Search results for "Apamin"

showing 10 items of 39 documents

Components of after-hyperpolarization in magnocellular neurones of the rat supraoptic nucleusin vitro

1998

1. The pharmacological sensitivity of hyperpolarizing components of spike train after-potentials was examined in sixty-one magnocellular neurones of the rat supraoptic nucleus using intracellular recording techniques in a brain slice preparation. 2. In 26 % of all neurones a slow after-hyperpolarization (AHP) was observed in addition to a fast AHP. In 31 % of all neurones a depolarizing after-potential (DAP) was observed. 3. The fast AHP was blocked by apamin whereas the slow AHP was blocked by charybdotoxin (ChTX). The DAP was enhanced by ChTX or a DAP was unmasked if not present during the control period. 4. Low concentrations of TEA (0.15-1.5 mM) induced effects on the slow AHP and the D…

MalePotassium ChannelsCharybdotoxinPhysiologySpike trainAction PotentialsApaminSupraoptic nucleusRats Sprague-DawleySK channelchemistry.chemical_compoundSlice preparationAnimalsNeuronsKv1.3 Potassium ChannelVoltage-gated ion channelChemistryMargatoxinTetraethylammoniumOriginal ArticlesIberiotoxinImmunohistochemistryRatsElectrophysiologyApaminPotassium Channels Voltage-GatedBiophysicsSupraoptic NucleusNeuroscienceThe Journal of Physiology
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The Janus face of chlorogenic acid on vascular reactivity: A study on rat isolated vessels

2016

Abstract Background Chlorogenic acid (CGA), the main polyphenol contained in coffee, is a major contributor to dietary polyphenol intake. Few studies reported its anti-hypertensive properties but the mechanisms are still indefinite. Purpose The present study assessed the direct effect of CGA in endothelium denuded or intact aortic rings from male Wistar rats and the mechanisms involved. Methods/Results CGA induced a direct endothelium-dependent relaxation that was significantly reduced by L-NAME (10 −4  M), indomethacin (10 −5  M) and combination of apamin (10 −7  M) and charybdotoxin (10 −7  M). Incubation of rings with CGA induced a dual effect on agonist-induced vasorelaxation. At 10 −6 …

Maleendocrine systemCharybdotoxinEndotheliumPharmaceutical ScienceVasodilation030204 cardiovascular system & hematologyPharmacologyApaminMuscle Smooth Vascular03 medical and health scienceschemistry.chemical_compound0302 clinical medicineDrug DiscoverymedicineAnimals[CHIM]Chemical SciencesRats WistarPhenylephrineAntihypertensive AgentsComputingMilieux_MISCELLANEOUSPharmacology[SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciencesRatsVasodilationmedicine.anatomical_structureComplementary and alternative medicineBiochemistrychemistry030220 oncology & carcinogenesisHypertensionMolecular MedicineSodium nitroprussideEndothelium Vascularmedicine.symptomChlorogenic AcidVasoconstrictionAcetylcholinemedicine.drug
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Role of cholinergic neurons in the motor effects of glucagon-like peptide-2 in mouse colon

2010

Glucagon-like peptide-2 (GLP-2) reduces mouse gastric tone and small intestine transit, but its action on large intestine motility is still unknown. The purposes of the present study were 1) to examine the influence of GLP-2 on spontaneous mechanical activity and on neurally evoked responses, by recording intraluminal pressure from mouse isolated colonic segments; 2) to characterize GLP-2 mechanism of action; and 3) to determine the distribution of GLP-2 receptor (GLP-2R) in the mouse colonic muscle coat by immunohistochemistry. Exogenous GLP-2 (0.1–300 nM) induced a concentration-dependent reduction of the spontaneous mechanical activity, which was abolished by the desensitization of GLP-…

Maleendocrine systemmedicine.medical_specialtyCarbacholColonPhysiologymedicine.drug_classBlotting WesternBiologyApaminSettore BIO/09 - FisiologiaMicechemistry.chemical_compoundenteric nervous systemcolonic motilityPhysiology (medical)Internal medicineGlucagon-Like Peptide 2Receptors GlucagonmedicineAnimalsCholinergic neuronNeuronsAnalysis of VarianceDose-Response Relationship DrugHepatologydigestive oral and skin physiologyGastroenterologyMuscle Smoothgastrointestinal hormoneMotor neuronReceptor antagonistImmunohistochemistryCholine acetyltransferaseElectric StimulationacetylcholineEndocrinologymedicine.anatomical_structurechemistryGlucagon-Like Peptide-2 ReceptorCholinergicGastrointestinal Motilityhormones hormone substitutes and hormone antagonistsAcetylcholineMuscle Contractionmedicine.drugAmerican Journal of Physiology-Gastrointestinal and Liver Physiology
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Interplay between PACAP and NO in mouse ileum

2003

Abstract We investigated the possibility that pituitary adenylate cyclase activating peptide (PACAP) has a role in the control of contractility in the mouse ileum. PACAP-(1-27) produced tetrodotoxin (TTX)-insensitive, concentration-dependent reduction of the amplitude of the spontaneous contractions of longitudinal muscle up to their complete disappearance. This effect was inhibited by PACAP-(6-38), PACAP receptor antagonist, and by apamin, blocker of small-conductance Ca2+-activated K+-channels. Nω-nitro- l -arginine methyl ester (L-NAME), nitric oxide (NO) synthase inhibitor, reduced the PACAP-inhibitory response, and the joint application of apamin plus L-NAME produced additive effects. …

Maleendocrine systemmedicine.medical_specialtyMuscle RelaxationMouse ileumStimulationIn Vitro TechniquesApaminSettore BIO/09 - FisiologiaContractilityMiceCellular and Molecular Neurosciencechemistry.chemical_compoundSmooth muscleIleumInternal medicinemedicineAnimalsMyocyteNitric Oxide DonorsPharmacologyDose-Response Relationship DrugNeuropeptidesNitric oxideSmooth muscle contractionMice Inbred C57BLPituitary adenylate cyclase-activating peptideEndocrinologyApaminchemistryTetrodotoxinPituitary Adenylate Cyclase-Activating PolypeptideSodium nitroprussidePACAP (pituitary adenylate cyclase activating peptide)hormones hormone substitutes and hormone antagonistsmedicine.drugNeuropharmacology
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A1 receptors mediate adenosine inhibitory effects in mouse ileum via activation of potassium channels.

2008

Abstract Aims We investigated the effects induced by exogenous adenosine on the spontaneous contractile activity of the longitudinal muscle of a mouse ileum, the receptor subtypes activated, the involvement of enteric nerves and whether opening of K + channels was a downstream event leading to the observed effects. Main methods Mechanical responses of the mouse ileal longitudinal muscle to adenosine were examined in vitro as changes in isometric tension. Key findings Adenosine caused a concentration-dependent reduction of the spontaneous contraction amplitude of the ileal longitudinal muscle up to its complete disappearance. This effect induced was markedly reduced by an A 1 receptor antago…

Malemedicine.medical_specialtyAdenosinePotassium ChannelsAdenosine A2 Receptor AgonistsMouse ileumBlotting WesternAdenosine A3 Receptor AntagonistsAdenosine A1 Receptor AntagonistsApaminSettore BIO/09 - FisiologiaGeneral Biochemistry Genetics and Molecular BiologyAdenosine A1 receptorchemistry.chemical_compoundMiceAdenosine A3 Receptor AgonistsIleumInternal medicineNeural PathwaysmedicinePotassium Channel BlockersPurinergic P1 Receptor AgonistsAnimalsGeneral Pharmacology Toxicology and PharmaceuticsP1 purinoceptorDose-Response Relationship DrugChemistryReceptor Adenosine A1Mechanical activityMuscle SmoothGeneral MedicinePurinergic signallingIberiotoxinAdenosine A3 receptorAdenosineAdenosine receptorAdenosine A1 Receptor AgonistsAdenosine A2 Receptor AntagonistsMice Inbred C57BLEndocrinologyPurinergic P1 Receptor AntagonistsAdenosine A2B receptormedicine.drugMuscle ContractionLife sciences
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Tetrodotoxin-dependent effects of menthol on mouse gastric motor function.

2013

Menthol, the main active constituent of peppermint oil, exerts gut spasmolytic effects, although its mechanism of action remains unclear. We investigated the effects of menthol on gastric emptying and spontaneous- or evoked- mechanical activity of whole murine stomach. Gastric emptying was calculated after i.p. administration of menthol (50mg/Kg). Responses induced by menthol on gastric intraluminal pressure and evoked-cholinergic contractions were analyzed in vitro. Menthol decreased the gastric emptying rate. In vitro, menthol (0.3-30 mM) produced a concentration-dependent relaxation of whole stomach, that was significantly reduced by tetrodotoxin or ω-conotoxin GVIA. The gastric relaxant…

Malemedicine.medical_specialtyCarbacholVasoactive intestinal peptideTetrodotoxinPharmacologyIn Vitro TechniquesApaminNoradrenergic pathwaychemistry.chemical_compoundMicePhentolamineInternal medicinemedicineAnimalsGuanethidinePharmacologyGastric emptyingStomachAntagonistAcetylcholineBiomechanical PhenomenaMice Inbred C57BLMentholEndocrinologychemistryGastric EmptyingGastric MucosaEnteric nervous systemMentholmedicine.drugMuscle ContractionEuropean journal of pharmacology
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Neurotensin: dual effect on the motor activity of rat duodenum

1992

The effects of neurotensin on mechanical activity of rat duodenum were investigated using an isometric-isovolumic preparation. Neurotensin (1 pM to 10 nM) induced a concentration-dependent, tetrodotoxin (TTX)-insensitive fall in both endoluminal pressure and isometric tension. At higher concentrations of neurotensin (1 nM to 1 microM) the relaxation was followed by a concentration-dependent TTX-insensitive contraction, detected only by an increase in endoluminal pressure. Different concentrations of neurotensin were required to desensitize the relaxant and the contractile actions of the neuropeptide. The relaxation was antagonized by apamin, while the contractile response was blocked by nif…

Malemedicine.medical_specialtyContraction (grammar)NifedipineDuodenumMuscle RelaxationNeuropeptideIn Vitro TechniquesBiologyApamincomplex mixturesdigestive systemchemistry.chemical_compoundNifedipineInternal medicinemedicineAnimalsReceptors NeurotensinNeurotensinPharmacologymusculoskeletal neural and ocular physiologydigestive oral and skin physiologyRats Inbred StrainsElectric StimulationRatsReceptors NeurotransmitterMuscle relaxationEndocrinologyApaminnervous systemchemistryTetrodotoxinCalciummedicine.symptomGastrointestinal MotilityMuscle ContractionNeurotensinmedicine.drugMuscle contractionEuropean Journal of Pharmacology
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On the peptidergic hypothesis for non-adrenergic non-cholinergic innervation in the rat duodenum

1992

1. The nature of the non-adrenergic, non-cholinergic (NANC) transmitter was studied in vitro in the rat duodenum, by use of an isometric-isovolumic preparation. 2. Electrical field stimulation (EFS) induced a tetrodotoxin (TTX)-sensitive fall both in luminal pressure and in isometric tension. 3. Neurotensin (NT) induced TTX-insensitive inhibitory responses similar to those induced by EFS. Vasoactive intestinal peptide (VIP) caused a delayed, slow, concentration-dependent, TTX-insensitive inhibitory effect, detected only by a change in luminal pressure. 4. alpha-chymotrypsin prevented the NT- and VIP-induced inhibitory effects and antagonized the response to EFS. 5. Apamin antagonized the EF…

Malemedicine.medical_specialtyDuodenumMuscle RelaxationVasoactive intestinal peptideIn Vitro TechniquesBiologyAutonomic Nervous SystemApaminInhibitory postsynaptic potentialchemistry.chemical_compoundDesensitization (telecommunications)Isometric ContractionInternal medicinemedicineAnimalsChymotrypsinReceptorNeurotensinPharmacologymusculoskeletal neural and ocular physiologyGeneral NeuroscienceNeuropeptidesMuscle SmoothRats Inbred StrainsElectric StimulationRatsmedicine.anatomical_structureEndocrinologyApaminchemistryTetrodotoxinDuodenumhormones hormone substitutes and hormone antagonistsVasoactive Intestinal PeptideNeurotensinJournal of Autonomic Pharmacology
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Functional evidence for different roles of GABAA and GABAB receptors in modulating mouse gastric tone

2010

Abstract The aims of the present study were to investigate, using mouse whole stomach in vitro , the effects of γ-aminobutyric acid (GABA) and GABA receptor agonists on the spontaneous gastric tone, to examine the subtypes of GABA receptors involved in the responses and to determine the possible site(s) of action. GABA induced gastric relaxation, which was antagonized by the GABA A -receptor antagonist, bicuculline, potentiated by phaclofen, GABA B -receptor antagonist, but not affected by 1,2,5,6-Tetrahydropyridin-4-yl methylphosphinic acid hydrate (TPMPA), GABA C -receptor antagonist. Muscimol, GABA A -receptor agonist, mimicked GABA effects inducing relaxation, which was significantly re…

Malemedicine.medical_specialtymedicine.drug_classMuscle RelaxationIn Vitro TechniquesGABAB receptorApaminSettore BIO/09 - FisiologiaMicePotassium Channels Calcium-ActivatedGABACellular and Molecular Neurosciencechemistry.chemical_compoundPhaclofenReceptors GABAGABA receptorNANC inhibitory nerves.GABA receptorInternal medicinemedicineAnimalsGABA-A Receptor AgonistsGABA-A Receptor Antagonistsgamma-Aminobutyric AcidPharmacologyGABAA receptorMuscle SmoothBicucullineReceptors GABA-AReceptor antagonistMice Inbred C57BLEndocrinologyReceptors GABA-Bnervous systemMuscimolchemistryGABA-B Receptor AgonistsMuscle Tonuscholinergic excitatory nerveNitric Oxide SynthaseGABA-B Receptor Antagonistsstomachmedicine.drugNeuropharmacology
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NANC inhibitory neurotransmission in mouse isolated stomach: Involvement of nitric oxide, ATP and vasoactive intestinal polypeptide

2003

1. The neurotransmitters involved in NANC relaxation and their possible interactions were investigated in mouse isolated stomach, recording the motor responses as changes of endoluminal pressure from whole organ. 2. Field stimulation produced tetrodotoxin-sensitive, frequency-dependent, biphasic responses: rapid transient relaxation followed by a delayed inhibitory component. 3. The inhibitor of the synthesis of nitric oxide (NO), L-NAME, abolished the rapid relaxation and significantly reduced the slow relaxation. Apamin, blocker of Ca 2+-dependent K + channels, or ADPβS, which desensitises P 2y purinoceptors, reduced the slow relaxation to 2-8 Hz, without affecting that to 16-32 Hz or the…

NitroprussideMuscle RelaxationNANC inhibitory neurotransmitterNitric OxideSynaptic TransmissionSettore BIO/09 - FisiologiaGastric relaxationMiceAdenosine TriphosphateAdrenergic FiberChymotrypsinEnzyme InhibitorThionucleotideCholinergic FiberPharmacologyDose-Response Relationship DrugAnimalIn Vitro TechniqueMouse stomachStomachNitric Oxide DonorElectric StimulationATPVIPAdenosine DiphosphateMice Inbred C57BLNG-Nitroarginine Methyl EsterApaminReceptors Vasoactive Intestinal PeptideNitric Oxide SynthaseVasoactive Intestinal Peptide
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