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https://www.readbyqxmd.com/read/28916501/awakenings-in-rats-by-ultrasounds-a-new-animal-model-for-paradoxical-kinesia
#1
Luan Castro Tonelli, Markus Wöhr, Rainer Schwarting, Liana Melo-Thomas
Paradoxical kinesia refers to a sudden transient ability of akinetic patients to perform motor tasks they are otherwise unable to perform. The mechanisms underlying this phenomenon are unknown due a paucity of valid animal models that faithfully reproduce paradoxical kinesia. Here, in a first experiment, we present a new method to study paradoxical kinesia by "awakening" cataleptic rats through presenting appetitive 50-kHz ultrasonic vocalizations (USV), which are typical for social situations with positive valence, like juvenile play or sexual encounters ("rat laughter")...
September 12, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28916137/oxytocin-induces-penile-erection-and-yawning-when-injected-into-the-bed-nucleus-of-the-stria-terminalis-involvement-of-glutamic-acid-dopamine-and-nitric-oxide
#2
Fabrizio Sanna, Jessica Bratzu, Antonio Argiolas, Maria Rosaria Melis
Oxytocin (5-100ng), but not Arg(8)-vasopressin (100ng), injected unilaterally into the bed nucleus of the stria terminalis (BNST) induces penile erection and yawning in a dose-dependent manner in male rats. The minimal effective dose was 20ng for penile erection and 5ng for yawning. Oxytocin responses were abolished not only by the oxytocin receptor antagonist d(CH2)5Tyr(Me)(2)-Orn(8)-vasotocin (1μg), but also by (+) MK-801 (1μg), an excitatory amino acid receptor antagonist of the N-methyl-d-aspartic acid (NMDA) subtype, SCH 23390 (1μg), a D1 receptor antagonist, but not haloperidol (1μg), a D2 receptor antagonist, and SMTC (40μg), an inhibitor of neuronal nitric oxide synthase, injected into the BNST 15min before oxytocin...
September 12, 2017: Hormones and Behavior
https://www.readbyqxmd.com/read/28914976/haloperidol-versus-5-ht3-receptor-antagonists-for-postoperative-vomiting-and-qtc-prolongation-a-noninferiority-meta-analysis-and-trial-sequential-analysis-of-randomized-controlled-trials
#3
REVIEW
Preet Mohinder Singh, Anuradha Borle, Jeetinder Kaur Makkar, Anjan Trikha, David Fish, Ashish Sinha
Haloperidol is an antipsychotic with well-known antiemetic potential. It is underutilized for postoperative nausea vomiting due to reported corrected QT interval (QTc) prolongation. This meta-analysis evaluates its safety and efficacy as an antiemetic in the perioperative period. Trials comparing haloperidol to 5-HT3 -receptor antagonists (5-HT3 -RA) for 24 postoperative vomiting incidences published up to May 2017 were searched in the medical database. Comparisons were made for antiemetic efficiency variables (vomiting incidence, rescue antiemetic need, and patients with complete response) during early (until 6 hours) and late postoperative phases...
September 15, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28912551/the-antipsychotic-drugs-olanzapine-and-haloperidol-modify-network-connectivity-and-spontaneous-activity-of-neural-networks-in-vitro
#4
Egor Dzyubenko, Georg Juckel, Andreas Faissner
Impaired neural synchronization is a hallmark of psychotic conditions such as schizophrenia. It has been proposed that schizophrenia-related cognitive deficits are caused by an unbalance of reciprocal inhibitory and stimulatory signaling. This supposedly leads to decreased power of induced gamma oscillations during the performance of cognitive tasks. In light of this hypothesis an efficient antipsychotic treatment should modify the connectivity and synchronization of local neural circuits. To address this issue, we investigated a model of hippocampal neuronal networks in vitro...
September 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28905207/role-of-vasopressin-v1a-receptor-in-%C3%A2-9-tetrahydrocannabinol-induced-cataleptic-immobilization-in-mice
#5
Nobuaki Egashira, Emi Koushi, Takayuki Myose, Akito Tanoue, Kenichi Mishima, Ryota Tsuchihashi, Junei Kinjo, Hiroyuki Tanaka, Satoshi Morimoto, Katsunori Iwasaki
RATIONALE: Cannabis is a widely used illicit substance. ∆(9)-tetrahydrocannabinol (THC), the major psychoactive component of cannabis, is known to cause catalepsy in rodents. Recent studies have shown that vasopressin V1a and V1b receptors are widely distributed in the central nervous system and are capable of influencing a wide variety of brain functions such as social behavior, emotionality, and learning and memory. OBJECTIVES: The present study was designed to examine the possible involvement of V1a and V1b receptors in THC-induced catalepsy-like immobilization...
September 14, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28904993/abnormalities-of-signal-transduction-networks-in-chronic-schizophrenia
#6
Jennifer L McGuire, Erica A Depasquale, Adam J Funk, Sinead M O'Donnovan, Kathryn Hasselfeld, Shruti Marwaha, John H Hammond, Vahram Hartounian, James H Meador-Woodruff, Jarek Meller, Robert E McCullumsmith
Schizophrenia is a serious neuropsychiatric disorder characterized by disruptions of brain cell metabolism, microstructure, and neurotransmission. All of these processes require coordination of multiple kinase-mediated signaling events. We hypothesize that imbalances in kinase activity propagate through an interconnected network of intracellular signaling with potential to simultaneously contribute to many or all of the observed deficits in schizophrenia. We established a workflow distinguishing schizophrenia-altered kinases in anterior cingulate cortex using a previously published kinome array data set...
2017: NPJ Schizophrenia
https://www.readbyqxmd.com/read/28902994/discovery-structure-activity-relationship-and-anti-parkinsonian-effect-of-a-potent-and-brain-penetrant-chemical-series-of-positive-allosteric-modulators-of-metabotropic-glutamate-receptor-4
#7
Delphine Charvin, Vincent Pomel, Millan Ortiz, Mélanie Frauli, Sophie Scheffler, Edith Steinberg, Luc Baron, Laurène Deshons, Rachel Rudigier, Delphine Thiarc, Christophe Morice, Baptiste Manteau, Stanislas Mayer, Danielle Graham, Bruno Giethlen, Nadia Brugger, Gaël Hedou, François Conquet, Stephan Schann
The metabotropic glutamate receptor 4 (mGluR4) is an emerging target for the treatment of Parkinson's disease (PD). However, since the discovery of its therapeutic potential, no ligand has been successfully developed enough to be tested in the clinic. In the present paper, we report for the first time the medicinal chemistry efforts conducted around the pharmacological tool (-)-PHCCC. This work led to the identification of compound 40, a potent and selective mGluR4 positive allosteric modulator (PAM) with good water solubility and demonstrating consistent activity across validated preclinical rodent models of PD motor symptoms, after intraperitoneal administration: haloperidol-induced catalepsy in mouse and the rat 6-hydroxydopamine (6-OHDA) lesion model...
September 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28900113/abnormalities-of-signal-transduction-networks-in-chronic-schizophrenia
#8
Jennifer L McGuire, Erica A Depasquale, Adam J Funk, Sinead M O'Donnovan, Kathryn Hasselfeld, Shruti Marwaha, John H Hammond, Vahram Hartounian, James H Meador-Woodruff, Jarek Meller, Robert E McCullumsmith
Schizophrenia is a serious neuropsychiatric disorder characterized by disruptions of brain cell metabolism, microstructure, and neurotransmission. All of these processes require coordination of multiple kinase-mediated signaling events. We hypothesize that imbalances in kinase activity propagate through an interconnected network of intracellular signaling with potential to simultaneously contribute to many or all of the observed deficits in schizophrenia. We established a workflow distinguishing schizophrenia-altered kinases in anterior cingulate cortex using a previously published kinome array data set...
September 12, 2017: NPJ Schizophrenia
https://www.readbyqxmd.com/read/28899760/chronic-atypical-antipsychotics-but-not-haloperidol-increase-neurogenesis-in-the-hippocampus-of-adult-mouse
#9
Koji Chikama, Hidetaka Yamada, Tatsuo Tsukamoto, Kosuke Kajitani, Yusaku Nakabeppu, Naohisa Uchimura
It is suggested that altered neuroplasticity contributes to the pathophysiology of schizophrenia and antipsychotics may exhibit some of their therapeutic efficacies by improving neurogenesis and/or proliferation of neural progenitors. The aim of this study is to investigate whether chronic antipsychotics treatment affect neurogenesis in adult mouse hippocampus. Animals were administered olanzapine, quetiapine, clozapine, risperidone, aripiprazole, or haloperidol via the osmotic minipump for 21 days and then injected with 5-bromo-2'-deoxyuridine (BrdU) to label mitotic cells...
September 9, 2017: Brain Research
https://www.readbyqxmd.com/read/28895028/prevalence-of-qt-interval-prolonging-drug-drug-interactions-qt-ddis-in-psychiatry-wards-of-tertiary-care-hospitals-in-pakistan-a-multicenter-cross-sectional-study
#10
Qasim Khan, Mohammad Ismail, Iqbal Haider, Fahadullah Khan
Background QT prolongation and associated arrhythmias, torsades de pointes (TdP), are considerable negative outcomes of many antipsychotic and antidepressant agents frequently used by psychiatric patients. Objective To identify the prevalence, levels, and predictors of QT prolonging drug-drug interactions (QT-DDIs), and AZCERT (Arizona Center for Education and Research on Therapeutics) classification of drugs involved in QT-DDIs. Setting Psychiatry wards of three major tertiary care hospitals of Khyber-Pakhtunkhwa, Pakistan...
September 12, 2017: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/28890266/in-line-coupling-of-supported-liquid-membrane-extraction-to-capillary-electrophoresis-for-simultaneous-analysis-of-basic-and-acidic-drugs-in-urine
#11
Pavla Pantůčková, Pavel Kubáň
Simultaneous extraction of basic and acidic drugs across thin supported liquid membrane (SLM) and direct injection of the extracted drugs from SLM surface into capillary electrophoresis (CE) were demonstrated. A microextraction device compatible with injection system of commercial CE instrument was filled with 20μL of sample and 10μL of acceptor solution, which were interspaced by the SLM impregnated with 5μL of organic solvent. Extractions of three basic drugs (nortriptyline, haloperidol and loperamide) and two acidic drugs (ketoprofen and naproxen) were achieved at optimized conditions including 1-ethyl-2-nitrobenzene as SLM solvent, natural pH of sample solution, 2...
September 7, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28886082/haloperidol-induces-pharmacoepigenetic-response-by-modulating-mirna-expression-global-dna-methylation-and-expression-profiles-of-methylation-maintenance-genes-and-genes-involved-in-neurotransmission-in-neuronal-cells
#12
Babu Swathy, Moinak Banerjee
INTRODUCTION: Haloperidol has been extensively used in various psychiatric conditions. It has also been reported to induce severe side effects. We aimed to evaluate whether haloperidol can influence host methylome, and if so what are the possible mechanisms for it in neuronal cells. Impact on host methylome and miRNAs can have wide spread alterations in gene expression, which might possibly help in understanding how haloperidol may impact treatment response or induce side effects. METHODS: SK-N-SH, a neuroblasoma cell line was treated with haloperidol at 10μm concentration for 24 hours and global DNA methylation was evaluated...
2017: PloS One
https://www.readbyqxmd.com/read/28881851/the-involvement-of-darpp-32-in-the-pathophysiology-of-schizophrenia
#13
REVIEW
Haitao Wang, Mohd Farhan, Jiangping Xu, Philip Lazarovici, Wenhua Zheng
Schizophrenia is one of the most devastating heterogeneous psychiatric disorders. The dopamine hypothesis is the longest standing pathoetiologic theory of schizophrenia based on neurochemical evidences of elevated brain striatal dopamine synthesis capacity and increased dopamine release in response to stress. Dopamine and cyclic AMP-regulated phosphoprotein of relative molecular mass 32,000 (DARPP-32) is a cytosolic protein highly enriched in the medium spiny neurons of the neostriatum, considered as the most important integrator between the cortical input and the basal ganglia, and associated with motor control...
August 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28876362/psychotropic-prescriptions-for-the-treatment-of-schizophrenia-in-an-outpatient-clinic
#14
Christopher Izehinosen Okpataku, David Tawani
Introduction: There is an unpredictable pattern in the prescription of antipsychotics and other psychotropic medications for the treatment of schizophrenia, particularly in resource-limited settings in developing countries. Objective: To determine the psychotropic prescriptions given to patients with schizophrenia in an outpatient clinic of a tertiary hospital and to describe the choices and trends of these prescriptions. Methods: This was a cross-sectional descriptive study of prescriptions for adults with schizophrenia...
August 31, 2017: Trends in Psychiatry and Psychotherapy
https://www.readbyqxmd.com/read/28869398/synthesis-and-evaluation-of-haloperidol-metabolite-ii-prodrugs-as-anticancer-agents
#15
Maria Dichiara, Emanuele Amata, Antonio Rescifina, Orazio Prezzavento, Giuseppe Floresta, Carmela Parenti, Valeria Pittalà, Agostino Marrazzo
The use of haloperidol metabolite II (HP-metabolite II) prodrugs is an emerging strategy in the treatment of cancer. HP-metabolite II exhibits antiproliferative properties at micromolar concentrations inducing apoptosis in different types of cancer. Thus, the application of the prodrug approach appears as a useful method leading to much more desirable pharmacokinetic and pharmacodynamic properties. Some studies have shown that the esterification of the hydroxyl group of HP-metabolite II with 4-phenylbutiric acid (4-PBA) or valproic acid enhances the anticancer therapeutic potency...
September 4, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28865447/multicenter-assessment-of-sedation-and-delirium-practices-in-the-intensive-care-units-in-poland-is-this-common-practice-in-eastern-europe
#16
Katarzyna Kotfis, Małgorzata Zegan-Barańska, Maciej Żukowski, Krzysztof Kusza, Mariusz Kaczmarczyk, E Wesley Ely
BACKGROUND: The majority of critically ill patients experience distress during their stay in the Intensive Care Unit (ICU), resulting from systemic illness, multiple interventions and environmental factors. Providing humane care should address concomitant treatment of pain, agitation and delirium. The use of sedation and approaches to ICU delirium should be monitored according to structured guidelines. However, it is unknown to what extent these concepts are followed in Eastern European countries like Poland...
September 2, 2017: BMC Anesthesiology
https://www.readbyqxmd.com/read/28857746/purinergic-regulation-of-brain-catecholamine-neurotransmission-in-vivo-electrophysiology-and-microdialysis-study-in-rats
#17
Eliyahu Dremencov, Lubica Lacinova, Gunnar Flik, Joost Ha Folgering, Thomas Ifh Cremers, Ben Hc Westerink
It was previously reported that adenosine-2A (A2A) receptors interact with dopamine-2 (D2) receptors on a molecular level. The aim of the current study was to investigate the functional output of this interaction. In vivo microdialysis was used to assess the effects of an antagonist of A2A receptors, ZM 241385, and an antagonist of D2 receptors haloperidol, either alone or in combination, on brain catecholamine levels. It was found that ZM 241385 did not alter catecholamine levels by its own, but potentiated haloperidol-induced dopamine and norepinephrine release in the nucleus accumbens and prefrontal cortex, respectively...
August 31, 2017: General Physiology and Biophysics
https://www.readbyqxmd.com/read/28852259/chlorpromazine-as-prophylaxis-for-bipolar-disorder-with-treatment-and-electroconvulsive-therapy-refractory-mania-old-horse-new-trick
#18
Tamonud Modak, Saurabh Kumar, Arghya Pal, Rishab Gupta, Raman Deep Pattanayak, Sudhir Kumar Khandelwal
A 22-year-old male diagnosed with bipolar affective disorder presented to us with a 3(rd) episode mania resistant to both olanzapine and haloperidol as well as electroconvulsive therapy. He, however, responded to chlorpromazine (CPZ) which was also effective as a mood stabilizer. The patient had a relapse of his illness when CPZ was stopped and responded again when it was started. The case demonstrates that CPZ may have a role in as both an anti-manic agent and for the maintenance for bipolar disorders. The possible underlying mechanism for this role is also discussed...
July 2017: Indian Journal of Psychological Medicine
https://www.readbyqxmd.com/read/28844183/attenuation-of-oxidative-damage-by-coenzyme-q10-loaded-nanoemulsion-via-oral-route-for-the-management-of-parkinson-s-disease
#19
Sanjula Baboota, Bijay Kumar Gupta, Shobhit Kumar, Harleen Kaur, Javed Ali
Coenzyme Q10 (CoQ10) is a well known antioxidant molecule which is used in the treatment of neurodegenerative disorders but due to poor solubility it suffers with the drawback of low oral bioavailability. The aim of present study was to prepare and characterize CoQ10 loaded nanoemulsion to improve the oral bioavailability. Prepared formulation was studied for droplet size, polydispersity index (PDI), percentage transmittance, refractive index, viscosity, zeta potential, surface morphology by transmission electron microscopy (TEM) and in vitro release study...
August 26, 2017: Rejuvenation Research
https://www.readbyqxmd.com/read/28843554/comprehensive-study-of-buffer-systems-and-local-ph-effects-in-electromembrane-extraction
#20
Magnus Saed Restan, Henrik Jensen, Xiantao Shen, Chuixiu Huang, Ørjan Grøttem Martinsen, Pavel Kubáň, Astrid Gjelstad, Stig Pedersen-Bjergaard
Different phosphate-, acetate- and formate buffers in the pH range 2.0-6.8 were tested for electromembrane extraction (EME) in a 96-well system. The five basic drugs haloperidol, loperamide, methadone, nortriptyline, and pethidine were selected as model analytes. The EME performance was tested with respect to extraction recovery, extraction current and pH-stability. The analytes were extracted from 200 μL buffer, through a 100 μm thick supported liquid membrane (SLM) of 2-nitrophenyl octyl ether (NPOE) immobilized in the pores of filters in a 96-well plate, and into 100 μL buffer acceptor phase...
September 1, 2017: Analytica Chimica Acta
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