissues and around the epithelium. The pattern of distribution of vasoactive intestinal polypeptide (VIP)- and tyrosine hydroxylase (TH)-immunoreactive fibers in the epididymis was similar but the latter was generally more numerous in a given region as compared to that of nNOS-IR fibers. A popu…

MaleStilbamidinesTyrosine 3-MonooxygenaseVasoactive intestinal peptidePopulationBiologyRats Sprague-DawleyNerve FibersDorsal root ganglionGanglia SpinalmedicineAnimalseducationMolecular Biologyreproductive and urinary physiologyFluorescent DyesEpididymisNeuronseducation.field_of_studyNeurotransmitter AgentsHypogastric PlexusGeneral NeuroscienceVas deferensSmooth muscle contractionAnatomyEpididymisCholine acetyltransferaseImmunohistochemistryEpitheliumRatsbody regionsmedicine.anatomical_structurePhenotypenervous systemNeurology (clinical)Nitric Oxide SynthaseDevelopmental BiologyVasoactive Intestinal PeptideBrain research
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Controlled Iontophoretic Delivery in Vitro and in Vivo of ARN14140—A Multitarget Compound for Alzheimer’s Disease

2019

ARN14140 is a galantamine-memantine conjugate that acts upon both cholinergic and glutamatergic pathways for better management of Alzheimer's disease. Poor oral bioavailability and pharmacokinetics meant that earlier preclinical in vivo studies employed intracerebroventricular injection to administer ARN14140 directly to the brain. The aim of the present study was to evaluate the feasibility of using constant current transdermal iontophoresis for the noninvasive systemic delivery of ARN14140 and to quantify the amounts present in the blood and the brain. Preliminary experiments in vitro were performed using porcine skin and validated with human skin. Cumulative ARN14140 permeation across th…

MaleSwineSkin Absorptionbrain deliveryBiological AvailabilityPharmaceutical ScienceHuman skin02 engineering and technologyPharmacologyAdministration Cutaneous030226 pharmacology & pharmacyPermeability03 medical and health sciences0302 clinical medicineDrug StabilityPharmacokineticsIn vivoDrug DiscoveryARN14140AnimalsBrain/metabolismHumansSkin/metabolismMedicineTissue DistributionRats WistarNootropic Agents/administration & dosage/pharmacokineticsTransdermalddc:615galantamine-memantine conjugateAlzheimer Disease/drug therapyIontophoresisbusiness.industryGalantamine/administration & dosage/pharmacokineticsiontophoresiIontophoresisMemantine/administration & dosage/pharmacokinetics021001 nanoscience & nanotechnologyIn vitroRatsBioavailabilityHeterocyclic Compounds 4 or More Rings/administration & dosage/pharmacologytransdermalFeasibility StudiesMolecular MedicineCholinergic0210 nano-technologybusinessMolecular Pharmaceutics
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