Search results for "Piper"

showing 10 items of 632 documents

Role of K+ and Ca2+ fluxes in the cerebroarterial vasoactive effects of sildenafil

2007

The aim of this study was to assess the role of K(+) and Ca(2+) fluxes in the cerebroarterial vasoactive effects of the phosphodiesterase-5 inhibitor sildenafil. We used isolated rabbit basilar arteries to assess the effects of extracellular K(+) raising on sildenafil-induced vasodilatation, and studied the pharmacological interaction of sildenafil with selective modulators of membrane K(+) and Ca(2+) channels. Expression of Kv1 subunits of K(+) channels was assessed at messenger and protein levels. Parallel experiments were carried out with zaprinast for comparison. Sildenafil (10 nM-0.1 mM) induced concentration-dependent relaxation of endothelin-1 (10 nM)-precontracted arteries, which wa…

Malemedicine.medical_specialtyCalcium Channels L-Typemedicine.drug_mechanism_of_actionPhosphodiesterase InhibitorsVasodilationIn Vitro TechniquesPharmacologyPiperazinesSildenafil Citratechemistry.chemical_compoundInternal medicinemedicineAnimalsChannel blockerRNA MessengerSulfonesPharmacologyTetraethylammoniumDose-Response Relationship DrugChemistryDepolarization3-Pyridinecarboxylic acid 14-dihydro-26-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)- Methyl esterIberiotoxinEndocrinologyPurinesBasilar ArterycGMP-specific phosphodiesterase type 5PotassiumShaker Superfamily of Potassium ChannelsCalciumRabbitsZaprinastPhosphodiesterase 5 inhibitorEuropean Journal of Pharmacology
researchProduct

Antidepressant-like behavioral effects of impaired cannabinoid receptor type 1 signaling coincide with exaggerated corticosterone secretion in mice.

2007

Hypothalamic-pituitary-adrenocortical (HPA) axis hyperactivity is associated with major depressive disorders, and treatment with classical antidepressants ameliorates not only psychopathological symptoms, but also the dysregulation of the HPA axis. Here, we further elucidated the role of impaired cannabinoid type 1 receptor (CB1) signaling for neuroendocrine and behavioral stress coping in the mouse forced swim test (FST). We demonstrate that the genetic inactivation of CB1 is accompanied by increased plasma corticosterone levels both under basal conditions and at different time points following exposure to the FST. The latter effect could be mimicked in C57BL/6N mice by acute, subchronic, …

Malemedicine.medical_specialtyCannabinoid receptorTime FactorsEndocrinology Diabetes and Metabolismmedicine.medical_treatmentAntidepressive Agents TricyclicStatistics NonparametricArticlechemistry.chemical_compoundMiceEndocrinologyRimonabantPiperidinesReceptor Cannabinoid CB1CorticosteroneDesipramineInternal medicineCannabinoid receptor type 1Adaptation PsychologicalmedicineAnimalsBiological PsychiatrySwimmingMice KnockoutAnalysis of VarianceEndocrine and Autonomic SystemsDepressionDesipramineMice Inbred C57BLPsychiatry and Mental healthDisease Models AnimalEndocrinologychemistrynervous systemPyrazoleslipids (amino acids peptides and proteins)FemaleCannabinoidRimonabantPsychologyCorticosteronehuman activitiesGlucocorticoidStress Psychologicalmedicine.drugBehavioural despair testSignal TransductionPsychoneuroendocrinology
researchProduct

Impaired cannabinoid receptor type 1 signaling interferes with stress-coping behavior in mice.

2007

Dysregulation of the endocannabinoid system is known to interfere with emotional processing of stressful events. Here, we studied the role of cannabinoid receptor type 1 (CB1) signaling in stress-coping behaviors using the forced swim test (FST) with repeated exposures. We compared effects of genetic inactivation with pharmacological blockade of CB1 receptors both in male and female mice. In addition, we investigated potential interactions of the endocannabinoid system with monoaminergic and neurotrophin systems of the brain. Naive CB1 receptor-deficient mice (CB1-/-) showed increased passive stress-coping behaviors as compared to wild-type littermates (CB1+/+) in the FST, independent of se…

Malemedicine.medical_specialtyCannabinoid receptormedicine.medical_treatmentBiologyPharmacologyHippocampusMicePiperidinesReceptor Cannabinoid CB1Internal medicineCannabinoid receptor type 1MonoaminergicAdaptation PsychologicalGeneticsmedicineAnimalsBiogenic MonoaminesRNA MessengerReceptorMonoamine OxidaseSwimmingPharmacologyBrain-derived neurotrophic factormusculoskeletal neural and ocular physiologyBrain-Derived Neurotrophic FactorDesipraminefood and beveragesEndocannabinoid systemMice Inbred C57BLMonoamine neurotransmitterEndocrinologynervous systemVesicular Glutamate Transport Protein 1Molecular MedicinePyrazoleslipids (amino acids peptides and proteins)FemaleCannabinoidRimonabantpsychological phenomena and processesStress PsychologicalSignal TransductionThe pharmacogenomics journal
researchProduct

Gastric Emptying in Infants with Gastroesophageal Reflux: Ultrasound Evaluation before and after Cisapride Administration

1992

The present study aimed to evaluate gastric emptying in children with gastroesophageal reflux (GER) by means of real-time ultrasonography, on the basis of measurements of the cross-sectional area of the gastric antrum. Twelve children with GER were studied (seven males, five females; age range, 3-13 months) and compared with 12 normal control children (six males, six females; age range, 3-13 months). The diagnosis of GER was confirmed by 24-h esophageal pH-monitoring. The GER patients had a significantly greater antral area than the controls at 90, 105, and 120 min after eating a standard meal (cow's milk formula, 300 ml/m2 body surface area); in addition, final gastric emptying time was si…

Malemedicine.medical_specialtyGastroenterologyPiperidinesInternal medicinemedicineHumansAntrumUltrasonographyBody surface areaCisaprideGastric Acidity DeterminationGastric emptyingEsophageal diseasebusiness.industryStomachStomachdigestive oral and skin physiologyGastroenterologyRefluxInfantGastric Acidity Determinationmedicine.diseasemedicine.anatomical_structureGastric EmptyingCisaprideGastroesophageal RefluxFemaleSerotonin Antagonistsbusinessmedicine.drugScandinavian Journal of Gastroenterology
researchProduct

Gastrointestinal stromal tumour of the rectum: Report of a case and review of literature

2008

Gastrointestinal stromal tumour (GIST) is a rare tumour of the gastrointestinal tract which does not generally originate in the rectum. The authors describe a case of a 70-year-old man who underwent an anterior resection of the rectum for a low-risk GIST. The patient was not given adjuvant chemotherapy with imatinib and is still disease-free 30 mo after surgery. The authors conclude that although rectal GIST is extremely uncommon, it should be included in differential diagnosis when a tumour in the rectum is detected. Biopsy of the tumour is essential, since this makes it possible to reach a sure preoperative diagnosis based on the immunohistological features of the CD117 and CD34. Although…

Malemedicine.medical_specialtyGastrointestinal Stromal TumorsCD34RectumAntigens CD34Antineoplastic AgentsCase ReportPiperazinesGIST;BiopsymedicineHumansneoplasmsAgedGastrointestinal tractGiSTmedicine.diagnostic_testbiologyRectal NeoplasmsCD117business.industryGastroenterologyGeneral MedicineCombined Modality Therapydigestive system diseasesSurgeryProto-Oncogene Proteins c-kitPyrimidinesTreatment Outcomemedicine.anatomical_structureImatinib mesylateBenzamidesImatinib Mesylatebiology.proteinDifferential diagnosisbusinessGISTWorld Journal of Gastroenterology
researchProduct

Presynaptic nicotine receptors mediating a positive feed-back on transmitter release from the rat phrenic nerve.

1986

The effects of 1,1-dimethyl-4-phenylpiperazinium (DMPP) and of nicotine receptor antagonists on [3H]acetylcholine release from the rat phrenic nerve preincubated with [3H]choline were investigated in the absence and presence of cholinesterase inhibitors (presynaptic effects). Additionally, the effects of hexamethonium and tubocurarine on the muscle contraction of the indirectly stimulated diaphragm were examined (postsynaptic effects). DMPP (1-30 microM) increased (76-92%), whereas hexamethonium (0.001-1 mM) and tubocurarine (1-10 microM) decreased (52-60%) the release of [3H]acetylcholine following a train of 100 pulses at 5 Hz. The release caused by a longer train (750 pulses at 5 Hz) was…

Malemedicine.medical_specialtyMotor nerveTubocurarineHexamethonium CompoundsIn Vitro TechniquesReceptors NicotinicNeuromuscular junctionFeedbackchemistry.chemical_compoundPostsynaptic potentialInternal medicinemedicineAnimalsCholinesterasePhrenic nervePharmacologyNeurotransmitter AgentsbiologyRats Inbred StrainsGeneral Medicinemusculoskeletal systemElectric StimulationRatsPhrenic NerveEndocrinologymedicine.anatomical_structurechemistrybiology.proteinHexamethoniummedicine.symptomDimethylphenylpiperazinium IodideAcetylcholineMuscle contractionmedicine.drugNaunyn-Schmiedeberg's archives of pharmacology
researchProduct

Endothelin-1-induced potentiation of adrenergic responses in the rabbit pulmonary artery: role of thromboxane A(2).

2001

Abstract To examine whether low concentrations of endothelin-1 potentiate the vasocontrictor response to adrenergic stimulation, we recorded the isometric response of rings of rabbit pulmonary artery to electrical stimulation and noradrenaline. Endothelin-1 (10 −10 M) potentiated the contractions induced by electrical stimulation and noradrenaline. The endothelin ET B receptor antagonist (2,6-dimethylpiperidinecarbonyl-γ-methyl-Leu- N in -[Methoxycarbonyl]- d -Trp- d -Nle) (BQ-788, 10 −6 M), but not the endothelin ET A receptor antagonist cyclo( d -Asp-Pro- d -Val-Leu- d -TRP) (BQ-123, 10 −6 M), inhibited the potentiating effects of endothelin-1. Pretreatment with the cyclooxygenase inhibit…

Malemedicine.medical_specialtyNifedipineThromboxanemedicine.drug_classAdrenergicPulmonary ArteryThromboxane A2chemistry.chemical_compoundNorepinephrineThromboxane A2PiperidinesInternal medicinemedicineAnimalsVasoconstrictor AgentsAntihypertensive AgentsPharmacologybiologyDose-Response Relationship DrugEndothelin-1Receptors EndothelinReceptor antagonistCalcium Channel BlockersEndothelin 1Receptor Endothelin BElectric StimulationEndocrinologychemistryVasoconstrictionbiology.proteinCyclooxygenaseThromboxane-A synthaseRabbitsEndothelin receptorOligopeptidesEuropean journal of pharmacology
researchProduct

Cannabinoid type 1 receptor blockade promotes mitochondrial biogenesis through endothelial nitric oxide synthase expression in white adipocytes

2008

OBJECTIVE—Cannabinoid type 1 (CB1) receptor blockade decreases body weight and adiposity in obese subjects; however, the underlying mechanism is not yet fully understood. Nitric oxide (NO) produced by endothelial NO synthase (eNOS) induces mitochondrial biogenesis and function in adipocytes. This study was undertaken to test whether CB1 receptor blockade increases the espression of eNOS and mitochondrial biogenesis in white adipocytes. RESEARCH DESIGN AND METHODS—We examined the effects on eNOS and mitochondrial biogenesis of selective pharmacological blockade of CB1 receptors by SR141716 (rimonabant) in mouse primary white adipocytes. We also examined eNOS expression and mitochondrial biog…

Malemedicine.medical_specialtyNitric Oxide Synthase Type IIIEndocrinology Diabetes and MetabolismAdipocytes WhiteImmunoblottingCitrate (si)-SynthaseWhite adipose tissueAMP-Activated Protein KinasesProtein Serine-Threonine KinasesMitochondrionDNA MitochondrialMicechemistry.chemical_compoundAdenosine TriphosphatePiperidinesReceptor Cannabinoid CB1AMP-activated protein kinaseMultienzyme ComplexesEnosAdipocyteInternal medicineInternal MedicinemedicineAnimalsPhosphorylationRNA Small InterferingReceptorCells CulturedDose-Response Relationship DrugbiologyReverse Transcriptase Polymerase Chain ReactionFlow Cytometrybiology.organism_classificationMitochondriaMice Inbred C57BLNitric oxide synthaseMetabolismEndocrinologychemistryMitochondrial biogenesisbiology.proteinSettore BIO/14 - FarmacologiaPyrazolesRimonabant
researchProduct

Lower self-reported depression in patients with erectile dysfunction after treatment with sildenafil

2001

Abstract Background: Depressive symptoms in men with erectile dysfunction (ED) may improve under successful ED treatment. Self-reported depressive symptoms were compared in men with ED after sildenafil treatment to a group of untreated patients. Methods: In an open study, self-reported depressive symptoms of 54 men after successful treatment with sildenafil (>4 weeks) and 51 men awaiting ED treatment were investigated with the Center of Epidemiologic Studies–Depression Scale (CES–D). CES–D items were subjected to an exploratory factor analysis and group differences in CES–D items and factors were analyzed. Results: Groups were comparable with respect to demographic characteristics and illne…

Malemedicine.medical_specialtyPersonality InventoryDepression scaleSildenafilmedia_common.quotation_subjectPiperazinesSildenafil Citratechemistry.chemical_compoundErectile DysfunctionInternal medicinemedicineHumansIn patientSulfonesRisk factorDepression (differential diagnoses)Agedmedia_commonSelection biasDepressionMiddle Agedmedicine.diseasePsychiatry and Mental healthClinical PsychologyCross-Sectional StudiesTreatment OutcomeErectile dysfunctionchemistryPurinesPsychologyAfter treatmentClinical psychologyJournal of Affective Disorders
researchProduct

Relaxant effect of sildenafil in the rabbit basilar artery

2005

We hypothesized that sildenafil, inhibitor of phosphodiesterase-5 (PDE-5), interacts with the nitric oxide (NO)-cGMP pathway in the cerebral arteries and shows vasoactive effects. To prove it in the isolated rabbit basilar artery, we compared the effects of sildenafil with other PDE-5 inhibitors, assessed the endothelial dependence of the vasoactive responses, and used modulators of the cGMP and cAMP signaling processes. Sildenafil (10 nM-0.1 mM) induced concentration-dependent relaxations of endothelin-1 (10 nM)-precontracted basilar artery, which were partially inhibited both in endothelium-denuded arteries and in arteries precontracted by depolarization with KCl (50 mM). Endothelin-1 (1 …

Malemedicine.medical_specialtyPhosphodiesterase InhibitorsPhysiologySildenafilVasodilator AgentsCerebral arteriesVasodilationIn Vitro TechniquesPiperazinesSildenafil Citratechemistry.chemical_compound3'5'-Cyclic-GMP PhosphodiesterasesQuinoxalinesmedicine.arteryInternal medicinemedicineBasilar arteryAnimalsSulfonesCyclic Nucleotide Phosphodiesterases Type 5PharmacologyOxadiazolesDose-Response Relationship DrugPhosphoric Diester HydrolasesPDE5 drug designVasodilationNG-Nitroarginine Methyl EsterEndocrinologychemistryGuanylate CyclasePurinesBasilar Arterycardiovascular systemMolecular MedicineRabbitsSodium nitroprussideNitric Oxide SynthaseSoluble guanylyl cyclaseZaprinastSignal Transductionmedicine.drugVascular Pharmacology
researchProduct