Search results for "Dopamine Antagonists"

showing 10 items of 44 documents

Brain histamine depletion enhances the behavioural sequences complexity of mice tested in the open-field: Partial reversal effect of the dopamine D2/…

2017

Markers of histaminergic dysregulation were found in several neuropsychiatric disorders characterized by repetitive behaviours, thoughts and stereotypies. We analysed the effect of acute histamine depletion by means of i. c.v. injections of alpha-fluoromethylhistidine, a blocker of histidine decarboxylase, on the temporal organization of motor sequences of CD1 mice behaviour in the open-field test. An ethogram encompassing 9 behavioural components was employed. Durations and frequencies were only slightly affected by treatments. However, as revealed by multivariate t-pattern analysis, histamine depletion was associated with a striking increase in the number of behavioural patterns. We found…

0301 basic medicineMaleDopaminePharmacologyT-pattern analysisSettore BIO/09 - FisiologiaOpen fieldAlpha-fluoromethilhistidine03 medical and health sciencesCellular and Molecular Neurosciencechemistry.chemical_compoundMiceRandom Allocation0302 clinical medicineDopamineDopamine receptor D2medicineAnimalsPharmacologyReceptors Dopamine D2Multivariate analysiAntagonistHistaminergicReceptors Dopamine D3BrainHistidine decarboxylaseGrooming030104 developmental biologychemistryExploratory BehaviorDopamine AntagonistsSulpirideSulpiridePsychology030217 neurology & neurosurgeryHistaminemedicine.drugHistamineNeuropharmacology
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[123I]IBZM SPECT in patients treated with typical and atypical neuroleptics: relationship to drug plasma levels and extrapyramidal side effects

1997

[123I]Iodobenzamide (IBZM) is an iodine-labeled dopamine receptor ligand and can be used to visualize brain D2 receptors in humans with single photon emission computerized tomography (SPECT). The ratio of striatal IBZM uptake to uptake in frontal cortex (ST/FC ratio) represents a semiquantitative measure of D2 receptor binding in the striatum. Our study sample included six patients treated with haloperidol (3.0-8.0 mg/day orally; one patient with an average of 0.9 mg/day intramuscularly), five patients with benperidol (9.0-15.0 mg/day orally) and nine patients treated with clozapine (200.0-600.0 mg/day orally). Typical neuroleptics (TNs) and atypical neuroleptics (ANs) were significantly di…

AdultMalemedicine.medical_specialtyBipolar DisorderPyrrolidinesNeuroscience (miscellaneous)Benperidolchemistry.chemical_compoundIodobenzamideBasal Ganglia DiseasesDopamineInternal medicineDopamine receptor D2medicineHaloperidolHumansRadiology Nuclear Medicine and imagingChlorpromazineClozapineClozapineAgedNeurologic ExaminationPsychiatric Status Rating ScalesTomography Emission-Computed Single-PhotonDepressive Disorder MajorSchizophrenia ParanoidDose-Response Relationship DrugReceptors Dopamine D2business.industryBenperidolBrainMiddle AgedCorpus StriatumFrontal LobePsychiatry and Mental healthEndocrinologychemistryDopamine receptorBenzamidesDopamine AntagonistsHaloperidolFemalebusinessAntipsychotic Agentsmedicine.drugPsychiatry Research: Neuroimaging
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Baseline [18F]-FDOPA kinetics are predictive of haloperidol-induced changes in dopamine turnover and cognitive performance: A positron emission tomog…

2007

The telencephalic dopamine innervations contribute to the modulation of cognitive processing. However, the relationship between cognitive effects of D(2/3)-receptor antagonism and dopamine transmission is not described in healthy subjects. We therefore tested effects of acute haloperidol (5 mg/d over 3 days) on continuous performance task (CPT) performance and 6-[(18)F]-fluoro-l-DOPA (FDOPA) PET parameters. Nine physically and mentally healthy male men performed two FDOPA-PET scans including arterial plasma withdrawal. Over 3 days before the second scan, all subjects were treated with 5 mg/d haloperidol orally. Using our novel steady-state analysis, we calculated the intrinsic rate of the c…

AdultMalemedicine.medical_specialtyCognitive NeuroscienceDopamineKineticsStriatumNeuropsychological TestsCognitionDopamineContinuous performance taskFluorodeoxyglucose F18Predictive Value of TestsInternal medicinemedicineHaloperidolImage Processing Computer-AssistedHumansEffects of sleep deprivation on cognitive performancePsychiatryBrain Chemistrymedicine.diagnostic_testHealthy subjectsReceptors Dopamine D3BrainMiddle AgedDopamine D2 Receptor AntagonistsEndocrinologyNeurologyPositron emission tomographyData Interpretation StatisticalPositron-Emission TomographyDopamine AntagonistsHaloperidolFemaleRadiopharmaceuticalsPsychologyAlgorithmsPsychomotor Performancemedicine.drugNeuroImage
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Striatal and extrastriatal D2/D3-receptor-binding properties of ziprasidone: a positron emission tomography study with [18F]Fallypride and [11C]raclo…

2008

To elucidate the Batypicality( of ziprasidone, its striatal and extrastriatal D2/D3-receptor binding was characterized in patients with schizophrenia under steady-state conditions. These data were compared with striatal receptor occupancy values after single-dose ziprasidone ingestion in healthy controls. ( 18 F)fallypride positron emission tomography (PET) recordings were obtained in 15 patients under steady-state ziprasidone treatment at varying time points after the last dose. Binding potentials were calculated for striatal and extrastriatal regions. D2/D3-receptor occupancies were expressed relative to binding potentials in 8 unmedicated patients. In a parallel ( 11 C)raclopride-PET stu…

AdultMalemedicine.medical_specialtyFluorine RadioisotopesPyrrolidinesTime Factorsmedicine.drug_classAtypical antipsychoticPharmacologyBinding CompetitiveBasal GangliaPiperazinesYoung AdultDopamine receptor D3Internal medicinemedicineHaloperidolHumansPharmacology (medical)ZiprasidoneCarbon RadioisotopesTemporal cortexRacloprideDose-Response Relationship DrugChemistryReceptors Dopamine D2Dopamine antagonistReceptors Dopamine D3Psychiatry and Mental healthThiazolesEndocrinologyFallyprideRaclopridePositron-Emission TomographyBenzamidesSchizophreniaDopamine AntagonistsFemaleRadiopharmaceuticalsmedicine.drugAntipsychotic AgentsJournal of clinical psychopharmacology
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Stratified Care vs Step Care Strategies for Migraine

2000

ContextVarious guidelines recommend different strategies for selecting and sequencing acute treatments for migraine. In step care, treatment is escalated after first-line medications fail. In stratified care, initial treatment is based on measurement of the severity of illness or other factors. These strategies for migraine have not been rigorously evaluated.ObjectiveTo compare the clinical benefits of 3 strategies: stratified care, step care within attacks, and step care across attacks, among patients with migraine.Design and SettingRandomized, controlled, parallel-group clinical trial conducted by the Disability in Strategies Study group from December 1997 to March 1999 in 88 clinical cen…

AdultMalemedicine.medical_specialtyMetoclopramideMigraine DisordersPopulationZolmitriptanSeverity of Illness IndexDrug Administration Schedulelaw.inventionRandomized controlled triallawInternal medicineSeverity of illnessHumansMedicineeducationOxazolidinonesAspirineducation.field_of_studyAspirinbusiness.industryAnti-Inflammatory Agents Non-SteroidalArea under the curveGeneral MedicineMiddle Agedmedicine.diseaseTryptaminesSerotonin Receptor AgonistsClinical trialMigraineCritical PathwaysPhysical therapyDopamine AntagonistsFemalebusinessmedicine.drugJAMA
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Prolactin plasma levels and D2-dopamine receptor occupancy measured with IBZM-SPECT

1996

By the application of 123([123I]IBZM), an iodine-labelled dopamine D2-receptor antagonist, brain D2 receptors in humans can be visualized with single photon emission computed tomography (SPECT). The ratio of IBZM binding to striatal regions versus binding to frontal cortex (ST/FC ratio) provided a semiquantitative measurement of D2 receptor binding in the striatum. This study investigated the relationship between receptor occupancy and plasma prolactin levels in 12 male patients treated with haloperidol, benperidol or clozapine. Prolactin levels were positively correlated with D2 receptor occupancy, reflecting at least in part a comparable dopamine receptor antagonism in different dopaminer…

AdultMalemedicine.medical_specialtyPyrrolidinesStriatumIodine RadioisotopesBenperidolProsencephalonDopamineDopamine receptor D2Internal medicinemedicineHumansReceptorClozapineTomography Emission-Computed Single-PhotonPharmacologySchizophrenia ParanoidReceptors Dopamine D2ChemistryBenperidolMiddle AgedCorpus StriatumProlactinProlactinEndocrinologymedicine.anatomical_structureDopamine receptorDopaminergic pathwaysBenzamidesDopamine AntagonistsHaloperidolAntipsychotic Agentsmedicine.drugPsychopharmacology
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In vitro P-glycoprotein efflux inhibition by atypical antipsychotics is in vivo nicely reflected by pharmacodynamic but less by pharmacokinetic chang…

2011

Abstract Background P-glycoprotein (P-gp), an efflux transporter of the blood–brain barrier, limits the access of multiple xenobiotics to the central nervous system (CNS). Thus drug-dependent inhibition, induction or genetic variation of P-gp impacts drug therapy. Methods We investigated atypical antipsychotics and their interaction with P-gp. Amisulpride, clozapine, N-desmethylclozapine, olanzapine, and quetiapine were assessed in vitro on their inhibitory potential and in vivo on their disposition in mouse serum and brain, and behaviourally on the RotaRod test. In vivo wildtype (WT) and mdr1a/1b double knockout mice (mdr1a/1b (−/−, −/−); KO) were investigated. Results In rhodamine 123 eff…

Clinical BiochemistryIn Vitro TechniquesPharmacologyToxicologyBlood–brain barrierBiochemistryRhodamine 123Rotarod performance testMiceBehavioral Neurosciencechemistry.chemical_compoundPharmacokineticsIn vivoCell Line TumormedicineAnimalsRhodamine 123ATP Binding Cassette Transporter Subfamily B Member 1Biological PsychiatryClozapineP-glycoproteinMice KnockoutPharmacologybiologyReceptors Dopamine D2Protein Transportmedicine.anatomical_structurechemistryRotarod Performance Testbiology.proteinDopamine AntagonistsEffluxAntipsychotic Agentsmedicine.drugPharmacology Biochemistry and Behavior
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Preclinical evidence of new opioid modulators for the treatment of addiction.

2010

Addiction to opiates is one of the most severe forms of substance dependence, and despite a variety of pharmacological approaches to treat it, relapse is observed in a high percentage of subjects. New pharmacological compounds are necessary to improve the outcome of treatments and reduce adverse side effects. Moreover, drugs that act on the opioid system can also be of benefit in the treatment of alcohol or cocaine addiction. AREA COVERED BY THIS REVIEW: Recent preclinical studies of pharmacological agents for the treatment of opiate addiction (2008 to the present date).The reader will be informed of the latest drugs shown in animal models to modify dependence on opiates and the reinforcing…

DrugGABA Agentsmedia_common.quotation_subjectNarcotic AntagonistsDrug Evaluation PreclinicalReceptors Opioid muPharmacologyReceptors NicotinicBioinformaticsPharmacotherapyDopamineReceptors Opioid deltaCannabinoid Receptor ModulatorsmedicineAdrenergic alpha-2 Receptor AgonistsAnimalsPharmacology (medical)Adverse effectmedia_commonPharmacologySubstance dependencebusiness.industryAddictionReceptors Opioid kappaAntagonistGeneral Medicinemedicine.diseaseOpioid-Related DisordersRatsSubstance Withdrawal SyndromeOpioidReceptors OpioidDopamine AntagonistsFemalebusinessExcitatory Amino Acid Antagonistsmedicine.drugExpert opinion on investigational drugs
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Diagnosis and therapeutic management of primary headache in an emergency setting

2013

Introduction and aim: Much headachers are under or mis-diagnoses and data regarding the proportion of patients attending an emergency department (ED) because of headache are still few. We conducted a retrospective observational study in an ED with the following aims: (a) estimate the proportion of headache attending to an ED (b) to estimate and describe the therapeutic management of primary headache and (c) to assessment the exam most frequently requested. Materials and methods: We collected data regarding patients diagnosed with headache consecutively attending the ED of the University of Palermo between September 2011 and March 2012. The study was approved by the ethics committee. Results: Between the semester evaluated 25110 subjects were admitted to ED headache suffers were equal to 1.6 %. Of these 263 (63.1 %) were woman and 154 (36.9 %). Mean age was 44.2 (DS ± 18.4) years (p = 0.068).According to ED registry headache admission was as follow assigned: 76.5 % with a diagnosis of headache 22.8 % with a secondary headache 0.7 % with Trigeminal Autonomic Cephalgias (TACs). Among those with a primary headache about 36 % of patient did not received a pharmacological treatment. Monotherapy was prescribed less frequently than combination therapy (19.1 vs 44.5 %).In monotherapy the most frequent medication were NSAIDs (28.3 %) benzodiazepines (26.7 %) and dopamine antagonists (11.7 %). Among those with a primary headache a CT scan was performed in the 124 subjects and 111 (34.8 %) had a neurologist consultation. Discussion: Our data are in line with the one previously reported in literature. The most frequently medication in the Italian ED were NSAIDs benzodiazepines dopamine antagonists and steroids. Neverless our data unlikely can be compared to other study give a snapshot. We believe that much more can be done to improve treatment of primary headache in ED.Settore MED/26 - Neurologia
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Anti-anhedonic actions of the novel serotonergic agent flibanserin, a potential rapidly-acting antidepressant

1998

Chronic exposure to mild unpredictable stress has previously been found to depress the consumption of palatable sweet solutions and to block the formation of conditioned place preferences; these effects are reversed by chronic treatment with tricyclic or atypical antidepressant drugs. The present study was designed to evaluate the antidepressant-like activity in this model of flibaserin (BIMT-17), a novel serotonergic agent with 5-HT1A receptor agonist and 5-HT2 receptor antagonist properties. Two experiments were conducted, using rats (experiment 1) and mice (experiment 2). In experiment 1, decreases in sucrose intake were seen in rats exposed to chronic mild stress, but the effect was unr…

MaleAgonistSucrosemedicine.medical_specialtyQuinpirolemedicine.drug_classMotor ActivityMiceSerotonin AgentsQuinpiroleDopamine receptor D3Dopamine receptor D2Internal medicineSalicylamidesmedicineAnimalsRats WistarPharmacologyRacloprideFluoxetinebusiness.industryBody WeightFeeding BehaviorConditioned place preferenceRatsEndocrinologyRacloprideAntidepressive Agents Second-GenerationConditioning OperantDopamine AntagonistsFlibanserinBenzimidazolesbusinessStress Psychologicalmedicine.drugEuropean Journal of Pharmacology
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