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[PMID]:26147897
[Au] Autor:Shi XN; Li H; Yao H; Liu X; Li L; Leung KS; Kung HF; Lu D; Wong MH; Lin MC
[Ad] Endereço:Biotechnology Center, Kunming Medical University, Kunming, Yunnan, China; Department of Medicine, Southwest Guizhou Vocational and Technical College for Nationalities, Guizhou, China.
[Ti] Título:In Silico Identification and In Vitro and In Vivo Validation of Anti-Psychotic Drug Fluspirilene as a Potential CDK2 Inhibitor and a Candidate Anti-Cancer Drug.
[So] Source:PLoS One;10(7):e0132072, 2015.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Hepatocellular carcinoma (HCC) is one of the leading causes of cancer-related deaths worldwide. Surgical resection and conventional chemotherapy and radiotherapy ultimately fail due to tumor recurrence and HCC's resistance. The development of novel therapies against HCC is thus urgently required. The cyclin-dependent kinase (CDK) pathways are important and well-established targets for cancer treatment. In particular, CDK2 is a key factor regulating the cell cycle G1 to S transition and a hallmark for cancers. In this study, we utilized our free and open-source protein-ligand docking software, idock, prospectively to identify potential CDK2 inhibitors from 4,311 FDA-approved small molecule drugs using a repurposing strategy and an ensemble docking methodology. Sorted by average idock score, nine compounds were purchased and tested in vitro. Among them, the anti-psychotic drug fluspirilene exhibited the highest anti-proliferative effect in human hepatocellular carcinoma HepG2 and Huh7 cells. We demonstrated for the first time that fluspirilene treatment significantly increased the percentage of cells in G1 phase, and decreased the expressions of CDK2, cyclin E and Rb, as well as the phosphorylations of CDK2 on Thr160 and Rb on Ser795. We also examined the anti-cancer effect of fluspirilene in vivo in BALB/C nude mice subcutaneously xenografted with human hepatocellular carcinoma Huh7 cells. Our results showed that oral fluspirilene treatment significantly inhibited tumor growth. Fluspirilene (15 mg/kg) exhibited strong anti-tumor activity, comparable to that of the leading cancer drug 5-fluorouracil (10 mg/kg). Moreover, the cocktail treatment with fluspirilene and 5-fluorouracil exhibited the highest therapeutic effect. These results suggested for the first time that fluspirilene is a potential CDK2 inhibitor and a candidate anti-cancer drug for the treatment of human hepatocellular carcinoma. In view of the fact that fluspirilene has a long history of safe human use, our discovery of fluspirilene as a potential anti-HCC drug may present an immediately applicable clinical therapy.
[Mh] Termos MeSH primário: Antipsicóticos/farmacologia
Carcinoma Hepatocelular/tratamento farmacológico
Quinase 2 Dependente de Ciclina/antagonistas & inibidores
Fluspirileno/farmacologia
Neoplasias Hepáticas/tratamento farmacológico
Simulação de Acoplamento Molecular
Proteínas de Neoplasias/antagonistas & inibidores
[Mh] Termos MeSH secundário: Animais
Carcinoma Hepatocelular/enzimologia
Carcinoma Hepatocelular/patologia
Simulação por Computador
Quinase 2 Dependente de Ciclina/metabolismo
Feminino
Fase G1/efeitos dos fármacos
Células Hep G2
Seres Humanos
Neoplasias Hepáticas/enzimologia
Neoplasias Hepáticas/patologia
Camundongos
Camundongos Endogâmicos BALB C
Camundongos Nus
Proteínas de Neoplasias/metabolismo
Fase S/efeitos dos fármacos
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Neoplasm Proteins); C5QA4GLR9M (Fluspirilene); EC 2.7.11.22 (CDK2 protein, human); EC 2.7.11.22 (Cyclin-Dependent Kinase 2)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:150719
[Lr] Data última revisão:
150719
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150707
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0132072


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[PMID]:25788571
[Au] Autor:Enyeart JJ; Enyeart JA
[Ad] Endereço:Department of Neuroscience, Wexner Medical Center, The Ohio State University, Columbus, Ohio enyeart.1@osu.edu.
[Ti] Título:Adrenal fasciculata cells express T-type and rapidly and slowly activating L-type Ca2+ channels that regulate cortisol secretion.
[So] Source:Am J Physiol Cell Physiol;308(11):C899-918, 2015 Jun 01.
[Is] ISSN:1522-1563
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In whole cell patch-clamp recordings, we characterized the L-type Ca(2+) currents in bovine adrenal zona fasciculata (AZF) cells and explored their role, along with the role of T-type channels, in ACTH- and angiotensin II (ANG II)-stimulated cortisol secretion. Two distinct dihydropyridine-sensitive L-type currents were identified, both of which were activated at relatively hyperpolarized potentials. One activated with rapid kinetics and, in conjunction with Northern blotting and PCR, was determined to be Cav1.3. The other, expressed in approximately one-half of AZF cells, activated with extremely slow voltage-dependent kinetics and combined properties not previously reported for an L-type Ca(2+) channel. The T-type Ca(2+) channel antagonist 3,5-dichloro-N-[1-(2,2-dimethyl-tetrahydro-pyran-4-ylmethyl)-4-fluoro-piperidin-4-ylmethyl]-benzamide (TTA-P2) inhibited Cav3.2 current in these cells, as well as ACTH- and ANG II-stimulated cortisol secretion, at concentrations that did not affect L-type currents. In contrast, nifedipine specifically inhibited L-type currents and cortisol secretion, but less effectively than TTA-P2. Diphenylbutylpiperidine Ca(2+) antagonists, including pimozide, penfluridol, and fluspirilene, and the dihydropyridine niguldipine blocked Cav3.2 and L-type currents and inhibited ACTH-stimulated cortisol secretion with similar potency. This study shows that bovine AZF cells express three Ca(2+) channels, the voltage-dependent gating and kinetics of which could orchestrate complex mechanisms linking peptide hormone receptors to cortisol secretion through action potentials or sustained depolarization. The function of the novel, slowly activating L-type channel is of particular interest in this respect. Regardless, the well-correlated selective inhibition of T- and L-type currents and ACTH- and ANG II-stimulated cortisol secretion by TTA-P2 and nifedipine establish the critical importance of these channels in AZF cell physiology.
[Mh] Termos MeSH primário: Potenciais de Ação/efeitos dos fármacos
Canais de Cálcio Tipo L/genética
Canais de Cálcio Tipo T/genética
Cálcio/metabolismo
Hidrocortisona/secreção
Zona Fasciculada/metabolismo
[Mh] Termos MeSH secundário: Hormônio Adrenocorticotrópico/farmacologia
Angiotensina II/farmacologia
Animais
Benzamidas/farmacologia
Bloqueadores dos Canais de Cálcio/farmacologia
Canais de Cálcio Tipo L/metabolismo
Canais de Cálcio Tipo T/metabolismo
Bovinos
AMP Cíclico/farmacologia
Di-Hidropiridinas/farmacologia
Fluspirileno/farmacologia
Expressão Gênica
Microeletrodos
Nifedipino/farmacologia
Técnicas de Patch-Clamp
Penfluridol/farmacologia
Pimozida/farmacologia
Piperidinas/farmacologia
Isoformas de Proteínas/genética
Isoformas de Proteínas/metabolismo
Análise de Célula Única
Zona Fasciculada/citologia
Zona Fasciculada/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (3,5-dichloro-N-(1-(2,2-dimethyltetrahydropyran-4-ylmethyl)-4-fluoropiperidin-4-ylmethyl)benzamide); 0 (Benzamides); 0 (Calcium Channel Blockers); 0 (Calcium Channels, L-Type); 0 (Calcium Channels, T-Type); 0 (Dihydropyridines); 0 (Piperidines); 0 (Protein Isoforms); 11128-99-7 (Angiotensin II); 1HIZ4DL86F (Pimozide); 25TLU22Q8H (Penfluridol); 9002-60-2 (Adrenocorticotropic Hormone); C5QA4GLR9M (Fluspirilene); E0399OZS9N (Cyclic AMP); I9ZF7L6G2L (Nifedipine); SY7Q814VUP (Calcium); WI4X0X7BPJ (Hydrocortisone); Z81N45O25Z (niguldipine)
[Em] Mês de entrada:1508
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150320
[St] Status:MEDLINE
[do] DOI:10.1152/ajpcell.00002.2015


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[PMID]:25377899
[Au] Autor:Patil SP; Pacitti MF; Gilroy KS; Ruggiero JC; Griffin JD; Butera JJ; Notarfrancesco JM; Tran S; Stoddart JW
[Ad] Endereço:NanoBio Laboratory, Department of Chemical Engineering, Widener University, Chester, PA, 19013, USA, spatil@widener.edu.
[Ti] Título:Identification of antipsychotic drug fluspirilene as a potential p53-MDM2 inhibitor: a combined computational and experimental study.
[So] Source:J Comput Aided Mol Des;29(2):155-63, 2015 Feb.
[Is] ISSN:1573-4951
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The inhibition of tumor suppressor p53 protein due to its direct interaction with oncogenic murine double minute 2 (MDM2) protein, plays a central role in almost 50 % of all human tumor cells. Therefore, pharmacological inhibition of the p53-binding pocket on MDM2, leading to p53 activation, presents an important therapeutic target against these cancers expressing wild-type p53. In this context, the present study utilized an integrated virtual and experimental screening approach to screen a database of approved drugs for potential p53-MDM2 interaction inhibitors. Specifically, using an ensemble rigid-receptor docking approach with four MDM2 protein crystal structures, six drug molecules were identified as possible p53-MDM2 inhibitors. These drug molecules were then subjected to further molecular modeling investigation through flexible-receptor docking followed by Prime/MM-GBSA binding energy analysis. These studies identified fluspirilene, an approved antipsychotic drug, as a top hit with MDM2 binding mode and energy similar to that of a native MDM2 crystal ligand. The molecular dynamics simulations suggested stable binding of fluspirilene to the p53-binding pocket on MDM2 protein. The experimental testing of fluspirilene showed significant growth inhibition of human colon tumor cells in a p53-dependent manner. Fluspirilene also inhibited growth of several other human tumor cell lines in the NCI60 cell line panel. Taken together, these computational and experimental data suggest a potentially novel role of fluspirilene in inhibiting the p53-MDM2 interaction. It is noteworthy here that fluspirilene has a long history of safe human use, thus presenting immediate clinical potential as a cancer therapeutic. Furthermore, fluspirilene could also serve as a structurally-novel lead molecule for the development of more potent, small-molecule p53-MDM2 inhibitors against several types of cancer. Importantly, the combined computational and experimental screening protocol presented in this study may also prove useful for screening other commercially-available compound databases for identification of novel, small molecule p53-MDM2 inhibitors.
[Mh] Termos MeSH primário: Neoplasias do Colo/tratamento farmacológico
Fluspirileno/química
Proteínas Proto-Oncogênicas c-mdm2/química
Proteína Supressora de Tumor p53/química
[Mh] Termos MeSH secundário: Animais
Neoplasias do Colo/patologia
Cristalografia por Raios X
Fluspirileno/uso terapêutico
Seres Humanos
Camundongos
Simulação de Acoplamento Molecular
Simulação de Dinâmica Molecular
Ligação Proteica
Proteínas Proto-Oncogênicas c-mdm2/antagonistas & inibidores
Proteína Supressora de Tumor p53/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (TP53 protein, human); 0 (Tumor Suppressor Protein p53); C5QA4GLR9M (Fluspirilene); EC 2.3.2.27 (MDM2 protein, human); EC 2.3.2.27 (Proto-Oncogene Proteins c-mdm2)
[Em] Mês de entrada:1509
[Cu] Atualização por classe:171021
[Lr] Data última revisão:
171021
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141108
[St] Status:MEDLINE
[do] DOI:10.1007/s10822-014-9811-6


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[PMID]:19901552
[Au] Autor:Xia HG; Zhang L; Chen G; Zhang T; Liu J; Jin M; Ma X; Ma D; Yuan J
[Ad] Endereço:State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai, China.
[Ti] Título:Control of basal autophagy by calpain1 mediated cleavage of ATG5.
[So] Source:Autophagy;6(1):61-6, 2010 Jan.
[Is] ISSN:1554-8635
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Autophagy functions as an important catabolic mechanism by mediating the turnover of intracellular organelles and protein complexes. Although the induction of autophagy by starvation has been extensively studied, we still understand very little about how autophagy is regulated under normal nutritional conditions. Here we describe a study using a small molecule autophagy inducer, fluspirilene, as a tool to explore the mechanism of autophagy induction in normal living cells. We confirm the activity of fluspirilene in inhibiting Ca(2+) flux. Furthermore, we show that reducing intracellular Ca(2+) prevents the cleavage of ATG5, which in turn increases the levels of full-length ATG5 and ATG12-ATG5 conjugate. Using siRNA mediated gene silencing, we demonstrate that inhibiting calpain1 is sufficient to induce autophagy in living cells. We conclude that calpain1 plays an important role in controlling the levels of autophagy in normal living cells by regulating the levels of a key signaling molecule, ATG12-ATG5 conjugate.
[Mh] Termos MeSH primário: Autofagia/genética
Calpaína/fisiologia
Proteínas Associadas aos Microtúbulos/metabolismo
[Mh] Termos MeSH secundário: Animais
Autofagia/efeitos dos fármacos
Proteína 12 Relacionada à Autofagia
Proteína 5 Relacionada à Autofagia
Canais de Cálcio/efeitos dos fármacos
Canais de Cálcio/metabolismo
Calpaína/antagonistas & inibidores
Calpaína/genética
Calpaína/metabolismo
Células Cultivadas
Antagonistas de Dopamina/farmacologia
Fluspirileno/farmacologia
Alimentos
Células HeLa
Seres Humanos
Camundongos
Ligação Proteica/efeitos dos fármacos
Processamento de Proteína Pós-Traducional/efeitos dos fármacos
Processamento de Proteína Pós-Traducional/genética
RNA Interferente Pequeno/farmacologia
Proteínas Modificadoras Pequenas Relacionadas à Ubiquitina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (ATG12 protein, human); 0 (ATG5 protein, human); 0 (Autophagy-Related Protein 12); 0 (Autophagy-Related Protein 5); 0 (Calcium Channels); 0 (Dopamine Antagonists); 0 (Microtubule-Associated Proteins); 0 (RNA, Small Interfering); 0 (Small Ubiquitin-Related Modifier Proteins); C5QA4GLR9M (Fluspirilene); EC 3.4.22.- (Calpain); EC 3.4.22.52 (CAPN1 protein, human)
[Em] Mês de entrada:1003
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:091111
[St] Status:MEDLINE


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[PMID]:18606114
[Au] Autor:Wolf F; Scherr M; Scherthöffer D; Bäuml J; Förstl H
[Ad] Endereço:Klinik für Psychiatrie und Psychotherapie, Universitätsklinikum des Saarlandes.
[Ti] Título:[Trichoma (Plica polonica) - a contemporary case with a historical disease].
[Ti] Título:Der Weichselzopf (Plica polonica) - eine aktuelle Kasuistik zu einem historischen Krankheitskonzept..
[So] Source:Neuropsychiatr;22(2):124-6, 2008.
[Is] ISSN:0948-6259
[Cp] País de publicação:Germany
[La] Idioma:ger
[Ab] Resumo:We describe a 62-year-old patient with a chronic delusional disorder who presented with severely matted hair ("plica polonica"). Until the late 19th century such dreadlocks were considered as cause, consequence and treatment of mental disease. The historical development of "plica polonica" is briefly reviewed as an example of early and once popular psychiatric disease concepts.
[Mh] Termos MeSH primário: Doenças do Cabelo/história
Doenças do Cabelo/psicologia
Cabelo
Higiene/história
Transtornos Mentais/história
Esquizofrenia Paranoide/história
Esquizofrenia Paranoide/psicologia
Isolamento Social
[Mh] Termos MeSH secundário: Antipsicóticos/uso terapêutico
Feminino
Fluspirileno/uso terapêutico
Alemanha
Doenças do Cabelo/tratamento farmacológico
História do Século XIX
Seres Humanos
Transtornos Mentais/psicologia
Meia-Idade
Esquizofrenia Paranoide/tratamento farmacológico
[Pt] Tipo de publicação:CASE REPORTS; ENGLISH ABSTRACT; HISTORICAL ARTICLE; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antipsychotic Agents); C5QA4GLR9M (Fluspirilene)
[Em] Mês de entrada:0809
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080709
[St] Status:MEDLINE


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[PMID]:18024584
[Au] Autor:Zhang L; Yu J; Pan H; Hu P; Hao Y; Cai W; Zhu H; Yu AD; Xie X; Ma D; Yuan J
[Ad] Endereço:State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032, China.
[Ti] Título:Small molecule regulators of autophagy identified by an image-based high-throughput screen.
[So] Source:Proc Natl Acad Sci U S A;104(48):19023-8, 2007 Nov 27.
[Is] ISSN:1091-6490
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Autophagy is a lysosome-dependent cellular catabolic mechanism mediating the turnover of intracellular organelles and long-lived proteins. Reduction of autophagy activity has been shown to lead to the accumulation of misfolded proteins in neurons and may be involved in chronic neurodegenerative diseases such as Huntington's disease and Alzheimer's disease. To explore the mechanism of autophagy and identify small molecules that can activate it, we developed a series of high-throughput image-based screens for small-molecule regulators of autophagy. This series of screens allowed us to distinguish compounds that can truly induce autophagic degradation from those that induce the accumulation of autophagosomes as a result of causing cellular damage or blocking downstream lysosomal functions. Our analyses led to the identification of eight compounds that can induce autophagy and promote long-lived protein degradation. Interestingly, seven of eight compounds are FDA-approved drugs for treatment of human diseases. Furthermore, we show that these compounds can reduce the levels of expanded polyglutamine repeats in cultured cells. Our studies suggest the possibility that some of these drugs may be useful for the treatment of Huntington's and other human diseases associated with the accumulation of misfolded proteins.
[Mh] Termos MeSH primário: Autofagia/efeitos dos fármacos
Avaliação Pré-Clínica de Medicamentos/métodos
Proteínas de Fluorescência Verde/análise
Proteínas Associadas aos Microtúbulos/análise
Fagossomos/efeitos dos fármacos
Bibliotecas de Moléculas Pequenas/farmacologia
[Mh] Termos MeSH secundário: Bloqueadores dos Canais de Cálcio/farmacologia
Linhagem Celular Tumoral
Avaliação Pré-Clínica de Medicamentos/instrumentação
Fluspirileno/farmacologia
Glioblastoma/metabolismo
Glioblastoma/patologia
Seres Humanos
Membranas Intracelulares/química
Loperamida/farmacologia
Micotoxinas/farmacologia
Peptídeos/metabolismo
Fagossomos/química
Fosfatos de Fosfatidilinositol/metabolismo
Pimozida/farmacologia
Proteínas Quinases/metabolismo
Proteínas Recombinantes de Fusão/análise
Sirolimo/farmacologia
Serina-Treonina Quinases TOR
Trifluoperazina/farmacologia
Dedos de Zinco/fisiologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Calcium Channel Blockers); 0 (Microtubule-Associated Proteins); 0 (Mycotoxins); 0 (Peptides); 0 (Phosphatidylinositol Phosphates); 0 (Recombinant Fusion Proteins); 0 (Small Molecule Libraries); 0 (light chain 3, human); 0 (phosphatidylinositol 3,4,5-triphosphate); 147336-22-9 (Green Fluorescent Proteins); 1HIZ4DL86F (Pimozide); 214IZI85K3 (Trifluoperazine); 26700-71-0 (polyglutamine); 37203-49-9 (tremortin); 6X9OC3H4II (Loperamide); C5QA4GLR9M (Fluspirilene); EC 2.7.- (Protein Kinases); EC 2.7.1.1 (MTOR protein, human); EC 2.7.1.1 (TOR Serine-Threonine Kinases); W36ZG6FT64 (Sirolimus)
[Em] Mês de entrada:0801
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:071121
[St] Status:MEDLINE


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[PMID]:17253464
[Au] Autor:Abhijnhan A; Adams CE; David A; Ozbilen M
[Ad] Endereço:Cochrane Schizophrenia Group, Academic unit of Psychiatry and Behavioural Sciences, 15 Hyde Terrace, Leeds, UK, LS2 9LT. akhil.abith@gmail.com
[Ti] Título:Depot fluspirilene for schizophrenia.
[So] Source:Cochrane Database Syst Rev;(1):CD001718, 2007 Jan 24.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Antipsychotic drugs are the mainstay treatment for schizophrenia and similar psychotic disorders. Long-acting depot injections of drugs such as fluspirilene are extensively used as a means of long-term maintenance treatment. OBJECTIVES: To review the effects of depot fluspirilene versus placebo, oral anti-psychotics and other depot antipsychotic preparations for people with schizophrenia in terms of clinical, social and economic outcomes. SEARCH STRATEGY: We searched the Cochrane Schizophrenia Group's Register (September 2005), inspected references of all identified studies, and contacted relevant pharmaceutical companies. SELECTION CRITERIA: We included all relevant randomised trials focusing on people with schizophrenia where depot fluspirilene, oral anti-psychotics, other depot preparations, or placebo were compared. Outcomes such as death, clinically significant change in global function, mental state, relapse, hospital admission, adverse effects and acceptability of treatment were sought. DATA COLLECTION AND ANALYSIS: Studies were reliably selected, quality rated and data extracted. For dichotomous data, we calculated relative risk (RR) with the 95% confidence intervals (CI). Where possible, the number needed to treat statistic (NNT) was calculated. Analysis was by intention-to-treat. We summated normal continuous data using the weighted mean difference (WMD). We presented scale data only for those tools that had attained pre-specified levels of quality. MAIN RESULTS: We included twelve randomised studies in this update of which five are additional studies. One trial compared fluspirilene and placebo and did not report important differences in the global improvement (n=60, 1 RCT, RR "no important improvement "0.97 CI 0.9 to 1.1). Though movement disorders (n=60, 1 RCT, RR 31.0 CI 1.9 to 495.6, NNH 4) were found only in the fluspirilene group, there were no convincing data showing the advantage of oral chlorpromazine or other depot antipsychotics over fluspirilene decanoate. We found no difference between depot fluspirilene and other oral antipsychotics with regard to relapses or to the number of people leaving the study early. Global state data (CGI) were not significantly different, in the short term when comparing fluspirilene with other depots (n=90, 2 RCTs, RR "no important improvement" 0.80 CI 0.2 to 2.8). No significant difference were apparent between fluspirilene and other depots with respect to the number of people leaving the trial early (n=83, 2 RCTs, RR 0.55 CI 0.1 to 2.3) or relapse rates (n=109, 3 RCTs, RR 0.55 CI 0.1 to 2.3). Extrapyramidal adverse effects were significantly less prevalent in the fluspirilene groups (n=164, 4 RCTs, RR 0.50 CI 0.3 to 0.8, NNH 5). Other adverse effects were not significantly different. Attrition in the one comparison between fluspirilene in weekly versus biweekly administration (n=34, RR 3.00 CI 0.1 to 68.8) and relapse rates (n=34 RR 3.18 CI 0.1 to 83.8) were not significantly different. There were no significant difference for movement disorders in one short term study. No study reported on hospital and service outcomes or commented on participants' overall satisfaction with care. Economic outcomes were not recorded by any of the included studies. AUTHORS' CONCLUSIONS: Participant numbers in each comparison were small and we found no clear differences between fluspirilene and oral medication or other depots. The choice of whether to use fluspirilene as a depot medication and whether it has advantages over other depots cannot, at present, be informed by trial-derived data. Well-conducted and reported randomised trials are still needed to inform practice.
[Mh] Termos MeSH primário: Antipsicóticos/uso terapêutico
Fluspirileno/uso terapêutico
Esquizofrenia/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração Oral
Antipsicóticos/administração & dosagem
Preparações de Ação Retardada/administração & dosagem
Preparações de Ação Retardada/uso terapêutico
Fluspirileno/administração & dosagem
Seres Humanos
Injeções Intramusculares
Ensaios Clínicos Controlados Aleatórios como Assunto
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; REVIEW
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Delayed-Action Preparations); C5QA4GLR9M (Fluspirilene)
[Em] Mês de entrada:0705
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:070127
[St] Status:MEDLINE


  8 / 106 MEDLINE  
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[PMID]:16766676
[Au] Autor:Zalejski C; Paradis S; Maldiney R; Habricot Y; Miginiac E; Rona JP; Jeannette E
[Ad] Endereço:Université Pierre et Marie Curie-Paris 6 and Centre National de la Recherche Scientifique, FRE 2846, Physiologie Cellulaire et Moléculaire des Plantes, F-94200 Ivry-sur-Seine, France.
[Ti] Título:Induction of abscisic acid-regulated gene expression by diacylglycerol pyrophosphate involves Ca2+ and anion currents in Arabidopsis suspension cells.
[So] Source:Plant Physiol;141(4):1555-62, 2006 Aug.
[Is] ISSN:0032-0889
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Diacylglycerol pyrophosphate (DGPP) was recently shown to be a possible intermediate in abscisic acid (ABA) signaling. In this study, reverse transcription-PCR of ABA up-regulated genes was used to evaluate the ability of DGPP to trigger gene expression in Arabidopsis (Arabidopsis thaliana) suspension cells. At5g06760, LTI30, RD29A, and RAB18 were stimulated by ABA and also specifically expressed in DGPP-treated cells. Use of the Ca2+ channel blockers fluspirilene and pimozide and the Ca2+ chelator EGTA showed that Ca2+ was required for ABA induction of DGPP formation. In addition, Ca2+ participated in DGPP induction of gene expression via stimulation of anion currents. Hence, a sequence of Ca2+, DGPP, and anion currents, constituting a core of early ABA-signaling events necessary for gene expression, is proposed.
[Mh] Termos MeSH primário: Ácido Abscísico/metabolismo
Proteínas de Arabidopsis/genética
Arabidopsis/genética
Cálcio/fisiologia
Difosfatos/metabolismo
Regulação da Expressão Gênica de Plantas
Glicerol/análogos & derivados
[Mh] Termos MeSH secundário: Ânions/metabolismo
Arabidopsis/citologia
Arabidopsis/fisiologia
Proteínas de Arabidopsis/metabolismo
Cálcio/metabolismo
Bloqueadores dos Canais de Cálcio/farmacologia
Técnicas de Cultura de Células
Células Cultivadas
Quelantes/farmacologia
Ácido Egtázico/farmacologia
Fluspirileno/farmacologia
Regulação da Expressão Gênica de Plantas/efeitos dos fármacos
Glicerol/metabolismo
Potenciais da Membrana
Pimozida/farmacologia
Transdução de Sinais
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anions); 0 (Arabidopsis Proteins); 0 (Calcium Channel Blockers); 0 (Chelating Agents); 0 (Diphosphates); 0 (diacylglycerol pyrophosphate); 1HIZ4DL86F (Pimozide); 526U7A2651 (Egtazic Acid); 72S9A8J5GW (Abscisic Acid); C5QA4GLR9M (Fluspirilene); PDC6A3C0OX (Glycerol); SY7Q814VUP (Calcium)
[Em] Mês de entrada:0611
[Cu] Atualização por classe:170219
[Lr] Data última revisão:
170219
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:060613
[St] Status:MEDLINE


  9 / 106 MEDLINE  
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[PMID]:12457021
[Au] Autor:Baethge C
[Ad] Endereço:Department of Psychiatry and Psychotherapy, Freie Universität Berlin, Germany. christopher.baethge@medizin.fu-berlin.de
[Ti] Título:Grief hallucinations: true or pseudo? Serious or not? An inquiry into psychopathological and clinical features of a common phenomenon.
[So] Source:Psychopathology;35(5):296-302, 2002 Sep-Oct.
[Is] ISSN:0254-4962
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:An inquiry into the psychopathology and the clinical significance of grief hallucinations is presented and two cases with severe grief hallucinations are described. Unlike many cases in the literature, the two female patients were young (aged 43 and 45, respectively) and both suffered from the loss of a daughter. The heterogeneous concept of grief hallucinations is described and discussed, focusing particularly on the difficulties of reaching a differentiation between hallucination and pseudohallucination. Basic theses of the article are: (1) Contrary to a widely held view, grief hallucinations can display all the characteristics of 'true' hallucinations. (2) The concept of grief hallucinations probably comprises a heterogeneous group of disturbances of perception and of thought processes. They can be experienced as comforting but can also cause considerable distress. (3) There are essentially two definitions of pseudohallucinations and they contradict each other. The extremely vague concept of pseudohallucinations appears to be of questionable value and should be abandoned.
[Mh] Termos MeSH primário: Pesar
Alucinações/psicologia
[Mh] Termos MeSH secundário: Adulto
Antipsicóticos/uso terapêutico
Luto
Feminino
Fluspirileno/uso terapêutico
Alucinações/tratamento farmacológico
Seres Humanos
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antipsychotic Agents); C5QA4GLR9M (Fluspirilene)
[Em] Mês de entrada:0304
[Cu] Atualização por classe:171101
[Lr] Data última revisão:
171101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:021129
[St] Status:MEDLINE


  10 / 106 MEDLINE  
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[PMID]:11842444
[Au] Autor:Wang SJ
[Ad] Endereço:School of Medicine, Fu Jen Catholic University, Hsin-Chuang, Taipei Hsien, Taiwan 24205. med0003@mails.fju.edu.tw
[Ti] Título:Inhibition of glutamate release by fluspirilene in cerebrocortical nerve terminals (synaptosomes).
[So] Source:Synapse;44(1):36-41, 2002 Apr.
[Is] ISSN:0887-4476
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Fluspirilene, a neuroleptic drug which is used clinically to treat schizophrenic patients, is a dopamine D2 receptor antagonist. Besides its well-known actions on the dopamine receptors, fluspirilene also displays calcium channel-blocking activity. The aim of this study was to investigate the effect of fluspirilene on the 4-aminopyridine (4AP)-evoked glutamate release in the cerebrocortical nerve terminals (synaptosomes). Fluspirilene reduced 4AP-evoked glutamate release in a concentration-dependent manner. This inhibitory effect was associated with a decrease in the depolarization-evoked increase in the cytoplasmic free Ca2+ concentration ([Ca2+]C), which could be completely abolished by the Ca2+ channel blocker omega-CgTX GVIA. Furthermore, fluspirilene did not produce any effect on ionomycin-evoked glutamate release. These results suggest that fluspirilene inhibits glutamate release primarily by reducing presynaptic Ca2+ influx via N-type Ca2+ channels in rat cerebrocortical nerve terminals. This finding implies that presynaptic Ca2+ channel blockade concomitant with inhibition of glutamate release and possibly other neurotransmitters release may contribute to the antischizophrenic action of fluspirilene.
[Mh] Termos MeSH primário: Canais de Cálcio Tipo N/efeitos dos fármacos
Sinalização do Cálcio/efeitos dos fármacos
Córtex Cerebral/efeitos dos fármacos
Antagonistas de Dopamina/farmacologia
Fluspirileno/farmacologia
Ácido Glutâmico/secreção
Terminações Pré-Sinápticas/efeitos dos fármacos
[Mh] Termos MeSH secundário: 4-Aminopiridina/farmacologia
Animais
Cálcio/metabolismo
Bloqueadores dos Canais de Cálcio/farmacologia
Canais de Cálcio Tipo N/metabolismo
Sinalização do Cálcio/fisiologia
Córtex Cerebral/metabolismo
Córtex Cerebral/secreção
Interações Medicamentosas
Ácido Glutâmico/metabolismo
Ionóforos/farmacologia
Masculino
Bloqueadores dos Canais de Potássio/farmacologia
Terminações Pré-Sinápticas/metabolismo
Terminações Pré-Sinápticas/secreção
Ratos
Ratos Sprague-Dawley
Transmissão Sináptica/efeitos dos fármacos
Transmissão Sináptica/fisiologia
Sinaptossomos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Calcium Channel Blockers); 0 (Calcium Channels, N-Type); 0 (Dopamine Antagonists); 0 (Ionophores); 0 (Potassium Channel Blockers); 3KX376GY7L (Glutamic Acid); BH3B64OKL9 (4-Aminopyridine); C5QA4GLR9M (Fluspirilene); SY7Q814VUP (Calcium)
[Em] Mês de entrada:0205
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:020214
[St] Status:MEDLINE



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