Search results for "Telenzepine"

showing 3 items of 3 documents

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…

medicine.medical_specialtyGuinea PigsMuscarinic AntagonistsInhibitory postsynaptic potentialchemistry.chemical_compoundHeart RateInternal medicineMuscarinic acetylcholine receptormedicineMuscarinic acetylcholine receptor M4AnimalsPharmacologyChemistryMyocardiumHeartMuscle SmoothGeneral MedicinePirenzepineMyocardial ContractionAcetylcholineElectric StimulationAtropineEndocrinologyTelenzepineAutoreceptorCholinesterase InhibitorsChickensAcetylcholinemedicine.drugNaunyn-Schmiedeberg's archives of pharmacology
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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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Cigarette smoke extract activates human bronchial epithelial cells affecting non-neuronal cholinergic system signalling in vitro.

2010

Abstract Aims Acetylcholine (ACh) is synthesized by Choline Acetyl-Transferase (ChAT) that exerts its physiological effects in airway epithelial cells via muscarinic receptor (MR) activation. We evaluate the effect of ACh stimulation on human bronchial epithelial cells (16-HBE) and test whether cigarette smoke extract (CSE) can modify the basal cellular response to ACh affecting the non-neuronal cholinergic system signalling. Main methods ACh stimulated 16-HBE were tested for ACh-binding, Leukotriene B 4 (LTB 4 ) release and ERK1/2 and NFkB pathway activation. Additionally, we investigated all the aforementioned parameters as well as ChAT and MR proteins and mRNA expression and endogenous A…

medicine.medical_specialtyLeukotriene B4Blotting WesternEndogenyStimulationBronchiPharmacologyBiologyComplex MixturesIn Vitro TechniquesLeukotriene B4General Biochemistry Genetics and Molecular BiologyCell LineCholine O-Acetyltransferasechemistry.chemical_compoundInternal medicineSmokeparasitic diseasesMuscarinic acetylcholine receptorTobaccomedicineHumansGeneral Pharmacology Toxicology and PharmaceuticsReceptorExtracellular Signal-Regulated MAP KinasesAnalysis of VarianceReverse Transcriptase Polymerase Chain ReactionNF-kappa BCholine Acetyl-TransferaseAcetylcholine muscarinic receptorhuman bronchial epithelial cellsGeneral MedicineFlow CytometryCholine acetyltransferaseReceptors MuscarinicAcetylcholineEndocrinologychemistryGene Expression RegulationTelenzepineAcetylcholinemedicine.drugSignal Transduction
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