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Haloperidol

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https://www.readbyqxmd.com/read/28336436/induction-of-dopamine-d1-and-d5-receptors-in-r28%C3%A2-cells-by-light-exposures
#1
Yan Ke, Wentao Li, Zhiqun Tan, Zhikuan Yang
Dopamine is known to play an important role in the pathophysiological process of myopia development relevant to the ambient lighting, but it is still poorly understood about how lighting regulates dopamine and its interaction with dopamine receptors to mediate the pathogenic signal transduction leading to alterations of ocular globe and the pathogenesis of myopia. Many studies have highlighted changes of ocular dopamine amount in response to different lighting conditions, but little attention has been paid to the dopamine receptors during these processes...
March 20, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28336342/pharmacological-assessments-of-potent-a2a-receptor-antagonist-idpu-1-7-imino-3-propyl-2-3-dihydrothiazolo-4-5-d-pyrimidin-6-7h-yl-urea-in-rodent-model-of-haloperidol-induced-parkinson-like-symptoms
#2
Namrata Kumari, Saurabh Agrawal, Pratibha Mehta Luthra
A2A receptor antagonists emerged as potential candidate for management of Parkinson's disease. Earlier we had reported the therapeutic potential of 1-(7-imino-3-propyl-2,3-dihydrothiazolo[4,5-d]pyrimidin-6(7H)-yl) urea (IDPU) as A2A receptor antagonist. Herein, we have investigated the effect of IDPU in attenuation of haloperidol induced Parkinson like symptoms in rats. It has successfully restored hypo-locomotion induced by haloperidol and NECA. IDPU also displayed protective effect against oxidative stress induced by chronic haloperidol treatment in rats...
March 20, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28333365/clozapine-combined-with-different-antipsychotic-drugs-for-treatment-resistant-schizophrenia
#3
REVIEW
Sarah Barber, Uwaila Olotu, Martina Corsi, Andrea Cipriani
BACKGROUND: Between 40% and 70% of people with treatment-resistant schizophrenia do not respond to clozapine, despite adequate blood levels. For these people, a number of treatment strategies have emerged, including the prescription of a second anti-psychotic drug in combination with clozapine. OBJECTIVES: To determine the clinical effects of various clozapine combination strategies with antipsychotic drugs in people with treatment-resistant schizophrenia both in terms of efficacy and tolerability...
March 23, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28329449/behavioural-and-neurochemical-effects-of-alpha-lipoic-acid-associated-with-omega-3-in-tardive-dyskinesia-induced-by-chronic-haloperidol-in-rats
#4
Dayane Pessoa Araújo, Thaisa Camboim, Ana Silva, Caio Fonseca, Rebeca Sousa, Mabson Barbosa, Lucidio Oliveira, José Cavalcanti, Eudes Lucena, Fausto Guzen
Tardive dyskinesia (TD) is characterized by involuntary movements of the lower portion of the face being related to typical antipsychotic therapy. TD is associated with the oxidative imbalance in the basal ganglia. Lipoic acid (LA) and omega 3 (ω-3) are antioxidants acting as enzyme cofactors, regenerating antioxidant enzymes. This study aimed to investigate behavioral and neurochemical effects of supplementation with of LA (100mg/Kg) and ω-3 (1g/Kg) in the treatment of TD-induced by chronic use haloperidol (HAL) (1mg/Kg) in rats...
March 22, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28326743/dopamine-receptors-modulate-t-lymphocytes-via-inhibition-of-camp-creb-signaling-pathway
#5
Yan Huang, Can-Can Chen, Ting-Ting Wang, Yi-Hua Qiu, Yu-Ping Peng
OBJECTIVES: We have previously reported that dopamine D2-like receptors including D2, D3 and D4 receptors are more important in mediating modulation of T cells than dopamine D1-like receptors (D1 and D5 receptors). Here we aimed to clarify the role of D2-like receptors in regulation of differentiation and function of T lymphocyte subsets, including helper T (Th)1, Th2, Th17 and regulatory T (Treg) cells. METHODS: Lymphocytes, separated from the mesenteric lymph nodes of mice, were stimulated with concanavalin A (Con A) and treated with the D2-like receptor agonist quinpirole or the antagonist haloperidol...
December 2016: Neuro Endocrinology Letters
https://www.readbyqxmd.com/read/28322938/visualization-of-protonation-deprotonation-of-active-pharmaceutical-ingredient-in-solid-state-by-vapor-phase-amine-selective-alkyne-tagging-and-raman-imaging
#6
Kei Moriyama, Yukiko Yasuhara, Hiromi Ota
Here we report a simple and direct method to visualize the protonation/deprotonation of an amine API in the solid state using a solid-vapor reaction with propargyl bromide and Raman imaging for the assessment of the API during the manufacturing process of solid formulations. An alkyne tagging occurred on the free-form of solid haloperidol by the vapor phase reaction, and a distinct Raman signal of alkyne was detected. Alkyne signal monitoring by Raman imaging enabled us to visualize the distribution of the free-form haloperidol in a solid formulation...
March 16, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28322891/effect-of-antipsychotics-on-mitochondrial-bioenergetics-of-rat-ovarian-theca-cells
#7
Ekramy Elmorsy, Ayat Al-Ghafari, Amal Misbah Aggour, Soaad Mohamed Mosad, Raheela Khan, Saad Amer
BACKGROUND: Antipsychotics (APs) are widely prescribed drugs, which are well known to cause reproductive adverse effects through mechanisms yet to be determined. The purpose of this study was to investigate the effect of antipsychotics on mitochondrial bioenergetics of rat ovarian theca cells as a possible mechanism of reproductive toxicity. METHODS: Isolated rat's theca interstitial cells (TICs) were treated with two typical (chlorpromazine [CPZ] and haloperidol [HAL]) and two atypical APs (risperidone [RIS] and clozapine [CLZ])...
March 17, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28320545/haloperidol-undermining-gastroparesis-symptoms-hugs-in-the-emergency-department
#8
Rene Ramirez, Philip Stalcup, Brandon Croft, Michael A Darracq
BACKGROUND: Gastroparesis associated nausea, vomiting & abdominal pain (GP N/V/AP) are common presentations to the emergency department (ED). Treatment is often limited to antiemetic, prokinetic, opioid, & nonopioid agents. Haloperidol (HP) has been shown to have analgesic & antiemetic properties. We sought to evaluate HP in the ED as an alternative treatment of GP N/V/AP. METHODS: Using an electronic medical record, 52 patients who presented to the ED w/GP N/V/AP secondary to diabetes mellitus and were treated w/HP were identified...
March 12, 2017: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/28320026/-alcohol-withdrawal-and-its-major-complications
#9
Klaus Junghanns, Tilman Wetterling
Delirium tremens is one of the most common complications of alcohol withdrawal. It is potentially lethal and therefore should be detected as early as possible and be monitored and treated intensively. The assessment of risk factors with the Luebeck Alcohol-Withdrawal Risk Scale short form (LARS-11) can help to predict the risk of severe withdrawal adequately. As delirium cannot be differentiated from Wernicke-Encephalopathy with sufficient certainty high parenteral doses of Vitamin B1 and Magnesium orally should be given in case of any severe withdrawal symptoms...
March 2017: Fortschritte der Neurologie-Psychiatrie
https://www.readbyqxmd.com/read/28320006/in-patients-receiving-palliative-care-risperidone-or-haloperidol-increased-delirium-symptoms-vs-placebo
#10
Justin Lee, Anne Holbrook
No abstract text is available yet for this article.
March 21, 2017: Annals of Internal Medicine
https://www.readbyqxmd.com/read/28318209/end-of-life-care-managing-common-symptoms
#11
REVIEW
Ross H Albert
Physicians should be proficient at managing symptoms as patients progress through the dying process. When possible, proactive regimens that prevent symptoms should be used, because it is generally easier to prevent than to treat an acute symptom. As swallowing function diminishes, medications are typically administered sublingually, transdermally, or via rectal suppository. Opiates are the medication of choice for the control of pain and dyspnea, which are common symptoms in the dying process. Delirium and agitation may be caused by reversible etiologies, which should be identified and treated when feasible...
March 15, 2017: American Family Physician
https://www.readbyqxmd.com/read/28316587/characterization-of-the-antinociceptive-mechanisms-of-khat-extract-catha-edulis-in-mice
#12
Elham A Afify, Huda M Alkreathy, Ahmed S Ali, Hassan A Alfaifi, Lateef M Khan
This study investigated the antinociceptive mechanisms of khat extract (100, 200, and 400 mg/kg, i.p.) in four pain models: two thermic (hot plate, tail-flick) and two chemical (acetic acid, formalin) models. Male mice were pretreated intraperitoneally (i.p.) with the opioid receptor blocker naloxone (5 mg/kg), the cholinergic antagonist atropine (2 mg/kg), the selective α1 blocker prazosin (1 mg/kg), the dopamine D2 antagonist haloperidol (1.5 mg/kg), or the GABAA receptor antagonist, bicuculline (1 mg/kg) 15 minutes prior to i...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28315150/radioiodination-and-preclinical-evaluation-of-4-benzyl-1-3-125-i-iodobenzylsulfonyl-piperidine-as-a-breast-tumor-imaging-tracer-in-mouse
#13
Masoud Sadeghzadeh, Behrouz Alirezapour, Ghorban Ali Charkhlooie, Maryam Keshavarz Baghery, Amir Khorouti
OBJECTIVE: 4-Benzyl-1-(3-iodobenzylsulfonyl)piperidine, 4-B-IBSP, has shown high-binding affinity to both sigma (σ) receptors in our previous work. In current study, radiolabeling and preclinical evaluation of 4-benzyl-1-(3-[(125)I]-iodobenzylsulfonyl)piperidine, 4-B-[(125)I]IBSP, in human ductal breast carcinoma (T47D) cells and in breast adenocarcinoma-bearing BALB/c mice are described. METHODS: Radioiodination of this new σ ligand was performed by a palladium-catalyzed stannylation approach followed by oxidative iododestannylation reaction using Iodo-Gen...
March 17, 2017: Annals of Nuclear Medicine
https://www.readbyqxmd.com/read/28314679/an-analysis-of-the-rewarding-and-aversive-associative-properties-of-nicotine-in-the-neonatal-quinpirole-model-effects-on-glial-cell-line-derived-neurotrophic-factor-gdnf
#14
Russell W Brown, Seth L Kirby, Adam R Denton, John M Dose, Elizabeth D Cummins, Wesley Drew Gill, Katherine C Burgess
This study analyzed the associative properties of nicotine in a conditioned place preference (CPP) paradigm in adolescent rats neonatally treated with quinpirole (NQ) or saline (NS). NQ produces dopamine D2 receptor supersensitivity that persists throughout the animal's lifetime, and therefore has relevance towards schizophrenia. In two experiments, rats were ip administered quinpirole (1mg/kg) or saline from postnatal day (P)1-21. After an initial preference test at P42-43, animals were conditioned for eight consecutive days with saline or nicotine (0...
March 14, 2017: Schizophrenia Research
https://www.readbyqxmd.com/read/28290080/a-retrospective-cohort-study-of-acute-kidney-injury-risk-associated-with-antipsychotics
#15
Yawen Jiang, Jeffrey S McCombs, Susie H Park
BACKGROUND: A recent large database analysis raised concerns of potential acute kidney injury (AKI) risk associated with antipsychotics. However, whether individual atypical and typical antipsychotics are associated with differential AKI risks has not been investigated. OBJECTIVE: The current study compared the risks of AKI and known causes of AKI associated with a broad range of atypical and typical antipsychotics. METHOD: This retrospective cohort analysis used January 2007-June 2013 US nationwide Humana claims data to define episodes of antipsychotic drug therapy for patients with schizophrenia and bipolar disorder...
March 13, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28283756/dopamine-t-cells-and-multiple-sclerosis-ms
#16
REVIEW
Mia Levite, Franca Marino, Marco Cosentino
Dopamine is a key neurotransmitter that induces critical effects in the nervous system and in many peripheral organs, via 5 dopamine receptors (DRs): D1R-D5R. Dopamine also induces many direct and very potent effects on many DR-expressing immune cells, primarily T cells and dendritic cells. In this review, we focus only on dopamine receptors, effects and production in T cells. Dopamine by itself (at an optimal concentration of~0.1 nM) induces multiple function of resting normal human T cells, among them: T cell adhesion, chemotactic migration, homing, cytokine secretion and others...
March 10, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28283227/clozapine-as-the-most-efficacious-antipsychotic-for-activating-erk-1-2-kinases-role-of-5-ht2a-receptor-agonism
#17
Stefano Aringhieri, Shivakumar Kolachalam, Claudio Gerace, Marco Carli, Valeria Verdesca, Maria Giulia Brunacci, Chiara Rossi, Chiara Ippolito, Anna Solini, Giovanni U Corsini, Marco Scarselli
Antipsychotics (APDs) are divided into first-generation antipsychotics (FGAs) and second-generation antipsychotics (SGAs) based on the concept that SGAs have reduced motor side effects. With this premise, this study examined in HeLa and other cell lines the effects of different APDs on the activation of ERK1/2 (Extracellular signal-regulated kinases) and AKT (Protein Kinase B) kinases, which may be affected in schizophrenia and bipolar disorder. Among the SGAs, Clozapine clearly resulted as the most effective drug inducing ERK1/2 phosphorylation with potency in the low micromolar range...
March 7, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28281228/development-of-a-risk-score-for-qtc-prolongation-the-risq-path-study
#18
Eline Vandael, Bert Vandenberk, Joris Vandenberghe, Isabel Spriet, Rik Willems, Veerle Foulon
Background More than 170 drugs are linked with QTc-prolongation, which in extreme cases can lead to Torsade de Pointes. Monitoring of this potential side effect is an important challenge in clinical practice. Objective To investigate the risk of QTc-prolongation in hospital patients who started a QTc-prolonging drug, and to develop a risk score to identify patients at high/low risk for QTc-prolongation. Setting University Hospitals Leuven, Belgium. Method All patients starting with haloperidol or a QTc-prolonging antibiotic/antimycotic were eligible for this observational study...
March 9, 2017: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/28279926/determination-of-drugs-in-plasma-samples-by-disposable-pipette-extraction-with-c18-bsa-phase-and-liquid-chromatography-tandem-mass-spectrometry
#19
Mônia Ap Lemos Pinto, Israel D de Souza, Maria Eugênia C Queiroz
This work describes restricted access material (RAM) constituted of porous octadecylsilane particles with the outer surface covered with bovine serum albumin (C18-BSA) as a stationary phase to extract drugs from plasma samples by disposable pipette extraction (DPX) for further analysis by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The C18-BSA phase simultaneously excluded macromolecules by chemical diffusion barrier (BSA network) and enrichment of the interior phase (C18) with drug traces by sorption...
March 1, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28279214/cardiotoxicity-evaluation-using-human-embryonic-stem-cells-and-induced-pluripotent-stem-cell-derived-cardiomyocytes
#20
Qi Zhao, Xijie Wang, Shuyan Wang, Zheng Song, Jiaxian Wang, Jing Ma
BACKGROUND: Cardiotoxicity remains an important concern in drug discovery. Human pluripotent stem cell-derived cardiomyocytes (hPSC-CMs) have become an attractive platform to evaluate cardiotoxicity. However, the consistency between human embryonic stem cell-derived cardiomyocytes (hESC-CMs) and human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) in prediction of cardiotoxicity has yet to be elucidated. METHODS: Here we screened the toxicities of four representative drugs (E-4031, isoprenaline, quinidine, and haloperidol) using both hESC-CMs and hiPSC-CMs, combined with an impedance-based bioanalytical method...
March 9, 2017: Stem Cell Research & Therapy
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