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Trifluoperazine

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https://www.readbyqxmd.com/read/28304162/rational-design-synthesis-and-biological-evaluation-of-heterocyclic-quinolones-targeting-the-respiratory-chain-of-mycobacterium-tuberculosis
#1
Weiqian David Hong, Peter D Gibbons, Suet C Leung, Richard Amewu, Paul A Stocks, Andrew Valentine Stachulski, Pedro C Horta, Maria Lurdes Santos 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 Louise Nixon
A High-throughput screen (HTS) was undertaken against the respiratory chain dehydrogenase component, NADH:menaquinone oxidoreductase (Ndh) of Mycobacterium tuberculosis (Mtb). 11,000 compounds were selected for the HTS based on the known phenothiazine Ndh inhibitors, trifluoperazine and thioridazine. Combined HTS (11,000 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...
March 17, 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
#2
Swaminath Srinivas, John E Cronan
FabG performs the NADPH-dependent reduction of ß-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 eight 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...
March 6, 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
#3
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
#4
Narges Jafari, Helia Dehganpour, Nava Ghavanini, Hamidreza Mollasalehi, Dariush Minai-Tehrani
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 treatment of schizophrenia, administering multiple drugs at the same time may counteract each other. In this study, the interaction between trifluoperazine and haloperidol as antipsychotic drugs on oral drug yeast sucrase was investigated. The results showed that both drugs could reduce sucrase activity and decrease the Vmax of the enzyme by non-competitive inhibition...
January 18, 2017: Current Clinical Pharmacology
https://www.readbyqxmd.com/read/28101459/venlafaxine-induced-cytotoxicity-towards-isolated-rat-hepatocytes-involves-oxidative-stress-and-mitochondrial-lysosomal-dysfunction
#5
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
#6
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...
January 16, 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
#7
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
https://www.readbyqxmd.com/read/27904048/inhibitory-effect-of-hesperetin-and-naringenin-on-human-udp-glucuronosyltransferase-enzymes-implications-for-herb-drug-interactions
#8
Dan Liu, Jie Wu, Hongbo Xie, Mingyi Liu, Isaiah Takau, Hong Zhang, Yuqing Xiong, Chunhua Xia
Hesperetin (HET) and naringenin (NGR) are flavanones found in citrus (oranges and grapefruit) and Aurantii Fructus Immaturus. The present study aims to investigate the inhibition potential of HET and NGR derivatives towards one of the most important phase II drug-metabolizing enzymes-uridine diphosphate (UDP)-glucuronosyltransferases (UGTs). We used trifluoperazine as a probe substrate to test UGT1A4 activity, and recombinant UGT-catalyzed 4-methylumbelliferone glucuronidation was used as a probe reaction for other UGT isoforms...
2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27858314/genetically-dissecting-p2rx7-expression-within-the-central-nervous-system-using-conditional-humanized-mice
#9
Michael W Metzger, Sandra M Walser, Fernando Aprile-Garcia, Nina Dedic, Alon Chen, Florian Holsboer, Eduardo Arzt, Wolfgang Wurst, Jan M Deussing
The purinergic P2X7 receptor (P2X7R) has attracted considerable interest as a potential target for various central nervous system (CNS) pathologies including affective and neurodegenerative disorders. To date, the distribution and cellular localization of the P2X7R in the brain are not fully resolved and a matter of debate mainly due to the limitations of existing tools. However, this knowledge should be a prerequisite for understanding the contribution of the P2X7R to brain disease. Here, we generated a genetic mouse model by humanizing the P2X7R in the mouse as mammalian model organism...
November 17, 2016: Purinergic Signalling
https://www.readbyqxmd.com/read/27777063/liraglutide-restores-angiogenesis-in-palmitate-impaired-human-endothelial-cells-through-pi3k-akt-foxo1-gtpch1-pathway
#10
Jing Ke, Rui Wei, Fei Yu, Jingjing Zhang, Tianpei Hong
Glucagon-like peptide-1 (GLP-1) and its analogues have a beneficial role in cardiovascular system. Here, we aimed to investigate whether liraglutide, a GLP-1 analogue, modulated angiogenesis impaired by palmitic acid (PA) in cultured human umbilical vein endothelial cells (HUVECs). Cells were incubated with liraglutide (3-100 nmol/L) in the presence of PA (0.5mmol/L), and endothelial tube formation was observed and quantified. The protein levels of signaling molecules were analyzed and the specific inhibitors were used to identify the signaling pathways through which liraglutide affected angiogenesis...
December 2016: Peptides
https://www.readbyqxmd.com/read/27703755/long-term-antipsychotic-treatment-in-schizophrenia-systematic-review-and-network-meta-analysis-of-randomised-controlled-trials
#11
Ying Jiao Zhao, Liang Lin, Monica Teng, Ai Leng Khoo, Lay Beng Soh, Toshiaki A Furukawa, Ross J Baldessarini, Boon Peng Lim, Kang Sim
BACKGROUND: For treatment of patients diagnosed with schizophrenia, comparative long-term effectiveness of antipsychotic drugs to reduce relapses when minimising adverse effects is of clinical interest, hence prompting this review. AIMS: To evaluate the comparative long-term effectiveness of antipsychotic drugs. METHOD: We systematically searched electronic databases for reports of randomised controlled trials (RCTs) of antipsychotic monotherapy aimed at reducing relapse risks in schizophrenia...
January 2016: BJPsych Open
https://www.readbyqxmd.com/read/27693219/fhcabp1-fh22-a-fasciola-hepatica-calcium-binding-protein-with-ef-hand-and-dynein-light-chain-domains
#12
Sarah Cheung, Charlotte M Thomas, David J Timson
FH22 has been previously identified as a calcium-binding protein from the common liver fluke, Fasciola hepatica. It is part of a family of at least four proteins in this organism which combine an EF-hand containing N-terminal domain with a C-terminal dynein light chain-like domain. Here we report further biochemical properties of FH22, which we propose should be renamed FhCaBP1 for consistency with other family members. Molecular modelling predicted that the two domains are linked by a flexible region and that the second EF-hand in the N-terminal domain is most likely the calcium ion binding site...
November 2016: Experimental Parasitology
https://www.readbyqxmd.com/read/27666479/trifluoperazine-blocks-the-human-cardiac-sodium-channel-nav1-5-independent-of-calmodulin
#13
Dong-Hyun Kim, Su-Jin Lee, Sang June Hahn, Jin-Sung Choi
Trifluoperazine is a phenothiazine derivative which is mainly used in the management of schizophrenia and also acts as a calmodulin inhibitor. We used the whole-cell patch-clamp technique to study the effects of trifluoperazine on human Nav1.5 (hNav1.5) currents expressed in HEK293 cells. The 50% inhibitory concentration of trifluoperazine was 15.5 ± 0.3 μM and the Hill coefficient was 2.7 ± 0.1. The effects of trifluoperazine on hNav1.5 were completely and repeatedly reversible after washout. Trifluoperazine caused depolarizing shifts in the activation and hyperpolarizing shifts in the steady-state inactivation of hNav1...
October 21, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27618117/inhibition-of-bacterial-rnase-p-rna-by-phenothiazine-derivatives
#14
Shiying Wu, Guanzhong Mao, Leif A Kirsebom
There is a need to identify novel scaffolds and targets to develop new antibiotics. Methylene blue is a phenothiazine derivative, and it has been shown to possess anti-malarial and anti-trypanosomal activities. Here, we show that different phenothiazine derivatives and pyronine G inhibited the activities of three structurally different bacterial RNase P RNAs (RPRs), including that from Mycobacterium tuberculosis, with Ki values in the lower μM range. Interestingly, three antipsychotic phenothiazines (chlorpromazine, thioridazine, and trifluoperazine), which are known to have antibacterial activities, also inhibited the activity of bacterial RPRs, albeit with higher Ki values than methylene blue...
September 8, 2016: Biomolecules
https://www.readbyqxmd.com/read/27600106/in-vitro-inhibition-of-ugt1a3-ugt1a4-by-ursolic-and-oleanolic-acid-and-drug-drug-interaction-risk-prediction
#15
Hongbo Xie, Jie Wu, Dan Liu, Mingyi Liu, Hong Zhang, Shibo Huang, Yuqing Xiong, Chunhua Xia
1. Ursolic acid (UA) and oleanolic acid (OA) may have important activity relevant to health and disease prevention. Thus, we studied the activity of UA and OA on UDP-glucuronosyltransferases (UGTs) and used trifluoperazine as a probe substrate to test UGT1A4 activity. Recombinant UGT-catalyzed 4-methylumbelliferone (4-MU) glucuronidation was used as a probe reaction for other UGT isoforms. 2. UA and OA inhibited UGT1A3 and UGT1A4 activity but did not inhibit other tested UGT isoforms. 3. UA-mediated inhibition of UGT1A3 catalyzed 4-MU-β-D-glucuronidation was via competitive inhibition (IC50 0...
September 7, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27558359/the-quality-of-lactation-studies-including-antipsychotics
#16
REVIEW
Hazel Hummels, Daphne Bertholee, Douwe van der Meer, Jan Pieter Smit, Bob Wilffert, Peter Ter Horst
THE AIM OF THE STUDY: The aim of this study is to determine the quality of lactation studies that investigated antipsychotics in breast milk according to the Food and Drug Administration (FDA) and International Lactation Consultant Association (ILCA) draft guidelines. MATERIALS AND METHODS: We used the draft FDA and ILCA guidelines to review the quality of articles including antipsychotic use during breastfeeding. We used PubMed and Lactmed for the literature search...
December 2016: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27476280/rapid-spectrophotometric-determination-of-trifluoperazine-dihydrochloride-as-base-form-in-pharmaceutical-formulation-through-charge-transfer-complexation
#17
Kudige Nagaraj Prashanth, Nagaraju Swamy, Kanakapura Basavaiah
Two simple and selective spectrophotometric methods are described for the determination of trifluoperazine dihydrochloride (TFH) as base form (TFP) in bulk drug, and in tablets. The methods are based on the molecular charge-transfer complexation of trifluoperazine base (TFP) with either 2,4,6-trinitrophenol (picric acid; PA) or 2,4-dinitrophenol (DNP). The yellow colored radical anions formed are quantified at 410 run (PA method) or 415 nm (DNP method). The assay conditions were optimized for both the methods...
May 2016: Acta Poloniae Pharmaceutica
https://www.readbyqxmd.com/read/27474355/identification-and-characterization-of-human-udp-glucuronosyltransferases-responsible-for-the-in%C3%A2-vitro-glucuronidation-of-ursolic-acid
#18
Rui Gao, Mingyi Liu, Yu Chen, Chunhua Xia, Hong Zhang, Yuqing Xiong, Shibo Huang
This study aims to characterize the glucuronidation kinetics of ursolic acid (UA) in human liver microsomes (HLMs) and intestinal microsomes (HIMs) and identify the main UDP-glucuronosyltransferases (UGTs) involved. In our present study, only one type of UA glucuronide was observed after incubation with HLMs and HIMs respectively and was identified as a UA hydroxyl O-glucuronide. The glucuronidation of UA can be shown in HLMs and HIMs with Km values of 3.29 ± 0.16 and 3.74 ± 0.22 μM and Vmax values of 0...
August 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27449396/phenothiazines-solution-complexity-determination-of-pka-and-solubility-ph-profiles-exhibiting-sub-micellar-aggregation-at-25-and-37%C3%A2-c
#19
Aneta Pobudkowska, Clara Ràfols, Xavier Subirats, Elisabeth Bosch, Alex Avdeef
The ionization constants (pKa) and the pH-dependent solubility (log S-pH) of six phenothiazine derivatives (promazine hydrochloride, chlorpromazine hydrochloride, triflupromazine hydrochloride, fluphenazine dihydrochloride, perphenazine free base, and trifluoperazine dihydrochloride) were determined at 25 and 37°C. The pKa values of these low-soluble surface active molecules were determined by the cosolvent method (n-propanol/water at 37°C and methanol/water at 25°C). The log S-pH profiles were measured at 24h incubation time in 0...
October 10, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27359323/the-inhibition-of-udp-glucuronosyltransferases-ugts-by-vitamin-a
#20
Xin Liu, Yun-Feng Cao, Pei-Pei Dong, Liang-Liang Zhu, Zhenying Zhao, Xue Wu, Zhi-Wei Fu, Chun-Ting Huang, Zhong-Ze Fang, Hong-Zhi Sun
1. The exposed level of vitamin A in plasma might be exceeded due to the both inadvertent and clinical utilization. The adverse effects of vitamin A have been frequently reported, however, the mechanism remains unclear. The inhibition of vitamin A on the activity of UDP-glucuronosyltransferases (UGTs) was determined using in vitro incubation system to explain the adverse effects of vitamin A from a new perspective. 2. UGT supersomes catalyzed glucuronidation of 4-methylumbelliferone (4-MU), trifluoperazine (TFP), and cotinine was used as the probe reaction to evaluate the inhibition of vitamin A toward UGT isoforms, and 100 μM of vitamin A significantly inhibited the activity of all the tested UGT isoforms...
June 30, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
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