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Supersensitization of intrastriatal dopamine receptors involved in opposite regulation of acetylcholine release in Parkinson's model rats.

Using striatal microdialysis, we studied effects of SKF 38393, a D1 agonist, and quinpirole, a D2 agonist, on the acetylcholine (ACh) release from the striatum of 6-hydroxydopamine (6-OHDA)-lesioned rats by local infusion into the striatum. The present experiments clearly demonstrated evidence for the existence of intrastriatal D1 and D2 receptors regulating ACh release and for supersensitization of the striatal stimulatory D1 and inhibitory D2 receptor mechanisms in 6-OHDA lesioned rats.

Thioridazine for schizophrenia.

BACKGROUND: Thioridazine is an antipsychotic that can still be used for schizophrenia although it is associated with the cardiac arrhythmia, … obal state rating did not reveal any short-term difference between thioridazine and remoxipride and sulpiride (n=203, RR not improved or worse 1.00 CI 0.8 to 1.3). Limited data did not highlight differences in adverse event profiles. AUTHORS' CONCLUSIONS: Although there are shortcomings, there appears to be enough consistency over different outcomes and pe …

A randomized, double-blind, cross-over study comparing a levosulpiride-based and a metoclopramide-based combination in the prevention of ProMECE-CytaBOM-induced emesis.

BACKGROUND: To test two different antiemetic regimens for preventing nausea and vomiting in patient with non-Hodgkin's lymphoma (NHL) undergoing systemic chemotherapy (CT) with ProMECE-CytaBOM (P-C). PATIENTS AND METHODS: Twenty consecutive untreated adult outpatients with histologically confirmed NHL and scheduled to receive P-C chemotherapy were registered in a randomized, double-blind, cross-over study to compare the antiemetic efficacy of a levosulpiride (LS)-based and metoclopramide (MTC)-based regimen. RESULTS: Complete protection from vomiting was recorded in 93% (62/67) of courses wi…

Levosulpiride and cisapride in the treatment of dysmotility-like functional dyspepsia: a randomized, double-masked trial.

BACKGROUND & AIMS: Levosulpiride is a benzamide derivate D(2) dopamine antagonist with prokinetic activity that can accelerate gastric emptying and reduce discomfort in response to gastric distention. The aim of the study is to compare the clinical efficacy of levosulpiride and cisapride in patients with dysmotility-like functional dyspepsia. METHODS: In a exploratory pilot study performed as a multicenter, randomized, double-masked trial, the effects of 8 weeks of treatment with either levosulpiride, 25 mg, 3 times daily (n = 69) or cisapride, 10 mg, 3 times daily (n = 71) were compared. Ind…

The temporal evolution of striatal dopamine receptor binding and mRNA expression following hypoxia-ischemia in the neonatal rat.

Neonatal hypoxic-ischemic (HI) brain injury in the rat alters dopamine receptors. To determine whether such changes are permanent, dopamine receptors and corresponding mRNA were examined at various time points after neonatal HI using receptor autoradiography and in situ hybridization. Rat pups underwent ligation of the left common carotid artery followed by hypoxic exposure (8.5% O2 for 3 h). Controls underwent sham surgery alone. Animals surviving for 2-80 days following HI were studied. Striatal D1 receptors (labeled by [3H]SCH23390) were reduced as early as 2 days following HI, remained dep

White-matter microstructure in previously drug-naive patients with schizophrenia after 6 weeks of treatment.

BACKGROUND: It is not clear whether the progressive changes in brain microstructural deficits documented in previous longitudinal magnetic resonance imaging (MRI) studies might be due to the disease process or to other factors such as medication. It is important to explore the longitudinal alterations in white-matter (WM) microstructure in antipsychotic-naive patients with first-episode schizophrenia during the very early phase of treatment when relatively 'free' from chronicity. METHOD: Thirty-five patients with first-episode schizophrenia and 22 healthy volunteers were recruited. High-resol

Switching antipsychotics: Imaging the differential effect on the topography of postsynaptic density transcripts in antipsychotic-naïve vs. antipsychotic-exposed rats.

The postsynaptic density (PSD) has been regarded as a functional switchboard at the crossroads of a dopamine-glutamate interaction, and it is putatively involved in the pathophysiology of psychosis. Indeed, it has been demonstrated that antipsychotics may modulate several PSD transcripts, such as PSD-95, Shank, and Homer. Despite switching antipsychotics is a frequent strategy to counteract lack of efficacy and/or side effect onset in clinical practice, no information is available on the effects of sequential treatments with different antipsychotics on PSD molecules. The aim of this study was

Clozapine-induced salivation: interaction with N-desmethylclozapine and amisulpride in an experimental rat model.

Many drugs (e.g. amisulpride) have been used to treat troublesome clozapine-induced salivation; however, varying success has been achieved in this respect, probably because, until recently, the salivatory action of clozapine has been largely unexplained. In the rat, clozapine and its main metabolite, N-desmethylclozapine, were found to exert mixed secretory actions: excitatory, through muscarinic acetylcholine M1-receptors giving rise to a long-lasting, low-level flow of saliva; and inhibitory, through muscarinic M3-receptors and α(1) -adrenoceptors reducing the parasympathetically and sympath

Profound changes in dopaminergic neurotransmission in the prefrontal cortex in response to flattening of the diurnal glucocorticoid rhythm: implications for bipolar disorder.

Patients with bipolar disorder have abnormalities in glucocorticoid secretion, dopaminergic neurotransmission, and prefrontal cortical function. We hypothesized that the flattening of the diurnal glucocorticoid rhythm, commonly seen in bipolar disorder, modulates dopaminergic neurotransmission in the prefrontal cortex (PFC) leading to abnormalities in prefrontally mediated neurocognitive functions. To address this hypothesis, we investigated the effects of a flattened glucocorticoid rhythm on (i) the release of dopamine in the PFC and (ii) the transcription of genes in the ventral tegmental ar

Bidirectional regulation of dopamine D2 and neurotensin NTS1 receptors in dopamine neurons.

Several lines of evidence suggest a close association between dopamine (DA) and neurotensin (NT) systems in the CNS. Indeed, in the rodent brain, abundant NT-containing fibres are found in DA-rich areas such as the ventral tegmental area and substantia nigra. Moreover, it has been shown in vivo that NT, acting through its high-affinity receptor (NTS1), reduces the physiological and behavioural effects of DA D2 receptor (D2R) activation, a critical autoreceptor feedback system regulating DA neurotransmission. However, the mechanism of this interaction is still elusive. The aim of our study was

Alternatives to estrogen.

For many years, women have sought alternative therapies for menopausal symptoms and for general health overall. The highly publicized findings from the Women's Health Initiative have led to an increased pressure on the medical community to find safe and alternative medications for female health. This article reviews the challenges and problems with the use of alternative medicines, and the clinical trials that prove their efficacy, and discusses the safety issues that may occur with these types of products.

Extracorporeal membrane oxygenation as bridge-to-decision in acute heart failure due to systemic light-chain amyloidosis.

PatientFemale, 58.Final diagnosisAcute hear failure.SymptomsDispnoea • edema • fatigue.Medication—Clinical procedureBone marrow biopsy • endomyocardial biopsy • abdominal subcutaneous fat biopsy under ECMO support.SpecialtyCardiology.ObjectiveRare disease.BackgroundCardiac amyloidosis results from the amyloid deposition in heart tissue, either in the context of a systemic disease or as a localized form. Several pro-amyloid proteins can produce amyloid deposits in the heart. Each of these amyloidoses has characteristic clinical (cardiac and extracardiac) features, and a specific diagnosis and t

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… Medication included ramipril and sulpiride. There were no known drug allergies. The patient was a single housewife without children. She did not smoke and rarely drank alcohol. There was no family history of cardiac disease. On physical examination the patient was not in distress. …

BMP inhibition by DAN in Hensen's node is a critical step for the establishment of left-right asymmetry in the chick embryo.

During left-right (L-R) axis formation, Nodal is expressed in the node and has a central role in the transfer of L-R information in the vertebrate embryo. Bone morphogenetic protein (BMP) signaling also has an important role for maintenance of gene expression around the node. Several members of the Cerberus/Dan family act on L-R patterning by regulating activity of the transforming growth factor-β (TGF-β) family. We demonstrate here that chicken Dan plays a critical role in L-R axis formation. Chicken Dan is expressed in the left side of the node shortly after left-handed Shh expression and be

Comparison of the Utility of Amplitude-Spectral and Coherence Features of Psychotropic Drugs' Action on ECoG Signal for Pharmaco-EEG Based Drug Screening in Rats.

A naive Bayesian classifier (NBC) combined with principal component analysis (PCA) effectively differentiates the dose-dependent effects of … f 12 pharmacological agents: the NMDA antagonist dizocilpine, the D2/D3 antagonists haloperidol and sulpiride, the M-anticholinergic tropicamide, the H1/5HT2A receptor blocker hydroxyzine, the acetylcholinesterase inhibitor galantamine, the alpha-2 adrenergic agonist dexmedetomidine, the alpha-2 adrenergic antagonist atipamezole, the adenosine receptor bloc …

Antipsychotics with inverse agonist activity at the dopamine D3 receptor.

In NG 108-15 cells expressing the recombinant human D3 receptor, dopamine agonists enhance [3H]thymidine incorporation and decrease cAMP accumulation. In these cells, but not in wild type cells, haloperidol, fluphenazine, and various other antipsychotics inhibited basal [3H]thymidine incorporation in a concentration-dependent manner. In contrast, other dopamine antagonists such as nafadotride or (+)AJ 76, two D3-preferring antagonists, were without effect. The concentration-response curve of haloperidol was shifted to the right in presence of nafadotride, with a potency compatible with its nan

[Investigation on the status of monotherapy for newly diagnosed tic disorders and its comorbidity in children].

Objective: To investigate the status of monotherapy for newly diagnosed tic disorders and its comorbidity in children, so as to provide a re … c disorders, mild chronic tic disorders and severe TS were all aripiprazole, tiapride, haloperidol, sulpiride, clonidine and topiramate. While clonidine, aripiprazole, tiapride could be considered as preferred drugs for severe transient tic disorders, moderate to severe chronic tic disorders and mild to moderate tic disorders. In the investigation of monoth …

Secretion of brain-derived neurotrophic factor from PC12 cells in response to oxidative stress requires autocrine dopamine signaling.

Expression of brain-derived neurotrophic factor (BDNF) is sensitive to changes in oxygen availability, suggesting that BDNF may be involved in adaptive responses to oxidative stress. However, it is unknown whether or not oxidative stress actually increases availability of BDNF by stimulating BDNF secretion. To approach this issue we examined BDNF release from PC12 cells, a well-established model of neurosecretion, in response to hypoxic stimuli. BDNF secretion from neuronally differentiated PC12 cells was strongly stimulated by exposure to intermittent hypoxia (IH). This response was inhibited

Prenatal and neonatal exposure to bisphenol-A enhances the central dopamine D1 receptor-mediated action in mice: enhancement of the methamphetamine-induced abuse state.

Bisphenol-A (BPA), one of the most common environmental endocrine disrupters, has been extensively evaluated for toxicity in a variety of tests in rodents, including developmental and reproductive toxicity, and carcinogenicity. However, little is known about its action on the CNS. In this report, we show that prenatal and neonatal exposure to BPA in mice leads to the enhancement of the dopamine D1 receptor-dependent rewarding effect induced by a psychostimulant methamphetamine. Furthermore, this treatment with BPA markedly enhanced hyperlocomotion and its sensitization induced by methamphetami

Карвацоль Ойл как нейропоохранный агент: обзор дизайна исследований и последних достижений.

Нейродегенеративные заболевания в основном воспринимаются как болезни стареющего населения, однако сегодня в день эти заболевания представляют угрозу для населения всех возрастных групп, несмотря на значительное улучшение качества жизни. Согласно сообщениям, почти все основные масла (ЭО) обладают определенными нейрозащитными способностями и на протяжении столетий использовались в качестве добавок к хорошему психическому здоровью. Этот обзор свидетельствует о терапевтическом потенциале одного такого монотерпенового фенола, карвакрула (CV), который может быть использован в качестве основного тер

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… effect. 3 | [ 53 ] | Solution | 12.5, 25, and 50 mg/ kg | <1 | Male Swiss Mice | PO | Behavioural tests (forced swimming test and tail suspension test) | The anti-mobility activity of CV in the forced swimming and tail suspension tests was completely blocked off by pre-treatment of mice with SCH23390 or sulpiride … These findings suggested that the antidepressant activity of CV is somehow dependent on the dopaminergic system that was blocked by sulpiride in the mice model. 4 | [ 54 ] | Solution | 20, 30, and 40 mg/kg | 21 | Albino Wistar Rats | IP | Corticosterone evaluation Measurement of lipid peroxidation Estimation …

Selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs) for the prevention of tension-type headache in adults.

BACKGROUND: This is an updated version of the Cochrane review published in 2005 on selective serotonin re-uptake inhibitors (SSRIs) for prev … evious version of this review, compared SSRIs to other antidepressants (amitriptyline, desipramine, sulpiride, mianserin). Most of the included studies had methodological and/or reporting shortcomings and lacked adequate power. Follow-up ranged between two and four months.Six studies explored the effect of SSRIs or SNRIs on tension-type headache frequency, …