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Trifluoperazine

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https://www.readbyqxmd.com/read/29348654/low-concentration-trifluoperazine-promotes-proliferation-and-reduces-calcium-dependent-apoptosis-in-glioma-cells
#1
Yulin Wen, Yong Zhang, Jinbang Li, Feng Luo, Zhongxi Huang, Kunping Liu
Glioma patients constitute the greatest percentage of depressed neoplasm patients. These patients often require antidepressant treatment, but the effect of antidepressant drugs on glioma cells requires further evaluation. In the present study, we evaluated the effect of trifluoperazine (TFP) on the proliferation and apoptosis of glioma cells. Transcriptomic and bioinformatics analysis results suggested that antidepressant drugs, especially TFP, may upregulate the drug-resistant ability of glioma cells. A low concentration of TFP upregulated the viability of glioma cells...
January 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29336441/a-high-pressure-study-of-calmodulin-ligand-interactions-using-small-angle-x-ray-and-elastic-incoherent-neutron-scattering
#2
Süleyman Cinar, Samy Al-Ayoubi, Christian Sternemann, Judith Peters, Roland Winter, Claus Czeslik
Calmodulin (CaM) is a Ca2+ sensor and mediates Ca2+ signaling through binding of numerous target ligands. The binding of ligands by Ca2+-saturated CaM (holo-CaM) is governed by attractive hydrophobic and electrostatic interactions that are weakened under high pressure in aqueous solutions. Moreover, the potential formation of void volumes upon ligand binding creates a further source of pressure sensitivity. Hence, high pressure is a suitable thermodynamic variable to probe protein-ligand interactions. In this study, we compare the binding of two different ligands to holo-CaM as a function of pressure by using X-ray and neutron scattering techniques...
January 16, 2018: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29322188/management-of-morgellons-disease-with-low-dose-trifluoperazine
#3
Bernice Y Yan, Joseph L Jorizzo
No abstract text is available yet for this article.
January 10, 2018: JAMA Dermatology
https://www.readbyqxmd.com/read/29287071/uptake-of-polyphosphate-microparticles-in-vitro-saos-2-and-huvec-cells-followed-by-an-increase-of-the-intracellular-atp-pool-size
#4
Werner E G Müller, Shunfeng Wang, Matthias Wiens, Meik Neufurth, Maximilian Ackermann, Dinko Relkovic, Maria Kokkinopoulou, Qingling Feng, Heinz C Schröder, Xiaohong Wang
Recently two approaches were reported that addressed a vitally important problem in regenerative medicine, i. e. the successful treatment of wounds even under diabetic conditions. Accordingly, these studies with diabetic rabbits [Sarojini et al. PLoS One 2017, 12(4):e0174899] and diabetic mice [Müller et al. Polymers 2017, 9, 300] identified a novel (potential) target for the acceleration of wound healing in diabetes. Both studies propose a raise of the intracellular metabolic energy status via exogenous administration either of ATP, encapsulated into lipid vesicles, or of polyphosphate (polyP) micro-/nanoparticles...
2017: PloS One
https://www.readbyqxmd.com/read/29273456/the-antipsychotic-trifluoperazine-reduces-marble-burying-behavior-in-mice-via-d2-and-5-ht2a-receptors-implications-for-obsessive-compulsive-disorder
#5
Nobuaki Egashira, Naoki Kubota, Yu Goto, Takuya Watanabe, Kaori Kubota, Shutaro Katsurabayashi, Katsunori Iwasaki
Trifluoperazine, a typical antipsychotic drug, not only antagonizes dopamine D2 receptors but also enhances serotonin 5-HT2 receptor-mediated behavior. Moreover, trifluoperazine suppresses human purinergic receptor P2X7 responses and calmodulin. However, the effect of trifluoperazine on marble-burying behavior, which has been considered an animal model of obsessive-compulsive disorder (OCD), has not been studied. Here, we examined the effect of trifluoperazine on marble-burying behavior in mice. Oral administration of paroxetine, a selective serotonin reuptake inhibitor, significantly reduced marble-burying behavior without affecting total locomotor activity...
December 19, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29227273/-poisoning-by-psychopharmacological-drugs-in-azerbaijan-the-results-of-8-year-prospective-observation
#6
I Afandiyev, V Azizov
Acute poisoning of chemical etiology is a significant global public health problem. The aim of this study was the analysis of the toxicoepidemiological structure of psychopharmacological drugs poisoning in Azerbaijan. We collected and analyzed the data on all cases of acute poisoning by psychopharmacological drugs (codes of categories T42/T43 ICD-10) undergoing inpatient treatment at the Center of Clinical Toxicology in Baku, Azerbaijan in 2009-2016. The total number of patients with acute intoxication by psychopharmacological drugs was 3,413, which was 48...
November 2017: Georgian Medical News
https://www.readbyqxmd.com/read/29215674/bioinspired-dynamic-microcapsules
#7
N F D AlDala'een, W N K W Mohamad, N Alias, A M Ali, J Shaikh Mohammed
There is an increasing interest in bioinspired dynamic materials. Abundant illustrations of protein domains exist in nature, with remarkable ligand binding characteristics and structures that undergo conformational changes. For example, calmodulin (CaM) can have three conformational states, which are the unstructured Apo-state, Ca2+-bound ligand-exposed binding state, and compact ligand-bound state. CaM's mechanical response to biological cues is highly suitable for engineering dynamic materials. The distance between CaM globular terminals in the Ca2+-bound state is 5 nm and in the ligand-bound state is 1...
December 7, 2017: Soft Matter
https://www.readbyqxmd.com/read/29144549/zuclopenthixol-dihydrochloride-for-schizophrenia
#8
REVIEW
Edward J Bryan, Marie Ann Purcell, Ajit Kumar
BACKGROUND: Oral zuclopenthixol dihydrochloride (Clopixol) is an anti-psychotic treatment for people with psychotic symptoms, especially those with schizophrenia. It is associated with neuroleptic malignant syndrome, a prolongation of the QTc interval, extra-pyramidal reactions, venous thromboembolism and may modify insulin and glucose responses. OBJECTIVES: To determine the effects of zuclopenthixol dihydrochloride for treatment of schizophrenia. SEARCH METHODS: We searched the Cochrane Schizophrenia Group's Trials Register (latest search 09 June 2015)...
November 16, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29109161/combating-multi-drug-resistant-pathogens-with-host-directed-non-antibiotic-therapeutics
#9
Jourdan A Andersson, Jian Sha, Michelle L Kirtley, Emily Reyes, Eric C Fitts, Sara M Dann, Ashok K Chopra
Earlier, we reported that 3 Food and Drug Administration-approved drugs, trifluoperazine (TFP, anti-psychotic), amoxapine (AXPN, anti-depressant), and doxapram (DXP, breathing stimulant), identified from an in vitro murine macrophage cytotoxicity screen, provided 40-60% protection to mice against pneumonic plague when administered at the time of infection for 1-3 days. In this study, the therapeutic potential of these drugs was further evaluated in mice when administered up to 48 h post-infection against pneumonic plague...
November 6, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29066348/a-chemical-screen-identifies-trifluoperazine-as-an-inhibitor-of-glioblastoma-growth
#10
Tiago Pinheiro, Magdalena Otrocka, Brinton Seashore-Ludlow, Vilma Rraklli, Johan Holmberg, Karin Forsberg-Nilsson, András Simon, Matthew Kirkham
Glioblastoma (GBM) is regarded as the most common malignant brain tumor but treatment options are limited. Thus, there is an unmet clinical need for compounds and corresponding targets that could inhibit GBM growth. We screened a library of 80 dopaminergic ligands with the aim of identifying compounds capable of inhibiting GBM cell line proliferation and survival. Out of 45 active compounds, 8 were further validated. We found that the dopamine receptor D2 antagonist trifluoperazine 2HCl inhibits growth and proliferation of GBM cells in a dose dependent manner...
October 21, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29058407/antifungal-phenothiazines-optimization-characterization-of-mechanism-and-modulation-of-neuroreceptor-activity
#11
Marhiah C Montoya, Louis DiDone, Richard F Heier, Marvin J Meyers, Damian J Krysan
New classes of antifungal drugs are an urgent unmet clinical need. One approach to the challenge of developing new antifungal drugs is to optimize the antifungal properties of currently used drugs with favorable pharmacologic properties, so-called drug or scaffold repurposing. New therapies for cryptococcal meningitis are particularly important given its worldwide burden of disease and limited therapeutic options. We report the first systematic structure-activity study of the anticryptococcal properties of the phenothiazines...
November 2, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28925524/hypothermia-increases-aquaporin-4-aqp4-plasma-membrane-abundance-in-human-primary-cortical-astrocytes-via-a-calcium-transient-receptor-potential-vanilloid-4-trpv4-and-calmodulin-mediated-mechanism
#12
Mootaz M Salman, Philip Kitchen, M Nicola Woodroofe, James E Brown, Roslyn M Bill, Alex C Conner, Matthew T Conner
Human aquaporin 4 (AQP4) is the primary water channel protein in brain astrocytes. Hypothermia is known to cause astrocyte swelling in culture, but the precise role of AQP4 in this process is unknown. Primary human cortical astrocytes were cultured under hypothermic (32 °C) or normothermic (37 °C) conditions. AQP4 transcript, total protein and surface-localized protein were quantified using RT-qPCR, sandwich ELISA with whole cell lysates or cell surface biotinylation, followed by ELISA analysis of the surface-localized protein, respectively...
September 19, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28891312/consequences-of-market-withdrawal-of-fluphenazine-and-trifluoperazine-letter-to-the-editor-and-case-series
#13
Jesse Zanker, Angelo Ferraro
No abstract text is available yet for this article.
September 1, 2017: Australian and New Zealand Journal of Psychiatry
https://www.readbyqxmd.com/read/28876084/trifluoperazine-activates-foxo1-related-signals-to-inhibit-tumor-growth-in-hepatocellular-carcinoma
#14
Jingwen Jiang, Zhongxi Huang, Xuewu Chen, Rongcheng Luo, Hongbin Cai, Hairu Wang, Hui Zhang, Tao Sun, Yunfang Zhang
Schizophrenic patients tend to have reduced incidence of some cancers due to the treatment of antipsychotic drugs with antitumor effects, such as chlorpromazine and trifluoperazine (TFP). Forkhead Box O1 (FOXO1) as tumor suppressor in many malignancies is often inactivated by nuclear export, which could be inhibited by TFP. However, the antitumor efficiency of TFP and related role of FOXO1 in hepatocellular carcinoma (HCC) are unclear. Thus, two HCC cell lines SMMC-7721 and Bel-7402 were treated with different concentrations of TFP and the IC50 was determined...
October 2017: DNA and Cell Biology
https://www.readbyqxmd.com/read/28870216/trifluoperazine-a-novel-autophagy-inhibitor-increases-radiosensitivity-in-glioblastoma-by-impairing-homologous-recombination
#15
Xin Zhang, Ran Xu, Chao Zhang, Yangyang Xu, Mingzhi Han, Bin Huang, Anjing Chen, Chen Qiu, Frits Thorsen, Lars Prestegarden, Rolf Bjerkvig, Jian Wang, Xingang Li
BACKGROUND: Resistance to adjuvant radiotherapy is a major cause of treatment failure in patients with glioblastoma (GBM). Autophagy inhibitors have been shown to enhance the efficacy of radiotherapy for certain solid tumors. However, current inhibitors do not penetrate the blood-brain-barrier (BBB). Here, we assessed the radiosensitivity effects of the antipsychotic drug trifluoperazine (TFP) on GBM in vitro and in vivo. METHODS: U251 and U87 GBM cell lines as well as GBM cells from a primary human biopsy (P3), were used in vitro and in vivo to evaluate the efficacy of TFP treatment...
September 5, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28821547/cultivation-in-space-flight-produces-minimal-alterations-in-the-susceptibility-of-bacillus-subtilis-cells-to-72-different-antibiotics-and-growth-inhibiting-compounds
#16
Michael D Morrison, Patricia Fajardo-Cavazos, Wayne L Nicholson
Past results have suggested that bacterial antibiotic susceptibility is altered during space flight. To test this notion, Bacillus subtilis cells were cultivated in matched hardware, medium, and environmental conditions either in spaceflight microgravity on the International Space Station, termed Flight (FL) samples, or at Earth-normal gravity, termed Ground Control (GC) samples. Susceptibility of FL and GC samples was compared to 72 antibiotics and growth-inhibitory compounds using the Omnilog Phenotype Microarray (PM) system...
August 18, 2017: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/28803208/n-glucuronidation-catalyzed-by-ugt1a4-and-ugt2b10-in-human-liver-microsomes-assay-optimization-and-substrate-identification
#17
Danyi Lu, Qian Xie, Baojian Wu
N-glucuronidation is an important pathway for metabolism and disposition of tertiary amines in humans. This reaction is mainly catalyzed by the enzymes UGT1A4 and UGT2B10. However, the metabolic patterns of UGT1A4- and UGT2B10-mediated N-glucuronidation are not fully clear. In this study, we first optimized in vitro reaction conditions for N-glucuronidation by using specific substrates (i.e., trifluoperazine for UGT1A4, cotinine and amitriptyline for UGT2B10). Furthermore, we found that hepatic N-glucuronidation showed significant species differences...
October 25, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28793283/trifluoperazine-induced-suicidal-erythrocyte-death-and-s-nitrosylation-inhibition-reversed-by-the-nitric-oxide-donor-sodium-nitroprusside
#18
Mehrdad Ghashghaeinia, Mauro Carlos Wesseling, Elena Ramos, Polina Petkova-Kirova, Sabrina Waibel, Elisabeth Lang, Rosi Bissinger, Kossai Alzoubi, Baerbel Edelmann, Zohreh Hosseinzadeh, Peter Dreischer, Azam Shahvaroughi-Farahani, Ulrich Mrowietz, Martin Köberle, Lars Kaestner, Ingolf Bernhardt, Antonio Martínez-Ruiz, Thomas Wieder, Florian Lang
BACKGROUND AND PURPOSE: The high potency antipsychotic drug trifluoperazine (10-[3-(4-methyl-1-piperazinyl)-propyl]-2-(trifluoromethyl)-(10)H-phenothiazine dihydrochloride; TFP) may either counteract or promote suicidal cell death or apoptosis. Similar to apoptosis, erythrocytes may enter eryptosis, characterized by phosphatidylserine exposure at the cell surface and cell shrinkage. Eryptosis can be stimulated by an increase in cytoplasmic Ca2+ concentration ([Ca2+]i) and inhibited by nitric oxide (NO)...
2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28725147/shortage-of-psychotropic-medications-in-community-pharmacies-in-saudi-arabia-causes-and-solutions
#19
Yazed Sulaiman Al-Ruthia, Wael Mansy, Mohammad Barasin, Yazeed Mohammad Ghawaa, Mohammed AlSultan, Mohammad A Alsenaidy, Solaiman Alhawas, Sultan AlGhadeer
Background: Patients with mental disorders, such as depression and anxiety, who seek medical care in private psychiatric clinics in Riyadh, Saudi Arabia, have recently expressed concerns to doctors about difficulty in filling psychotropic medications, such as Amitriptyline and Aripiprazole, at retail community pharmacies. Objectives: The aim of this study was to investigate whether there is a shortage of some commonly prescribed psychotropic medications in retail community pharmacies in Saudi Arabia, and if so, to explore the possible reasons behind the shortage of these medications...
July 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28720707/intrinsically-disordered-chromatin-protein-nupr1-binds-to-the-c-terminal-region-of-polycomb-ring1b
#20
Patricia Santofimia-Castaño, Bruno Rizzuti, Ángel L Pey, Philippe Soubeyran, Miguel Vidal, Raúl Urrutia, Juan L Iovanna, José L Neira
Intrinsically disordered proteins (IDPs) are ubiquitous in eukaryotes, and they are often associated with diseases in humans. The protein NUPR1 is a multifunctional IDP involved in chromatin remodeling and in the development and progression of pancreatic cancer; however, the details of such functions are unknown. Polycomb proteins are involved in specific transcriptional cascades and gene silencing. One of the proteins of the Polycomb complex is the Ring finger protein 1 (RING1). RING1 is related to aggressive tumor features in multiple cancer types...
July 18, 2017: Proceedings of the National Academy of Sciences of the United States of America
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