Search results for " M1"

showing 9 items of 49 documents

Facilitatory and inhibitory muscarine receptors on the rat phrenic nerve: effects of pirenzepine and dicyclomine

1988

Neuronal transmitter stores of the rat phrenic nerve were labelled by an incubation with [3H]choline. Release of [3H]acetylcholine was elicited either by a short (100 pulses, 5 Hz) or by a long (1500 pulses, 5 or 25 Hz) period of electrical nerve stimulation. Pirenzepine and dicyclomine enhanced transmitter release evoked by the short stimulation period. Both antagonists reduced transmitter release evoked by the long stimulation period. Pirenzepine reduced transmitter release at low concentrations (1 nmol/l) whereas a higher concentration was necessary for the enhancing effect; the opposite pattern was found for dicyclomine. A low concentration of oxotremorine (10 nmol/l) enhanced and a hig…

medicine.medical_specialtyCyclohexanecarboxylic AcidsNeuromuscular JunctionDicyclomineStimulationIn Vitro TechniquesSynaptic TransmissionDicyclominechemistry.chemical_compoundInternal medicineMuscarinic acetylcholine receptormedicineAnimalsEvoked PotentialsPharmacologyMuscarineChemistryRats Inbred StrainsMuscarinic acetylcholine receptor M2PirenzepineGeneral MedicineMuscarinic acetylcholine receptor M1Receptors MuscarinicPirenzepineAcetylcholineRatsPhrenic NerveEndocrinologyAcetylcholinemedicine.drugNaunyn-Schmiedeberg's Archives of Pharmacology
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Role of the M3 Muscarinic Acetylcholine Receptor Subtype in Murine Ophthalmic Arteries After Endothelial Removal

2014

We tested the hypothesis that the M3 muscarinic acetylcholine receptor subtype mediates cholinergic responses in murine ophthalmic arteries after endothelial removal.Muscarinic receptor gene expression was determined in ophthalmic arteries with intact and with removed endothelium using real-time PCR. To examine the role of the M3 receptor in mediating vascular responses, ophthalmic arteries from M3 receptor-deficient mice (M3R(-/-)) and respective wild-type controls were studied in vitro. Functional studies were performed in nonpreconstricted arteries with either intact or removed endothelium using video microscopy.In endothelium-intact ophthalmic arteries, mRNA for all five muscarinic rece…

medicine.medical_specialtyEndotheliumReal-Time Polymerase Chain ReactionMiceOphthalmic ArteryRetinal DiseasesInternal medicineMuscarinic acetylcholine receptormedicineMuscarinic acetylcholine receptor M4AnimalsRNA MessengerMice KnockoutReceptor Muscarinic M3business.industryMuscarinic acetylcholine receptor M3Muscarinic acetylcholine receptor M2Muscarinic acetylcholine receptor M1ArticlesDisease Models AnimalEndocrinologymedicine.anatomical_structureGene Expression RegulationVasoconstrictioncardiovascular systemCholinergicEndothelium VascularbusinessAcetylcholinemedicine.drug
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Functional relevance of presynaptic muscarinic autoreceptors.

1993

Pre- and postsynaptic muscarinic receptors have been characterized in the isolated trachea and ileal circular muscle of the guinea pig. The muscarinic autoreceptors mediating inhibition of acetylcholine release in the circular muscle belong to the M1 subtype, whereas those inhibiting acetylcholine release in the trachea are M2 or M4 receptors. In both tissues the postsynaptic muscarinic receptors are M3 receptors. Blockade of the autoreceptors by selective M1 and M2/M4 receptor antagonists leads to facilitation of cholinergic neurotransmission.

medicine.medical_specialtyGeneral NeuroscienceGuinea PigsPresynaptic TerminalsMuscarinic acetylcholine receptor M3Muscarinic acetylcholine receptor M2Muscle SmoothMuscarinic acetylcholine receptor M1PharmacologyBiologyIn Vitro TechniquesReceptors MuscarinicTracheaEndocrinologyPostsynaptic potentialIleumPhysiology (medical)Internal medicineMuscarinic acetylcholine receptorMuscarinic acetylcholine receptor M5medicineMuscarinic acetylcholine receptor M4AnimalsAcetylcholinemedicine.drugJournal of physiology, Paris
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Acetylcholine mediates the release of IL-8 in human bronchial epithelial cells by a NFkB/ERK-dependent mechanism

2007

Acetylcholine may play a role in cell activation and airway inflammation. We evaluated the levels of both mRNA and protein of muscarinic M(1), M(2), M(3) receptors in human bronchial epithelial cell line (16HBE). 16HBE cells were also stimulated with acetylcholine and extracellular signal-regulated kinase1/2 (ERK1/2) and NFkB pathway activation as well as the IL-8 release was assessed in the presence or absence of the inhibitor of Protein-kinase (PKC) (GF109203X), of the inhibitor of mitogenic activated protein-kinase kinase (MAPKK) (PDO9805), of the inhibitor of kinaseB-alpha phosphorilation (pIkBalpha) (BAY11-7082), and of muscarinic receptor antagonists tiotropium bromide, 4-Diphenylacet…

medicine.medical_specialtyIndolesNeutrophilsScopolamine DerivativesBronchiMuscarinic AntagonistsBiologyPharmacologyMaleimideschemistry.chemical_compoundPiperidinesInternal medicineNitrilesMuscarinic acetylcholine receptor M5Muscarinic acetylcholine receptormedicineHumansRNA MessengerSulfonesTiotropium BromideProtein Kinase CCell Line TransformedAcetylcholine receptorFlavonoidsMitogen-Activated Protein Kinase 1PharmacologyMitogen-Activated Protein Kinase 3Gallamine TriethiodideInterleukin-8NF-kappa BMuscarinic acetylcholine receptor M3Epithelial CellsMuscarinic acetylcholine receptor M2PirenzepineMuscarinic acetylcholine receptor M1Receptors MuscarinicAcetylcholineChemotaxis LeukocyteEndocrinologychemistryTelenzepineAcetylcholinemedicine.drugEuropean Journal of Pharmacology
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Control of Acetylcholine Release and of Intestinal Motility by Subtypes of Muscarine Receptors

1988

Two types of neuronal muscarine receptors have been investigated in the myenteric plexus preparation of the guinea-pig small intestine: 1. Presynaptic receptors activation of which inhibits the depolarization-evoked release of acetylcholine. Pirenzepine and dicyclomine have low affinities to the release-inhibitory receptors (pA2 values 6.9 and 7.6) which suggests that the presynaptic receptors (similar to the smooth muscle receptors) belong to the M2 subtype. The inhibition of the electrically-evoked acetylcholine release by muscarine (0.01 - 1 μmol/1) was not affected by forskolin (1μmol/l). This indicates that cyclic AMP is not crucially involved in the muscarinic inhibition of acetylchol…

medicine.medical_specialtyMuscarineChemistryMuscarinic acetylcholine receptor M1BicucullineDicyclominePirenzepinechemistry.chemical_compoundEndocrinologyInternal medicineMuscarinic acetylcholine receptormedicineReceptorAcetylcholinemedicine.drug
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The role of vagus activity in the presynaptic control of noradrenaline release from rabbit atria.

1990

Abstract On various heart preparations with the autonomic innervation left intact, vagus nerve stimulation (VNS) has been found to reduce the amount of noradrenaline (NA) that is released in response to sympathetic nerve stimulation (SNS). The following experiments were carried out on an innervated rabbit perfused atria preparation in which the overflow of NA and acetylcholine (ACh) could be determined simultaneously. VNS impulses applied at a fixed time interval before the corresponding SNS impulses reduced NA overflow when the interval was 3–10 ms (early peak) or 200–283 ms (late peak of inhibition). VNS applied 30–167 ms before SNS had no significant effect (“ineffectual period”). Both i…

medicine.medical_specialtyMuscarineMuscarinic acetylcholine receptor M2Cell BiologyMuscarinic acetylcholine receptor M1PirenzepineVagus nerveCellular and Molecular Neurosciencechemistry.chemical_compoundEndocrinologychemistryInternal medicineMuscarinic acetylcholine receptormedicineAutoreceptorAcetylcholinemedicine.drugNeurochemistry international
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The interferance of muscarinic receptors with the noradrenaline release from sympathetic nerve endings caused by nicotinic agents.

1968

medicine.medical_specialtySympathetic nervous systemSympathetic Nervous SystemReceptors DrugIn Vitro TechniquesPiperazinesNorepinephrineInternal medicineMuscarinic acetylcholine receptorMuscarinic acetylcholine receptor M4medicineAnimalsSympathomimeticsPharmacologyNerve EndingsChemistryMyocardiumMuscarinic acetylcholine receptor M3Muscarinic acetylcholine receptor M2General MedicineMuscarinic acetylcholine receptor M1AcetylcholinePerfusionEndocrinologymedicine.anatomical_structureRabbitsFree nerve endingAcetylcholinemedicine.drugNaunyn-Schmiedebergs Archiv fur experimentelle Pathologie und Pharmakologie
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Proliferative effect of acetylcholine on rat trachea epithelial cells is mediated by nicotinic receptors and muscarinic receptors of the M1-subtype.

2003

Acetylcholine (ACh), synthesized in mammalian non-neuronal cells such as epithelial cells of the airways, digestive tract and skin, is involved in the regulation of basic cell functions (so-called non-neuronal cholinergic system). In the present experiments rat trachea epithelial cells have been cultured to study the proliferative effect of applied ACh by [3H]thymidine incorporation. ACh (exposure time 24 h) caused a concentration-dependent increase in cell proliferation with a doubling of the [3H]thymidine incorporation at a concentration of 0.1 microM. This effect was partly reduced by 30 microM tubocurarine and completely abolished by the additional application of 1 microM atropine. The …

medicine.medical_specialtyTubocurarineMuscarinic AntagonistsNicotinic AntagonistsBiologyReceptors NicotinicGeneral Biochemistry Genetics and Molecular BiologyRats Sprague-DawleyInternal medicineMuscarinic acetylcholine receptormedicineMuscarinic acetylcholine receptor M4AnimalsGeneral Pharmacology Toxicology and PharmaceuticsNicotinic AntagonistReceptor Muscarinic M1Muscarinic acetylcholine receptor M3Muscarinic acetylcholine receptor M2Epithelial CellsGeneral MedicineMolecular biologyPirenzepineReceptors MuscarinicAcetylcholineRatsTracheaAtropineEndocrinologyAcetylcholineCell Divisionmedicine.drugThymidineLife sciences
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Effects of indomethacin on muscarinic inhibition of endogenous noradrenaline release from rat isolated trachea

1993

The release of endogenous noradrenaline from rat isolated tracheae was evoked by electrical field stimulation (3 Hz, 540 pulses) in the presence of yohimbine, desipramine and tyrosine. The muscarine receptor agonist oxotremorine concentration-dependently inhibited the evoked release of noradrenaline by 95% at 1 μmol/l, EC50 values in two series of experiments 41 and 57 nmol/l, respectively. The effect of oxotremorine was antagonized by the non-selective muscarine receptor antagonist scopolamine (10–1000 nmol/l) in a manner suggesting a simple competitive interaction (slope of Schild plot −0.94; pA2 value 8.88). However, the M2 selective muscarine receptor antagonist methoctramine (0.1–10 μm…

medicine.medical_specialtymedicine.drug_classIndomethacinDiaminesIn Vitro TechniquesRats Sprague-DawleyNorepinephrinechemistry.chemical_compoundInternal medicineMuscarinic acetylcholine receptormedicineOxotremorineMethoctramineAnimalsPharmacologyMuscarineOxotremorineGeneral MedicineMuscarinic acetylcholine receptor M1Receptor antagonistReceptors MuscarinicPirenzepineRatsTracheaSchild regressionEndocrinologychemistryProstaglandinsFemalemedicine.drugNaunyn-Schmiedeberg's Archives of Pharmacology
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