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Trifluoperazine

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https://www.readbyqxmd.com/read/28803208/n-glucuronidation-catalyzed-by-ugt1a4-and-ugt2b10-in-human-liver-microsomes-assay-optimization-and-substrate-identification
#1
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...
August 4, 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
#2
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)...
August 9, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28725147/shortage-of-psychotropic-medications-in-community-pharmacies-in-saudi-arabia-causes-and-solutions
#3
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
#4
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
https://www.readbyqxmd.com/read/28713408/transcriptome-analyses-shed-new-insights-into-primary-metabolism-and-regulation-of-blumeria-graminis-f-sp-tritici-during-conidiation
#5
Fan-Song Zeng, Fabrizio Menardo, Min-Feng Xue, Xue-Jiang Zhang, Shuang-Jun Gong, Li-Jun Yang, Wen-Qi Shi, Da-Zhao Yu
Conidia of the obligate biotrophic fungal pathogen Blumeria graminis f. sp. tritici (Bgt) play a vital role in its survival and rapid dispersal. However, little is known about the genetic basis for its asexual reproduction. To uncover the primary metabolic and regulatory events during conidiation, we sequenced the transcriptome of Bgt epiphytic structures at 3 (vegetative hyphae growth), 4 (foot cells initiation), and 5 (conidiophore erection) days post-inoculation (dpi). RNA-seq analyses identified 556 and 404 (combined 685) differentially expressed genes (DEGs) at 4 and 5 dpi compared with their expression levels at 3 dpi, respectively...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28713151/trifluoperazine-inhibits-mesangial-cell-proliferation-by-arresting-cell-cycle-dependent-mechanisms
#6
Baodong Wang, Xiaoshuang Zhou, Yanqin Wang, Rongshan Li
BACKGROUND It has been reported that trifluoperazine (TFP) inhibits proliferation of cancer cells, however, the effects of TFP in renal proliferation diseases are still unclear. This study examined the effects of TFP on proliferation of human renal mesangial cells and analyzed the underlying mechanisms. MATERIAL AND METHODS Cell proliferation in vivo was determined by HE staining, immunohistochemistry of proliferating cell nuclear antigen (PCNA), and Western blot analysis (Ki-67 and PCNA). Effects of different TFP concentrations and treatment duration on cell proliferation and cell cycle were analyzed using the MTT assay and flow cytometry...
July 17, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28658645/bioresponsive-interfaces-composed-of-calmodulin-and-poly-ethylene-glycol-toggling-the-interfacial-film-thickness-by-protein-ligand-binding
#7
Süleyman Cinar, Claus Czeslik
Responsive interfaces are often realized by polymer films that change their structure and properties upon changing the pH-value, ionic strength or temperature. Here, we present a bioresponsive interfacial structure that is based on a protein, calmodulin (CaM), which undergoes a huge conformational change upon ligand binding. At first, we characterize the conformational functionality of a double Cys mutant of CaM by small-angle X-ray scattering (SAXS) and Fourier transform infrared (FTIR) spectroscopy. The CaM mutant is then used to cross-link poly(ethylene glycol) (PEG) chains, which are bound covalently to a supporting planar Si surface...
June 21, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28649130/dopamine-d2-receptor-antagonist-sulpiride-enhances-dexamethasone-responses-in-the-treatment-of-drug-resistant-and-metastatic-breast-cancer
#8
Jian Li, Qing-Yu Yao, Jun-Sheng Xue, Li-Jie Wang, Yin Yuan, Xiu-Yun Tian, Hong Su, Si-Yuan Wang, Wen-Jun Chen, Wei Lu, Tian-Yan Zhou
Recent evidence shows that dopamine D2-like receptor (D2DR) antagonists, such as trifluoperazine and thioridazine, are effective for cancer therapy and inhibition of cancer stem-like cells (CSCs). In this study, we investigated the anti-cancer effects of combination therapy of dexamethasone (DEX) and sulpiride (SUL), an atypical antipsychotic, against drug-resistant and metastatic breast cancers and further explored the underlying mechanisms. Oral administration of SUL (25, 100 mg·kg(-1)·d(-1)) alone did not inhibit the tumor growth in human breast cancer MCF-7/Adr xenograft model, but dose-dependently decreased the proportion of CSCs in vitro and in vivo...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28615774/hypokalemia-with-trifluoperazine-at-therapeutic-dose
#9
Sajjadur Rehman, Dhruba Jyoti Chetia
This case report outlines a rare presentation of hypokalemia with therapeutic doses of trifluoperazine in a patient with schizophrenia. Although there was comorbid diabetes mellitus in the patient, its effect was ruled out subsequently. On recovery, rechallenge with trifluoperazine resulted in the same effect at a milder level. No cardiac abnormalities were detected with the presentation. Naranjo adverse drug reaction probability scale reported definite relation with the drug.
May 2017: Indian Journal of Psychological Medicine
https://www.readbyqxmd.com/read/28503408/trifluoperazine-inhibits-acetaminophen-induced-hepatotoxicity-and-hepatic-reactive-nitrogen-formation-in-mice-and-in-freshly-isolated-hepatocytes
#10
Sudip Banerjee, Stepan B Melnyk, Kimberly J Krager, Nukhet Aykin-Burns, Sandra S McCullough, Laura P James, Jack A Hinson
The hepatotoxicity of acetaminophen (APAP) occurs by initial metabolism to N-acetyl-p-benzoquinone imine which depletes GSH and forms APAP-protein adducts. Subsequently, the reactive nitrogen species peroxynitrite is formed from nitric oxide (NO) and superoxide leading to 3-nitrotyrosine in proteins. Toxicity occurs with inhibited mitochondrial function. We previously reported that in hepatocytes the nNOS (NOS1) inhibitor NANT inhibited APAP toxicity, reactive nitrogen and oxygen species formation, and mitochondrial dysfunction...
2017: Toxicology Reports
https://www.readbyqxmd.com/read/28431223/pink1-based-screen-shines-light-on-autophagy-enhancers-for-parkinson-s-disease
#11
Dominik Haddad, Ken Nakamura
In this issue of Cell Chemical Biology, Zhang et al. (2017) report a zebrafish model of Parkinson's disease (PD), incorporating the PD-protein PINK1 and rotenone, a toxin linked to PD. Using it as a drug-screening platform, they identify trifluoperazine and other piperazine phenothiazines as protective compounds that enhance autophagy independent of PINK1.
April 20, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28379700/building-polyelectrolyte-multilayers-with-calmodulin-a-neutron-and-x-ray-reflectivity-study
#12
Süleyman Cinar, Simone Möbitz, Samy Al-Ayoubi, Beatrix-Kamelia Seidlhofer, Claus Czeslik
We have studied the formation and functional properties of polyelectrolyte multilayers where calmodulin (CaM) is used as a polyanion. CaM is known to populate distinct conformational states upon binding Ca(2+) and small ligand molecules. Therefore, we have also probed the effects of Ca(2+) ions and trifluoperazine (TFP) as ligand molecule on the interfacial structures. Multilayers with the maximum sequence PEI-(PSS-PAH)x-CaM-PAH-CaM-PAH have been deposited on silicon wafers and characterized by X-ray and neutron reflectometry...
April 12, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28366621/rescue-of-pink1-deficiency-by-stress-dependent-activation-of-autophagy
#13
Yuxi Zhang, David T Nguyen, Ellen M Olzomer, Gin P Poon, Nicholas J Cole, Anita Puvanendran, Brigitte R Phillips, Daniel Hesselson
Stimulating autophagy is a promising therapeutic strategy for slowing the progression of neurodegenerative disease. Neurons are insensitive to current approaches based on mTOR inhibition for activating autophagy, and instead may rely on the Parkinson's disease-associated proteins PINK1 and PARKIN to activate the autophagy-lysosomal pathway in response to mitochondrial damage. We developed a multifactorial zebrafish drug-screening platform combining Pink1 deficiency with an environmental toxin to compromise mitochondrial function and trigger dopaminergic neuron loss...
April 20, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28304162/rational-design-synthesis-and-biological-evaluation-of-heterocyclic-quinolones-targeting-the-respiratory-chain-of-mycobacterium-tuberculosis
#14
W David Hong, Peter D Gibbons, Suet C Leung, Richard Amewu, Paul A Stocks, Andrew Stachulski, Pedro Horta, Maria L S Cristiano, Alison E Shone, Darren Moss, Alison Ardrey, Raman Sharma, Ashley J Warman, Paul T P Bedingfield, Nicholas E Fisher, Ghaith Aljayyoussi, Sally Mead, Maxine Caws, Neil G Berry, Stephen A Ward, Giancarlo A Biagini, Paul M O'Neill, Gemma L Nixon
A high-throughput screen (HTS) was undertaken against the respiratory chain dehydrogenase component, NADH:menaquinone oxidoreductase (Ndh) of Mycobacterium tuberculosis (Mtb). The 11000 compounds were selected for the HTS based on the known phenothiazine Ndh inhibitors, trifluoperazine and thioridazine. Combined HTS (11000 compounds) and in-house screening of a limited number of quinolones (50 compounds) identified ∼100 hits and four distinct chemotypes, the most promising of which contained the quinolone core...
May 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28264990/an-eight-residue-deletion-in-escherichia-coli-fabg-causes-temperature-sensitive-growth-and-lipid-synthesis-plus-resistance-to-the-calmodulin-inhibitor-trifluoperazine
#15
Swaminath Srinivas, John E Cronan
FabG performs the NADPH-dependent reduction of β-keto acyl-acyl carrier protein substrates in the elongation cycle of fatty acid synthesis. We report the characterization of a temperature-sensitive mutation (fabGΔ8) in Escherichia colifabG that results from an in-frame 8-amino-acid residue deletion in the α6/α7 subdomain. This region forms part of one of the two dimerization interfaces of this tetrameric enzyme and is reported to undergo significant conformational changes upon cofactor binding, which define the entrance to the active-site cleft...
May 15, 2017: Journal of Bacteriology
https://www.readbyqxmd.com/read/28109665/a-randomized-double-blind-comparison-of-the-efficacy-and-safety-of-low-dose-olanzapine-plus-low-dose-trifluoperazine-versus-full-dose-olanzapine-in-the-acute-treatment-of-schizophrenia
#16
Ching-Hua Lin, Fu-Chiang Wang, Shih-Chi Lin, Yu-Hui Huang, Cheng-Chung Chen
OBJECTIVE: Antipsychotic polypharmacy is common in clinical practice, but not recommended in guidelines for treating schizophrenia patients. This study aimed to compare the efficacy and safety of low-dose olanzapine plus low-dose trifluoperazine (a first-generation antipsychotic [FGA]) to full-dose olanzapine (a second-generation antipsychotic [SGA]) in the treatment of acute schizophrenia. METHOD: In this 6-week, double-blind, fixed-dose study, patients were randomized to receive 5mg/day of olanzapine plus 5mg/day of trifluoperazine or 10mg/day of olanzapine for 6weeks...
January 18, 2017: Schizophrenia Research
https://www.readbyqxmd.com/read/28103775/interaction-of-antipsychotic-drugs-with-sucrase-kinetics-and-structural-study
#17
Narges Jafari, Helia Dehganpour, Nava Ghavanini, Hamidreza Mollasalehi, Dariush Minai-Tehrani
BACKGROUND: In patients with the Congenital Sucrase-Isomaltase Deficiency (CSID), who lack intestinal sucrase-isomaltase enzyme, a suspension of yeast sucrase is applied as a drug to compensate the enzyme deficiency. While antipsychotic drugs are used for the treatment of schizophrenia, administering multiple drugs at the same time may counteract each other. METHODS: In this study, the interaction between trifluoperazine and haloperidol as antipsychotic drugs on oral drug yeast sucrase was investigated...
2017: Current Clinical Pharmacology
https://www.readbyqxmd.com/read/28101459/venlafaxine-induced-cytotoxicity-towards-isolated-rat-hepatocytes-involves-oxidative-stress-and-mitochondrial-lysosomal-dysfunction
#18
Elham Ahmadian, Hossein Babaei, Alireza Mohajjel Nayebi, Aziz Eftekhari, Mohammad Ali Eghbal
Purpose: Depression is a public disorder worldwide. Despite the widespread use of venlafaxine in the treatment of depression, it has been associated with the incidence of toxicities. Hence, the goal of the current investigation was to evaluate the mechanisms of venlafaxine-induced cell death in the model of the freshly isolated rat hepatocytes. Methods: Collagenase-perfused rat hepatocytes were treated with venlafaxine and other agents. Cell damage, reactive oxygen species (ROS) formation, lipid peroxidation, mitochondrial membrane potential decline, lysosomal damage, glutathione (GSH) level were analyzed...
December 2016: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28092099/calmodulin-binding-to-death-receptor-5-mediated-death-inducing-signaling-complex-in-breast-cancer-cells
#19
Romone M Fancy, Harrison Kim, Tong Zhou, Kurt R Zinn, Donald J Buchsbaum, Yuhua Song
Activation of death receptor-5 (DR5) leads to the formation of death-inducing signaling complex (DISC) for apoptotic signaling. TRA-8, a DR5 specific agonistic antibody, has demonstrated significant cytotoxic activity in vitro and in vivo without inducing hepatotoxicity. Calmodulin (CaM) that is overexpressed in breast cancer plays a critical role in regulating DR5-mediated apoptosis. However, the mechanism of CaM in regulating DR5-mediated apoptotic signaling remains unknown. In this study, we characterized CaM binding to DR5-mediated DISC for apoptosis in TRA-8 sensitive breast cancer cell lines using co-immunoprecipitation, fluorescence microscopic imaging, caspase signaling analysis, and cell viability assay...
August 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28062709/trifluoperazine-a-well-known-antipsychotic-inhibits-glioblastoma-invasion-by-binding-to-calmodulin-and-disinhibiting-calcium-release-channel-ip3r
#20
Seokmin Kang, Jinpyo Hong, Jung Moo Lee, Hyo Eun Moon, Borami Jeon, Jungil Choi, Nal Ae Yoon, Sun Ha Paek, Eun Joo Roh, C Justin Lee, Sang Soo Kang
Calcium (Ca(2+)) signaling is an important signaling process, implicated in cancer cell proliferation and motility of the deadly glioblastomas that aggressively invade neighboring brain tissue. We have previously demonstrated that caffeine blocks glioblastoma invasion and extends survival by inhibiting Ca(2+) release channel inositol 1,4,5-trisphosphate receptor (IP3R) subtype 3. Trifluoperazine (TFP) is an FDA-approved antipsychotic drug for schizophrenia. Interestingly, TFP has been recently reported to show a strong anticancer effect on lung cancer, hepatocellular carcinoma, and T-cell lymphoma...
January 2017: Molecular Cancer Therapeutics
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