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[PMID]:29336441
[Au] Autor:Cinar S; Al-Ayoubi S; Sternemann C; Peters J; Winter R; Czeslik C
[Ad] Endereço:Department of Chemistry and Chemical Biology, TU Dortmund University, D-44221 Dortmund, Germany. claus.czeslik@uni-dortmund.de.
[Ti] Título:A high pressure study of calmodulin-ligand interactions using small-angle X-ray and elastic incoherent neutron scattering.
[So] Source:Phys Chem Chem Phys;20(5):3514-3522, 2018 Jan 31.
[Is] ISSN:1463-9084
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Calmodulin (CaM) is a Ca sensor and mediates Ca signaling through binding of numerous target ligands. The binding of ligands by Ca -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. The two ligands are the farnesylated hypervariable region (HVR) of the K-Ras4B protein, which is a natural binding partner of holo-CaM, and the antagonist trifluoperazine (TFP), which is known to inhibit holo-CaM activity. From small-angle X-ray scattering experiments performed up to 3000 bar, we observe a pressure-induced partial unfolding of the free holo-CaM in the absence of ligands, where the two lobes of the dumbbell-shaped protein are slightly swelled. In contrast, upon binding TFP, holo-CaM forms a closed globular conformation, which is pressure stable at least up to 3000 bar. The HVR of K-Ras4B shows a different binding behavior, and the data suggest the dissociation of the holo-CaM/HVR complex under high pressure, probably due to a less dense protein contact of the HVR as compared to TFP. The elastic incoherent neutron scattering experiments corroborate these findings. Below 2000 bar, pressure induces enhanced atomic fluctuations in both holo-CaM/ligand complexes, but those of the holo-CaM/HVR complex seem to be larger. Thus, the inhibition of holo-CaM by TFP is supported by a low-volume ligand binding, albeit this is not associated with a rigidification of the complex structure on the sub-ns Å-scale.
[Mh] Termos MeSH primário: Calmodulina/química
Ligantes
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Cálcio/química
Cálcio/metabolismo
Calmodulina/metabolismo
Difração de Nêutrons
Pressão
Ligação Proteica
Espalhamento a Baixo Ângulo
Trifluoperazina/química
Trifluoperazina/metabolismo
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calmodulin); 0 (Ligands); 214IZI85K3 (Trifluoperazine); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180117
[St] Status:MEDLINE
[do] DOI:10.1039/c7cp07399b


  2 / 3184 MEDLINE  
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[PMID]:29235339
[Au] Autor:Babich LG; Shlykov SG; Kushnarova AM; Kosterin SO
[Ti] Título:Ca(2+)-dependent regulation of the Ca(2+) concentration in the myometrium mitochondria. I. Trifluoperazine effects on mitochondria membranes polarization and [Ca(2+)](m).
[So] Source:Ukr Biochem J;88(4):5-11, 2016 Jul-Aug.
[Is] ISSN:2409-4943
[Cp] País de publicação:Ukraine
[La] Idioma:eng
[Ab] Resumo:Са2+-dependent regulation of Ca2+ exchange in mitochondria is carried out with participation of calmodulin. We have shown previously that calmodulin antagonists reduced the level of mitochondrial membrane polarization and induced increase of the ionized Са concentration in both the mitochondrial matrix and cell cytoplasm. The concentration-dependent influence of trifluoperazine on the level of polarization of mitochondrial membranes has been shown in this work. The coordinates of the Hill graphs were used to calculate the constant K0.5 and the Hill coefficient. K0.5 was 24.4 ± 5 µM (n = 10). The Hill coefficient was 2.0 ± 0.2, indicating the presence of two centers of the trifluoperazine binding. We have also studied [Ca2+]m changes, when incubating mitochondria in mediums of different composition: without ATP and ions of Mg (0-medium), in the presence of 3 mM Mg (Mg-medium) and 3 mM Mg + 3 mM ATP (Mg,ATP-medium). It was shown that the composition of the incubation medium affected the [Ca2+]m values in the absence of exogenous Ca2+ and did not affect them in the presence of the latter. Preincubation of mitochondria in mediums of different composition with 25 µM trifluoperazine did not affect the [Ca2+]m values both before and after the addition of 100 µÐœ Са2+ to the incubation medium. It was concluded, that trifluoperazine depolarized myometrial mitochondria membranes in concentration-dependent manner. However, mitochondria preincubation with 25 µM trifluope­razine accompanied by 50% decrease in membrane polarization did not affect the [Ca2+]m values.
[Mh] Termos MeSH primário: Cálcio/metabolismo
Potencial da Membrana Mitocondrial/efeitos dos fármacos
Mitocôndrias/efeitos dos fármacos
Membranas Mitocondriais/efeitos dos fármacos
Trifluoperazina/farmacologia
[Mh] Termos MeSH secundário: Trifosfato de Adenosina/metabolismo
Animais
Calmodulina/antagonistas & inibidores
Calmodulina/metabolismo
Meios de Cultura/química
Relação Dose-Resposta a Droga
Feminino
Transporte de Íons/efeitos dos fármacos
Cinética
Magnésio/metabolismo
Mitocôndrias/metabolismo
Membranas Mitocondriais/metabolismo
Miométrio/química
Ratos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calmodulin); 0 (Culture Media); 214IZI85K3 (Trifluoperazine); 8L70Q75FXE (Adenosine Triphosphate); I38ZP9992A (Magnesium); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180116
[Lr] Data última revisão:
180116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171214
[St] Status:MEDLINE
[do] DOI:10.15407/ubj88.04.005


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[PMID]:28876084
[Au] Autor:Jiang J; Huang Z; Chen X; Luo R; Cai H; Wang H; Zhang H; Sun T; Zhang Y
[Ad] Endereço:1 Department of Medical Oncology, Hainan Province Hospital of Traditional Chinese Medicine , Haikou, China .
[Ti] Título:Trifluoperazine Activates FOXO1-Related Signals to Inhibit Tumor Growth in Hepatocellular Carcinoma.
[So] Source:DNA Cell Biol;36(10):813-821, 2017 Oct.
[Is] ISSN:1557-7430
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo: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. We found that TFP could inhibit the vitality of two cell lines and induce cell cycle arrest at G0/G1. Meanwhile, the apoptosis was also increased and the ability of migration or invasion was found to be impaired by TFP. Interestingly, TFP reversed the cytoplasmic localization of FOXO1 to nuclear and increased its expression in nuclear, and increased the ratio of Bax/Bcl-2. However, knockdown of FOXO1 significantly abrogated the TFP-induced apoptosis by increasing the Bcl-2 expression. Furthermore, we found that TFP in vivo could effectively restrict the angiogenesis and tumor growth with reduced expression of VEGF, Bcl-2, and PCNA, and increased the nuclear localization of FOXO1, which indicated its antitumor role in HCC.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Carcinoma Hepatocelular/metabolismo
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Proteína Forkhead Box O1/metabolismo
Neoplasias Hepáticas/imunologia
Trifluoperazina/farmacologia
[Mh] Termos MeSH secundário: Carcinoma Hepatocelular/irrigação sanguínea
Carcinoma Hepatocelular/tratamento farmacológico
Linhagem Celular Tumoral
Seres Humanos
Neoplasias Hepáticas/irrigação sanguínea
Neoplasias Hepáticas/tratamento farmacológico
Neoplasias Hepáticas/patologia
Neovascularização Patológica/tratamento farmacológico
Neovascularização Patológica/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Forkhead Box Protein O1); 0 (Foxo1 protein, mouse); 214IZI85K3 (Trifluoperazine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171020
[Lr] Data última revisão:
171020
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170907
[St] Status:MEDLINE
[do] DOI:10.1089/dna.2017.3790


  4 / 3184 MEDLINE  
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[PMID]:28264990
[Au] Autor:Srinivas S; Cronan JE
[Ad] Endereço:Department of Biochemistry, University of Illinois at Urbana-Champaign, Urbana, Illinois, USA.
[Ti] Título:An Eight-Residue Deletion in Escherichia coli FabG Causes Temperature-Sensitive Growth and Lipid Synthesis Plus Resistance to the Calmodulin Inhibitor Trifluoperazine.
[So] Source:J Bacteriol;199(10), 2017 May 15.
[Is] ISSN:1098-5530
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo: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 ( Δ ) in 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. The activity of the mutant enzyme is extremely thermolabile and is deficient in forming homodimers at nonpermissive temperatures with a corresponding decrease in fatty acid synthesis both and Surprisingly, the Δ strain reverts to temperature resistance at a rate reminiscent of that of a point mutant with intragenic pseudorevertants located either on the 2-fold axes of symmetry or at the mouth of the active-site cleft. The Δ mutation also confers resistance to the calmodulin inhibitor trifluoperazine and renders the enzyme extremely sensitive to Ca We also observed a significant alteration in the lipid A fatty acid composition of Δ strains but only in an background, probably due to alterations in the permeability of the outer membrane. These observations provide insights into the structural dynamics of FabG and hint at yet another point of regulation between fatty acid and lipid A biosynthesis. Membrane lipid homeostasis and its plasticity in a variety of environments are essential for bacterial survival. Since lipid biosynthesis in bacteria and plants is fundamentally distinct from that in animals, it is an ideal target for the development of antibacterial therapeutics. FabG, the subject of this study, catalyzes the first cofactor-dependent reduction in this pathway and is active only as a tetramer. This study examines the interactions responsible for tetramerization through the biochemical characterization of a novel temperature-sensitive mutation caused by a short deletion in an important helix-turn-helix motif. The mutant strain has altered phospholipid and lipid A compositions and is resistant to trifluoperazine, an inhibitor of mammalian calmodulin. Understanding its structural dynamics and its influence on lipid A synthesis also allows us to explore lipid homeostasis as a mechanism for antibiotic resistance.
[Mh] Termos MeSH primário: Oxirredutases do Álcool/genética
Farmacorresistência Bacteriana/efeitos da radiação
Escherichia coli/crescimento & desenvolvimento
Escherichia coli/efeitos da radiação
Metabolismo dos Lipídeos/efeitos da radiação
Deleção de Sequência
[Mh] Termos MeSH secundário: Oxirredutases do Álcool/química
Antibacterianos/farmacologia
Cálcio/toxicidade
Estabilidade Enzimática/efeitos da radiação
Escherichia coli/enzimologia
Escherichia coli/genética
Multimerização Proteica
Supressão Genética
Temperatura Ambiente
Trifluoperazina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 214IZI85K3 (Trifluoperazine); EC 1.1.- (Alcohol Oxidoreductases); EC 1.1.1.36 (acetoacetyl-CoA reductase); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171025
[Lr] Data última revisão:
171025
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170308
[St] Status:MEDLINE


  5 / 3184 MEDLINE  
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[PMID]:28062709
[Au] Autor:Kang S; Hong J; Lee JM; Moon HE; Jeon B; Choi J; Yoon NA; Paek SH; Roh EJ; Lee CJ; Kang SS
[Ad] Endereço:Department of Anatomy and Convergence Medical Science, Institute of Health Sciences, School of Medicine, Gyeongsang National University, Jinju, Republic of Korea.
[Ti] Título:Trifluoperazine, a Well-Known Antipsychotic, Inhibits Glioblastoma Invasion by Binding to Calmodulin and Disinhibiting Calcium Release Channel IP3R.
[So] Source:Mol Cancer Ther;16(1):217-227, 2017 Jan.
[Is] ISSN:1538-8514
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Calcium (Ca ) 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 release channel inositol 1,4,5-trisphosphate receptor (IP R) 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. However, the possible anticancer effect of TFP on glioblastoma has not been tested. Here, we report that TFP potently suppresses proliferation, motility, and invasion of glioblastoma cells in vitro, and tumor growth in in vivo xenograft mouse model. Unlike caffeine, TFP triggers massive and irreversible release of Ca from intracellular stores by IP R subtype 1 and 2 by directly interacting at the TFP-binding site of a Ca -binding protein, calmodulin subtype 2 (CaM2). TFP binding to CaM2 causes a dissociation of CaM2 from IP R and subsequent opening of IP R. Compared with the control neural stem cells, various glioblastoma cell lines showed enhanced expression of CaM2 and thus enhanced sensitivity to TFP. On the basis of these findings, we propose TFP as a potential therapeutic drug for glioblastoma by aberrantly and irreversibly increasing Ca in glioblastoma cells. Mol Cancer Ther; 16(1); 217-27. ©2016 AACR.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Cálcio/metabolismo
Calmodulina/metabolismo
Glioblastoma/metabolismo
Receptores de Inositol 1,4,5-Trifosfato/metabolismo
Trifluoperazina/farmacologia
[Mh] Termos MeSH secundário: Animais
Calmodulina/antagonistas & inibidores
Linhagem Celular Tumoral
Movimento Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Células Cultivadas
Modelos Animais de Doenças
Retículo Endoplasmático/metabolismo
Glioblastoma/patologia
Seres Humanos
Camundongos
Modelos Biológicos
Metástase Neoplásica
Ligação Proteica
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Calmodulin); 0 (Inositol 1,4,5-Trisphosphate Receptors); 214IZI85K3 (Trifluoperazine); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170629
[Lr] Data última revisão:
170629
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170108
[St] Status:MEDLINE
[do] DOI:10.1158/1535-7163.MCT-16-0169-T


  6 / 3184 MEDLINE  
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[PMID]:27904048
[Au] Autor:Liu D; Wu J; Xie H; Liu M; Takau I; Zhang H; Xiong Y; Xia C
[Ad] Endereço:Clinical Pharmacology Institute, Nanchang University.
[Ti] Título:Inhibitory Effect of Hesperetin and Naringenin on Human UDP-Glucuronosyltransferase Enzymes: Implications for Herb-Drug Interactions.
[So] Source:Biol Pharm Bull;39(12):2052-2059, 2016.
[Is] ISSN:1347-5215
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo: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. Data show that HET and NGR displayed broad-spectrum inhibition against human UGTs. Besides, HET exhibited strong inhibitory effects on UGT1A1, 1A3 and 1A9 (both IC and K values lower than 10 µM), and the inhibitory effects of NGR against three major UGTs, including UGT1A1, 1A3 and 2B7. In a combination of inhibition parameters (K ) and in vivo concentration of HET and NGR, the potential in vivo inhibition magnitude was predicted. Based on the reported maximum plasma concentration of HET and NGR in vivo, these findings indicate the potential herb-drug interactions (HDI) between HET or NGR and the drugs mainly undergoing UGT1A3 or UGT2B7 catalyzed metabolic elimination. Considering the variety of citrus that contains HET and NGR, so caution should be applied when taking drugs that utilize UGTs for metabolism and clearance with citrus fruits.
[Mh] Termos MeSH primário: Citrus
Flavanonas/farmacologia
Glucuronosiltransferase/antagonistas & inibidores
Interações Ervas-Drogas
Hesperidina/farmacologia
[Mh] Termos MeSH secundário: Animais
Linhagem Celular
Glucuronosiltransferase/metabolismo
Seres Humanos
Himecromona/farmacologia
Insetos
Proteínas Recombinantes/metabolismo
Trifluoperazina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Flavanones); 0 (Recombinant Proteins); 214IZI85K3 (Trifluoperazine); 3T5NG4Q468 (Hymecromone); E750O06Y6O (Hesperidin); EC 2.4.1.17 (Glucuronosyltransferase); HN5425SBF2 (naringenin); Q9Q3D557F1 (hesperetin)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161202
[St] Status:MEDLINE


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[PMID]:27693219
[Au] Autor:Cheung S; Thomas CM; Timson DJ
[Ad] Endereço:School of Biological Sciences, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast, BT9 7BL, UK.
[Ti] Título:FhCaBP1 (FH22): A Fasciola hepatica calcium-binding protein with EF-hand and dynein light chain domains.
[So] Source:Exp Parasitol;170:109-115, 2016 Nov.
[Is] ISSN:1090-2449
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo: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. Native gel electrophoresis demonstrated that the protein binds both calcium and manganese ions, but not cadmium, magnesium, strontium, barium, cobalt, copper(II), iron (II), nickel, zinc, lead or potassium ions. Calcium ion binding alters the conformation of the protein and increases its stability towards thermal denaturation. FhCaBP1 is a dimer in solution and calcium ions have no detectable effect on the protein's ability to dimerise. FhCaBP1 binds to the calmodulin antagonists trifluoperazine and chlorpromazine. Overall, the FhCaBP1's biochemical properties are most similar to FhCaBP2 a fact consistent with the close sequence and predicted structural similarity between the two proteins.
[Mh] Termos MeSH primário: Proteínas de Ligação ao Cálcio/química
Dineínas/química
Fasciola hepatica/metabolismo
Proteínas de Helminto/química
[Mh] Termos MeSH secundário: Animais
Cálcio/metabolismo
Proteínas de Ligação ao Cálcio/genética
Proteínas de Ligação ao Cálcio/isolamento & purificação
Proteínas de Ligação ao Cálcio/metabolismo
Calmodulina/antagonistas & inibidores
Clorpromazina/metabolismo
Eletroforese em Gel de Poliacrilamida
Fasciola hepatica/genética
Expressão Gênica
Proteínas de Helminto/genética
Proteínas de Helminto/isolamento & purificação
Proteínas de Helminto/metabolismo
Manganês/metabolismo
Conformação Proteica
Multimerização Proteica
Trifluoperazina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calcium-Binding Proteins); 0 (Calmodulin); 0 (Helminth Proteins); 214IZI85K3 (Trifluoperazine); 42Z2K6ZL8P (Manganese); EC 3.6.4.2 (Dyneins); EC 5.3.4.- (Ca2+-binding protein-1); SY7Q814VUP (Calcium); U42B7VYA4P (Chlorpromazine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170829
[Lr] Data última revisão:
170829
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161004
[St] Status:MEDLINE


  8 / 3184 MEDLINE  
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[PMID]:27666479
[Au] Autor:Kim DH; Lee SJ; Hahn SJ; Choi JS
[Ad] Endereço:College of Pharmacy, The Catholic University of Korea, Bucheon, Gyeonggi-do, 14662, South Korea.
[Ti] Título:Trifluoperazine blocks the human cardiac sodium channel, Na 1.5, independent of calmodulin.
[So] Source:Biochem Biophys Res Commun;479(3):584-589, 2016 Oct 21.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo: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 Na 1.5 (hNa 1.5) 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 hNa 1.5 were completely and repeatedly reversible after washout. Trifluoperazine caused depolarizing shifts in the activation and hyperpolarizing shifts in the steady-state inactivation of hNa 1.5. Trifluoperazine also showed strong use-dependent inhibition of hNa 1.5. The blockade of hNa 1.5 currents by trifluoperazine was not affected by the whole cell dialysis of the calmodulin inhibitory peptide. Our results indicated that trifluoperazine blocks hNa 1.5 current in concentration-, state- and use-dependent manners rather than via calmodulin inhibition.
[Mh] Termos MeSH primário: Canal de Sódio Disparado por Voltagem NAV1.5/metabolismo
Bloqueadores dos Canais de Sódio/química
Trifluoperazina/química
[Mh] Termos MeSH secundário: Antipsicóticos/química
Calmodulina/química
Células HEK293
Seres Humanos
Concentração Inibidora 50
Potenciais da Membrana/efeitos dos fármacos
Técnicas de Patch-Clamp
Peptídeos/química
Diálise Renal
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Calmodulin); 0 (NAV1.5 Voltage-Gated Sodium Channel); 0 (Peptides); 0 (SCN5A protein, human); 0 (Sodium Channel Blockers); 214IZI85K3 (Trifluoperazine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170827
[Lr] Data última revisão:
170827
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160927
[St] Status:MEDLINE


  9 / 3184 MEDLINE  
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[PMID]:27476280
[Au] Autor:Prashanth KN; Swamy N; Basavaiah K
[Ti] Título:RAPID SPECTROPHOTOMETRIC DETERMINATION OF TRIFLUOPERAZINE DIHYDROCHLORIDE AS BASE FORM IN PHARMACEUTICAL FORMULATION THROUGH CHARGE-TRANSFER COMPLEXATION.
[So] Source:Acta Pol Pharm;73(3):627-36, 2016 May-Jun.
[Is] ISSN:0001-6837
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo: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. Beer's law is obeyed over the concentration ranges of 1.5-24.0 pg/mL in PA method and 5.0-80.0 µg/mL in DNP method, with respective molar absorptivity values of 1.03 x 10(4) and 6.91 x 10(3) L mol-1 cm-1. The reaction stoichiometry in both methods was evaluated by Job's method of continuous variations and was found to be 1 : 2 (TFP : PA, TFP : DNP). The developed methods were successfully applied to the determination of TFP in pure form and commercial tablets with good accuracy and precision. Statistical comparison of the results was performed using Student's t-test and F-ratio at 95% confidence level and the results showed no significant difference between the reference and proposed methods with regard to accuracy and precision. Further, the accuracy and reliability of the methods were confirmed by recovery studies via standard addition technique.
[Mh] Termos MeSH primário: Antipsicóticos/análise
Trifluoperazina/análise
[Mh] Termos MeSH secundário: Calibragem
Química Farmacêutica
Indicadores e Reagentes
Reprodutibilidade dos Testes
Espectrofotometria Ultravioleta
Comprimidos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Indicators and Reagents); 0 (Tablets); 214IZI85K3 (Trifluoperazine)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:160801
[Lr] Data última revisão:
160801
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160802
[St] Status:MEDLINE


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[PMID]:27266180
[Au] Autor:Yemets AI; Fedorchuk VV; Blume YB
[Ti] Título:[ENHANCEMENT OF AGROBACTERIAL TRANSFORMATION OF PLANTS USING PROTEIN KINASE INHIBITORS TRIFLUOPERAZINE AND GENISTEIN].
[So] Source:Tsitol Genet;50(1):3-11, 2016 Jan-Feb.
[Is] ISSN:0564-3783
[Cp] País de publicação:Ukraine
[La] Idioma:ukr
[Ab] Resumo:The effect of different concentrations of protein tyrosine kinase inhibitor, genistein and serine/threonine protein kinase inhibitor, trifluoperazine, on the frequency of Agrobacterium-mediated transformation of leaf explants of N. tabacum was investigated. The influence of different concentrations of trifluoperazine in the range from 10 to 300 µM was investigated. It was found that 10 µM trifluoperazine provoked the increase of the frequency of agrobacterial transformation of tobacco leaf disks on 25%. In parallel, the influence of different concentrations of genistein in the range from 10 to 100 µM was investigated. It was found 100 µM genistein provoked the increase of the frequency of agrobacterial transformation of tobacco leaf disks on 12%.
[Mh] Termos MeSH primário: Agrobacterium tumefaciens/genética
Genisteína/farmacologia
Inibidores de Proteínas Quinases/farmacologia
Tabaco/crescimento & desenvolvimento
Transformação Genética/efeitos dos fármacos
Trifluoperazina/farmacologia
[Mh] Termos MeSH secundário: Agrobacterium tumefaciens/efeitos dos fármacos
Relação Dose-Resposta a Droga
Folhas de Planta/efeitos dos fármacos
Folhas de Planta/enzimologia
Folhas de Planta/genética
Folhas de Planta/crescimento & desenvolvimento
Tabaco/efeitos dos fármacos
Tabaco/enzimologia
Tabaco/genética
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Protein Kinase Inhibitors); 214IZI85K3 (Trifluoperazine); DH2M523P0H (Genistein)
[Em] Mês de entrada:1606
[Cu] Atualização por classe:160608
[Lr] Data última revisão:
160608
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160609
[St] Status:MEDLINE



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