Search results for "Contraction"

showing 10 items of 1092 documents

Über die pharmakologische Prüfung von 2-Skatyl-alkylpyridinen

1968

2-Skatyl-alkylpyridine wurden an verschiedenen isolierten Organen untersucht. Die Substanzen zeigten am isolierten Rattendarm eine kompetitiv-nichtkompetitive anticholinerge Wirkung, am isolierten Meerschweinchendarm eine kompetitiv-nichtkompetitive Antihistaminwirkung. An isolierten Meerschweinchenvorhofen trat nach Gabe der tertiaren 2-Skatyl-alkylpyridine eine durch Atropin aufzuhebende negativ inotrope Wirkung auf, die quartaren Substanzen waren dagegen positiv inotrop wirksam. Die tertiaren Stoffe wirkten blutdrucksenkend, die quartaren bei kleinen Dosen blutdrucksteigernd, bei hoheren Dosen blutdrucksenkend. 2-Skatyl-alkyl-pyridines have been studied on different isolated organs. The …

AtropineContraction amplitudeRat intestineChemistryStereochemistryDrug DiscoverymedicinePharmaceutical ScienceBlood pressure loweringPharmacologyGuinea pig ileumGuinea pig atriamedicine.drugArchiv der Pharmazie
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Involvement of purinergic nerves in the NANC inhibitory junction potentials in pigeon oesophageal smooth muscle.

2004

1. Electrical field stimulation (EFS) (0.5 ms in train of 2-32 Hz for 300 ms) in smooth muscle of pigeon oesophagus, in the presence of atropine (1 microm) and guanethidine (1 microm), elicited an inhibitory response consisting of a transient hyperpolarization (inhibitory junction potential, IJP) associated with muscle relaxation. 2. Sodium nitroprusside (SNP, 100 microm) induced hyperpolarization correlated to mechanical relaxation. 3. The nitric oxide (NO) synthase inhibitor N(omega)-nitro-l-arginine (from 0.1 to 100 microm) caused a concentration-dependent reduction of electromechanical response to EFS indicating a role for NO in this response. 4. Apamin (1 microm) reduced both IJP and r…

AtropineGuanethidineAdenosinePatch-Clamp TechniquesNeuromuscular JunctionMuscarinic AntagonistsPharmacologyIn Vitro TechniquesInhibitory postsynaptic potentialApaminAutonomic Nervous Systemchemistry.chemical_compoundAdrenergic AgentsEsophaguspigeon oesophageal smooth muscle NANC pathways electrical field stimulation IJPAdenine nucleotidemedicineAnimalsColumbidaePharmacologyAdenine NucleotidesPurinergic receptorMuscle SmoothHyperpolarization (biology)AdenosineElectric StimulationElectrophysiologyMuscle relaxationchemistryBiochemistryApaminPurinesmedicine.symptommedicine.drugMuscle contractionMuscle ContractionAutonomicautacoid pharmacology
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Evidence that adenosine is not involved in the non-adrenergic non-cholinergic relaxation in the rat duodenum.

1990

In rat isolated duodenal segments, adenosine induced, in the presence of atropine and guanethidine, a dose-dependent, long-lasting (about 20 s), tetrodotoxin (TTX)-resistant relaxation both in endoluminal pressure and in isometric tension. Electrical field stimulation (EFS) induced, in the presence of atropine and guanethidine, a TTX-sensitive short-lasting (about 6 s) relaxation followed by a sustained rebound contraction. Theophylline, a P1 receptor antagonist, at the concentration of 100 microM caused a marked inhibition of the adenosine-induced relaxation, while the EFS-induced relaxation was not modified. Our results suggest that adenosine induces relaxation of the rat duodenal smooth …

AtropineGuanethidinemedicine.medical_specialtyAdenosinePhysiologyDuodenumMuscle RelaxationTetrodotoxinIn Vitro TechniquesBiochemistrychemistry.chemical_compoundTheophyllineInternal medicineIsometric ContractionmedicinePressureAnimalsTheophyllineNeurotransmitterReceptorGuanethidineReceptors PurinergicMuscle SmoothAdenosineAdenosine receptorElectric StimulationRatsAtropineEndocrinologychemistryTetrodotoxinmedicine.drugArchives internationales de physiologie et de biochimie
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Cannabinoid CB1 receptor activation modulates spontaneous contractile activity in mouse ileal longitudinal muscle.

2007

The purpose of the present study was to examine whether cannabinoid receptor agonists influence spontaneous contractile activity of longitudinal muscle in mouse ileum in vitro. Isolated segments of mouse ileum displayed spontaneous contractions with an amplitude and frequency of about 300 mg and 30 cpm, respectively. The endocannabinoid anandamide (1-100 microM), the selective cannabinoid CB(1) receptor agonist, ACEA (0.1 microM-10 microM), but not the selective cannabinoid CB(2) receptor agonist, JWH 133 (0.1 microM-10 microM), reduced in a concentration-dependent manner the spontaneous mechanical activity. The inhibitory effect consisted in a decrease of the mean amplitude of longitudinal…

AtropineMaleAgonistmedicine.medical_specialtyCB1 receptorIndolesCannabinoid receptorPolyunsaturated Alkamidesmedicine.drug_classmedicine.medical_treatmentMouse ileumArachidonic AcidsTetrodotoxinIn Vitro TechniquesDepolarization-induced suppression of inhibitionHexamethoniumReceptor Cannabinoid CB2Micechemistry.chemical_compoundPiperidinesReceptor Cannabinoid CB1IleumInternal medicineCannabinoid Receptor ModulatorsmedicineAnimalsCannabinoidPharmacologyDose-Response Relationship DrugCannabinoidsChemistryMuscle SmoothCannabinoid Receptor AgonistsReceptor antagonistEndocannabinoid systemAcetylcholineMice Inbred C57BLNG-Nitroarginine Methyl EsterEndocrinologyApaminJWH-133PyrazolesCannabinoidRimonabantSpontaneous mechanical activityEndocannabinoidsMuscle Contraction
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Autoinhibition of nicotinic release of noradrenaline from postganglionic sympathetic nerves

1970

1. The effects of nicotine, DMPP (1,1-dimethylphenylpiperazine) and acetylcholine (plus atropine) on the isolated rabbit heart were investigated. Heart rate, amplitude of contraction, coronary flow and output of noradrenaline into the perfusate were recorded. Noradrenaline was estimated fluorimetrically. 2. All nicotinic drugs evoked a dose-dependent output of noradrenaline and increased the rate and the amplitude of contraction. Increases of heart rate in response to nicotine and DMPP and increases of amplitude of contraction in response to all nicotinic drugs were clearly related to the output of noradrenaline. 3. The dose-response curves of the noradrenaline output evoked by nicotine, DM…

AtropineMaleNicotinemedicine.medical_specialtySympathetic Nervous SystemContraction (grammar)Receptors DrugAdrenergicIn Vitro TechniquesPiperazinesNicotineNorepinephrinechemistry.chemical_compoundHeart RateInternal medicineHeart ratemedicineAnimalsFluorometryGanglia AutonomicNerve EndingsPharmacologyChemistryHeartGeneral MedicineAcetylcholineStimulation ChemicalPerfusionAtropineNicotinic agonistEndocrinologyFemaleHexamethoniumRabbitsAcetylcholineMuscle Contractionmedicine.drugNaunyn-Schmiedebergs Archiv f�r Pharmakologie
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Different muscarinic receptor subtypes modulate proliferation of primary human detrusor smooth muscle cells via Akt/PI3K and map kinases.

2013

While acetylcholine (ACh) and muscarinic receptors in the bladder are mainly known for their role in the regulation of smooth muscle contractility, in other tissues they are involved in tissue remodelling and promote cell growth and proliferation. In the present study we have used primary cultures of human detrusor smooth muscle cells (HDSMCs), in order to investigate the role of muscarinic receptors in HDSMC proliferation. Samples were obtained as discarded tissue from men >65 years undergoing radical cystectomy for bladder cancer and cut in pieces that were either immediately frozen or placed in culture medium for the cell culture establishment. HDSMCs were isolated from samples, propagat…

AtropineMalePyrrolidinesMessenger030232 urology & nephrologyGene ExpressionPhosphatidylinositol 3-Kinases0302 clinical medicineAged Atropine; pharmacology Benzofurans; pharmacology Carbachol; pharmacology Cell Proliferation Cells; Cultured Cholinergic Agonists; pharmacology Gene Expression Humans Male Mitogen-Activated Protein Kinases; metabolism Muscarinic Antagonists; pharmacology Myocytes; Smooth Muscle; metabolism Phosphatidylinositol 3-Kinases; metabolism Piperidines; pharmacology Pirenzepine; analogs /&/ derivatives/pharmacology Proto-Oncogene Proteins c-akt; metabolism Pyrrolidines; pharmacology RNA; Messenger; metabolism Receptors; Muscarinic; physiology Urinary Bladder; cytologyPiperidinesSmooth MuscleReceptorsMuscarinic acetylcholine receptor M5Muscarinic acetylcholine receptorCells CulturedCulturedMuscarinic acetylcholine receptor M3Muscarinic acetylcholine receptor M2Smooth muscle contractionMuscarinic acetylcholine receptor M1Receptors Muscarinic030220 oncology & carcinogenesisMitogen-Activated Protein KinasesAcetylcholinemedicine.drugmedicine.medical_specialtyCarbacholCellsMyocytes Smooth MuscleUrinary BladderMuscarinic AntagonistsBiologyCholinergic Agonists03 medical and health sciencesInternal medicineMuscarinicmedicineHumansRNA MessengerAgedBenzofuransCell ProliferationPharmacologyMyocytesPirenzepineEndocrinologyphysiologycytologyRNACarbacholanalogs /&/ derivatives/pharmacologymetabolismProto-Oncogene Proteins c-aktPharmacological research
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Antimuscarinic action of quinidine on the heart? A study in myocardial preparations from cat hearts

1984

Quinidine exerts anticholinergic effects which have been ascribed to atropine-like properties of the drug. We have examined the effects of acetylcholine on the force of contraction in isolated heart muscle preparations from cats and compared the inhibitory effects of atropine with those of quinidine. The effects of acetylcholine were antagonized competitively in the presence of atropine. The Schild-plot yielded a straight line; the slope was not significantly different from unity. In the presence of quinidine, the concentration-response curve of acetylcholine was shifted to the right as with atropine, however, the Schild-plot yielded a regression line which was not linear; the slope was sta…

AtropineMaleQuinidineInotropemedicine.medical_specialtymedicine.drug_classAction PotentialsIn Vitro TechniquesPharmacologyParasympatholyticInternal medicinemedicineAnticholinergicAnimalsPhosphodiesterase inhibitorPharmacologyPapaverineChemistryCell MembraneParasympatholyticsMyocardial ContractionQuinidineAcetylcholineElectrophysiologyAtropineEndocrinologyCatsFemaleAcetylcholineResearch Articlemedicine.drugBritish Journal of Pharmacology
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Evidence for the presence of functional protease activated receptor 4 (PAR4) in the rat colon

2004

Background and aims: Protease activated receptors (PARs) have been postulated to play a role during intestinal inflammation. The presence and role played by PAR4 in gastrointestinal functions have not been fully clarified. The aims of this study were: (i) to examine expression of PAR4 in rat proximal colon; (ii) to determine the mechanical effects induced by PAR4 activation in longitudinal muscle; and (iii) to characterise the underlying mechanisms. Methods: PAR4 expression was determined by reverse transcription-polymerase chain reaction (RT-PCR) and immunohistochemistry. Mechanical activity was recorded as changes in isometric tension. Results: A PCR product corresponding to the predicted…

AtropineMaleQuinuclidinesmedicine.medical_specialtyColonMotilityInflammationTetrodotoxinPROTEASE-ACTIVATED RECEPTORSBiologyIntestine InflammationSettore BIO/09 - Fisiologiachemistry.chemical_compoundNeurokinin-1 Receptor AntagonistsPiperidinesInternal medicinemedicineAnimalsRNA MessengerRats WistarReceptorSettore MED/12 - GastroenterologiaDose-Response Relationship DrugReverse Transcriptase Polymerase Chain ReactionGastroenterologyMuscle SmoothReceptors Neurokinin-2ColitisImmunohistochemistryRatsEndocrinologyMechanism of actionchemistryCapsaicinCROSS-REACTIVITYBenzamidesGASTRIC SMOOTH-MUSCLETetrodotoxinReceptors ThrombinCapsaicinmedicine.symptomGastrointestinal MotilityOligopeptidesAcetylcholineMuscle Contractionmedicine.drugMuscle contractionGut
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Arginine vasopressin, via activation of post-junctional V1 receptors, induces contractile effects in mouse distal colon

2013

The aim of this study was to analyze whether arginine vasopressin (AVP) may be considered a modulator of intestinal motility. In this view, we evaluated, in vitro, the effects induced by exogenous administration of AVP on the contractility of mouse distal colon, the subtype(s) of receptor(s) activated and the action mechanism. Isometric recordings were performed on longitudinal and circular muscle strips of mouse distal colon. AVP (0.001 nM-100 nM) caused concentration-dependent contractile effects only on the longitudinal muscle, antagonized by the V1 receptor antagonist, V-1880. AVP-induced effect was not modified by tetrodotoxin, atropine and indomethacin. Contractile response to AVP was…

AtropineMaleReceptors Vasopressinmedicine.medical_specialtyVasopressinCarbacholNifedipineColonPhysiologyIndomethacinClinical BiochemistryMuscarinic AntagonistsTetrodotoxinCholinergic AgonistsIn Vitro TechniquesBiologyBiochemistryContractilityMiceCellular and Molecular Neurosciencechemistry.chemical_compoundPhosphoinositide Phospholipase CEndocrinologyInternal medicinemedicineAnimalsCyclooxygenase InhibitorsReceptorVasopressin receptorPhospholipase CArginine vasopressin receptor 1AMuscle SmoothCalcium Channel BlockersArginine vasopressinIntestinalcontractility V1 receptorsPhospholipase C Mouse colonArginine VasopressinEnzyme ActivationMice Inbred C57BLEndocrinologychemistryCarbacholGastrointestinal MotilityCyclopiazonic acidhormones hormone substitutes and hormone antagonistsMuscle ContractionSignal Transductionmedicine.drugRegulatory Peptides
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Muscarine receptor types mediating autoinhibition of acetylcholine release and sphincter contraction in the guinea-pig iris.

1990

The potencies of several muscarine receptor antagonists in blocking either the autoinhibition of acetylcholine release or the muscarinic contraction of the sphincter muscle upon acetylcholine release were investigated in the guinea-pig iris. The agonist at pre- or postjunctional muscarine receptors was acetylcholine released upon field stimulation (5.5 Hz, 2 min) of the irides preloaded with 14C-choline. The stimulation-evoked 14C-overflow was doubled in the presence of atropine 0.1 mumol/l but unaffected by the agonist (+/-)-methacholine (50 mumol/l). Thus, under the present stimulation conditions, the autoinhibition of acetylcholine release on the guinea-pig iris cholinergic nerves was ne…

AtropineMalemedicine.medical_specialtyGuinea PigsNeuromuscular JunctionIrisBiologyDiaminesIn Vitro Techniqueschemistry.chemical_compoundInternal medicineMuscarinic acetylcholine receptormedicineMethoctramineAnimalsMethacholine CompoundsMethacholine ChloridePharmacologyMuscarineGallamine TriethiodideGallamine triethiodideMuscle SmoothGeneral MedicinePirenzepinePirenzepineReceptors MuscarinicAcetylcholineElectric StimulationEndocrinologychemistryCholinergicFemalemedicine.symptomAcetylcholineMuscle contractionmedicine.drugMuscle ContractionNaunyn-Schmiedeberg's archives of pharmacology
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