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[PMID]:27260201
[Au] Autor:Liu KS; Chen YW; Aljuffali IA; Chang CW; Wang JJ; Fang JY
[Ad] Endereço:Department of Pharmacy, Chia Nan University of Pharmacy and Science, Tainan, Taiwan.
[Ti] Título:Topically applied mesoridazine exhibits the strongest cutaneous analgesia and minimized skin disruption among tricyclic antidepressants: The skin absorption assessment.
[So] Source:Eur J Pharm Biopharm;105:59-68, 2016 Aug.
[Is] ISSN:1873-3441
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Tricyclic antidepressants (TCAs) are found to have an analgesic action for relieving cutaneous pain associated with neuropathies. The aim of this study was to assess cutaneous absorption and analgesia of topically applied TCAs. Percutaneous delivery was investigated using nude mouse and pig skin models at both infinite and saturated doses. We evaluated the cutaneous analgesia in nude mice using the pinprick scores. Among five antidepressants tested in the in vitro experiment, mesoridazine, promazine and doxepin showed a superior total absorption percentage. The drug with the lowest total absorption percentage was found to be fluphenazine (<7%) either at an infinite dose or at saturated solubility. The follicular pathway was important for mesoridazine and promazine delivery. Mesoridazine showed stronger skin analgesia than the other TCAs although the in vivo skin absorption of mesoridazine (0.34nmol/mg) was less than that of promazine (0.80nmol/mg) and doxepin (0.74nmol/mg). Mesoridazine had a prolonged duration of pain relief (165min) compared to promazine (83min) and doxepin (17min). The skin irritation test demonstrated an evident barrier function deterioration and cutaneous erythema by promazine and doxepin treatment, whereas mesoridazine caused no obvious adverse effect by topical application for up to 7days.
[Mh] Termos MeSH primário: Analgesia
Antidepressivos Tricíclicos/administração & dosagem
Mesoridazina/administração & dosagem
Absorção Cutânea
[Mh] Termos MeSH secundário: Administração Tópica
Animais
Feminino
Camundongos
Camundongos Nus
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antidepressive Agents, Tricyclic); 5XE4NWM740 (Mesoridazine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170303
[Lr] Data última revisão:
170303
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160605
[St] Status:MEDLINE


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[PMID]:24732149
[Au] Autor:Im SH; Park MJ; Seo H; Choi SH; Kim SK; Ahn SH
[Ad] Endereço:Department of Drug Discovery Platform Technology, Korea Research Institute of Chemical Technology (KRICT), Daejeon, Republic of Korea; College of Pharmacy, Chungnam National University, Daejeon, Republic of Korea.
[Ti] Título:Determination of mesoridazine by liquid chromatography-tandem mass spectrometry and its application to pharmacokinetic study in rats.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;958:117-23, 2014 May 01.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The object of the present study was to develop and validate an assay method of mesoridazine in rat plasma using liquid chromatography-tandem mass spectrometry (LC-MS/MS). Plasma samples from rats were prepared by simple protein precipitation and injected onto the LC-MS/MS system for quantification. Mesoridazine and chlorpromazine as an internal standard (IS) were separated by a reversed phase C18 column. A mobile phase was composed of 10mM ammonium formate in water and acetonitrile (ACN) (v/v) by a linear gradient system, increasing the percentage of ACN from 2% at 0.4min to 98% at 2.5min with 4min total run time. The ion transitions monitored in positive-ion mode [M+H](+) of multiple-reaction monitoring (MRM) were m/z 387>126 for mesoridazine and m/z 319>86 for IS. The detector response was specific and linear for mesoridazine at concentrations within the range 0.001-4µg/ml and the correlation coefficient (R(2)) was greater than 0.999 and the signal-to-noise ratios for the samples were ≥10. The intra- and inter-day precision and accuracy of the method were determined to be within the acceptance criteria for assay validation guidelines. The matrix effects were approximately 101 and 99.5% from rat plasma for mesoridazine and chlorpromazine, respectively. Mesoridazine was stable under various processing and/or handling conditions. Mesoridazine concentrations were readily measured in rat plasma samples after intravenous and oral administration. This assay method can be practically useful to the pharmacokinetic and/or toxicokinetic studies of mesoridazine.
[Mh] Termos MeSH primário: Antipsicóticos/sangue
Cromatografia Líquida de Alta Pressão/métodos
Mesoridazina/sangue
Ratos/sangue
[Mh] Termos MeSH secundário: Animais
Precipitação Química
Cromatografia Líquida de Alta Pressão/economia
Masculino
Ratos Sprague-Dawley
Espectrometria de Massas em Tandem/economia
Espectrometria de Massas em Tandem/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Antipsychotic Agents); 5XE4NWM740 (Mesoridazine)
[Em] Mês de entrada:1412
[Cu] Atualização por classe:140428
[Lr] Data última revisão:
140428
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140416
[St] Status:MEDLINE


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[PMID]:20395863
[Au] Autor:Baek JH; McKenzie S; Garcia-Aguilar J; Pigazzi A
[Ad] Endereço:Department of Surgery, Gachon University of Medicine and Science, Gil Medical Center, Namdong-gu, Incheon, Korea.
[Ti] Título:Oncologic outcomes of robotic-assisted total mesorectal excision for the treatment of rectal cancer.
[So] Source:Ann Surg;251(5):882-6, 2010 May.
[Is] ISSN:1528-1140
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To evaluate local recurrence and survival after robotic-assisted total mesorectal excision (RTME) for primary rectal cancer. SUMMARY BACKGROUND DATA: RTME is a novel approach for the treatment of rectal cancer and has been shown to be safe and effective. However, the oncologic results of this approach have not been reported in terms of local recurrence and survival rate. METHODS: Sixty-four consecutive rectal cancer patients with stage I-III disease treated between November 2004 and June 2008 were analyzed prospectively. RESULTS: All patients underwent RTME: 34 had colorectal anastomosis, 18 underwent coloanal anastomosis, and 12 received abdominoperineal resection. Operative mortality rate was 0%. The median operative time was 270 min and median blood loss was 200 mL. The conversion rate was 9.4%. Anastomotic leakage occurred in 4 of 52 (7.7%) patients with anastomosis. Median number of harvested lymph nodes was 14.5. Median distal margin of tumor was 3.4 cm. The circumferential resection margin was negative in all surgical specimens. No port-site recurrence occurred in any patient. Six patients developed recurrence: 2 combined local and distant, and 4 distal alone (mean follow-up of 20.2 months; range, 1.7-52.5). None of the patients developed isolated local recurrence. The mean time to local recurrence was 23 months. The 3-year overall and disease-free survival rates were 96.2% and 73.7%, respectively. CONCLUSIONS: RTME can be carried out safely and effectively in terms of recurrence and survival rates. Further prospective randomized trials are necessary to better define the absolute benefits and limitations of robotic rectal surgery.
[Mh] Termos MeSH primário: Procedimentos Cirúrgicos do Sistema Digestório/métodos
Neoplasias Retais/cirurgia
Robótica
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Intervalo Livre de Doença
Feminino
Seres Humanos
Masculino
Mesoridazina
Meia-Idade
Recidiva Local de Neoplasia/epidemiologia
Estudos Prospectivos
Neoplasias Retais/mortalidade
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
5XE4NWM740 (Mesoridazine)
[Em] Mês de entrada:1005
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:100417
[St] Status:MEDLINE
[do] DOI:10.1097/SLA.0b013e3181c79114


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[PMID]:19604081
[Au] Autor:Dorado P; Peñas-LLedó EM; de la Rubia A; LLerena A
[Ad] Endereço:CICAB Centro de Investigación Clínica, Area de Salud de Badajoz, Servicio Extremeño de Salud, Hospital Universitario Infanta Cristina, Badajoz, Spain.
[Ti] Título:Relevance of CYP2D6 -1584C>G polymorphism for thioridazine:mesoridazine plasma concentration ratio in psychiatric patients.
[So] Source:Pharmacogenomics;10(7):1083-9, 2009 Jul.
[Is] ISSN:1744-8042
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:AIMS: The CYP2D6 -1584C>G (rs1080985) polymorphism has been identified as another major factor for CYP2D6 function that is possibly associated with ultrarapid metabolism. The mutant -1584G promoter genotype seems to be consistently related to a higher protein expression than -1584C. However, the impact this SNP in the CYP2D6 promoter region has on plasma levels of patients taking CYP2D6 substrates, such as thioridazine, has not been studied. Previously, we showed the validity of the mesoridazine:thioridazine ratio to assess CYP2D6 activity in clinical settings. Therefore, the aim of this study was to analyze the relationship between the presence of the CYP2D6 -1584C>G polymorphism and the plasma concentrations of thioridazine and its metabolites in a previously studied population of patients in order to evaluate the implications for CYP2D6 hydroxylation capacity. MATERIALS & METHODS: The CYP2D6 -1584C>G polymorphism was determined by using a PCR-RFLP method in 61 Caucasian psychiatric patients receiving thioridazine monotherapy. RESULTS: Among patients with two active CYP2D6 genes, there were significant differences in the thioridazine:mesoridazine plasma concentrations ratio (p < 0.05) among the three CYP2D6 -1584C>G genotype groups. Moreover, in this group of patients the thioridazine:mesoridazine ratio was lower (p < 0.05) in carriers of CYP2D6 -1584G allele than in patients homozygous for CYP2D6 -1584C allele. However, no differences in thioridazine or its metabolite concentrations between homozygous CYP2D6 -1584C allele carriers and carriers of the -1584G allele were found. CONCLUSION: According to the present results the concentration ratio of thioridazine to mesoridazine was related to the CYP2D6 -1584C>G polymorphism. It is likely that individuals who carry CYP2D6 -1584G versus homozygotes for the -1584C allele may present an increased CYP2D6 activity.
[Mh] Termos MeSH primário: Antipsicóticos/sangue
Citocromo P-450 CYP2D6/genética
Citocromo P-450 CYP2D6/metabolismo
Transtornos Mentais/tratamento farmacológico
Transtornos Mentais/genética
Mesoridazina/sangue
Polimorfismo de Nucleotídeo Único/genética
Tioridazina/sangue
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Alelos
Feminino
Triagem de Portadores Genéticos
Genótipo
Seres Humanos
Masculino
Transtornos Mentais/sangue
Transtornos Mentais/enzimologia
Meia-Idade
Mutação
Especificidade por Substrato/genética
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antipsychotic Agents); 5XE4NWM740 (Mesoridazine); EC 1.14.14.1 (Cytochrome P-450 CYP2D6); N3D6TG58NI (Thioridazine)
[Em] Mês de entrada:1003
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090717
[St] Status:MEDLINE
[do] DOI:10.2217/pgs.09.57


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[PMID]:17460606
[Au] Autor:Thanacoody RH; Daly AK; Reilly JG; Ferrier IN; Thomas SH
[Ad] Endereço:School of Clinical and Laboratory Sciences, University of Newcastle, Newcastle upon Tyne, UK.
[Ti] Título:Factors affecting drug concentrations and QT interval during thioridazine therapy.
[So] Source:Clin Pharmacol Ther;82(5):555-65, 2007 Nov.
[Is] ISSN:1532-6535
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The objective of this study was to investigate factors affecting steady-state plasma concentrations of thioridazine. A cross-sectional study of patients receiving chronic thioridazine was employed. Common allelic variants of CYP2D6 and CYP2C19, as well as thioridazine and metabolite concentrations and QTc intervals, were determined. In 97 patients, dose-corrected plasma concentrations (C/Ds) of thioridazine and metabolites were correlated with age but not sex or CYP2C19 genotype. Patients with no functional CYP2D6 alleles (n=9) had significantly higher C/D for thioridazine (P=0.017) and the ring sulfoxide metabolite and a significantly higher thioridazine/mesoridazine ratio compared with those with >/=1 functional CYP2D6 allele (n=82). Smokers had significantly lower C/D for thioridazine, mesoridazine, and sulforidazine and significantly lower thioridazine/ring sulfoxide ratios than non-smokers. QTc interval was not significantly affected by CYP2D6 or CYP2C19 genotypes. Plasma concentrations of thioridazine are influenced by age, smoking, and CYP2D6 genotype, but CYP2D6 genotype does not appear to influence on-treatment QTc interval.
[Mh] Termos MeSH primário: Antipsicóticos/efeitos adversos
Antipsicóticos/sangue
Sistema de Condução Cardíaco/efeitos dos fármacos
Síndrome do QT Longo/induzido quimicamente
Tioridazina/efeitos adversos
Tioridazina/sangue
[Mh] Termos MeSH secundário: Adulto
Fatores Etários
Idoso
Idoso de 80 Anos ou mais
Alelos
Antipsicóticos/administração & dosagem
Antipsicóticos/farmacocinética
Hidrocarboneto de Aril Hidroxilases/genética
Hidrocarboneto de Aril Hidroxilases/metabolismo
Estudos Transversais
Citocromo P-450 CYP2C19
Citocromo P-450 CYP2D6/genética
Citocromo P-450 CYP2D6/metabolismo
Antagonistas de Dopamina/efeitos adversos
Antagonistas de Dopamina/sangue
Grupo com Ancestrais do Continente Europeu/genética
Feminino
Variação Genética
Genótipo
Seres Humanos
Modelos Lineares
Síndrome do QT Longo/sangue
Síndrome do QT Longo/fisiopatologia
Masculino
Mesoridazina/efeitos adversos
Mesoridazina/sangue
Meia-Idade
Oxigenases de Função Mista/genética
Oxigenases de Função Mista/metabolismo
Fatores de Risco
Esquizofrenia/tratamento farmacológico
Fatores Sexuais
Fumar/efeitos adversos
Tioridazina/administração & dosagem
Tioridazina/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Dopamine Antagonists); 5XE4NWM740 (Mesoridazine); EC 1.- (Mixed Function Oxygenases); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (CYP2C19 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP2C19); EC 1.14.14.1 (Cytochrome P-450 CYP2D6); N3D6TG58NI (Thioridazine)
[Em] Mês de entrada:0711
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:070427
[St] Status:MEDLINE


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[PMID]:17410120
[Au] Autor:Salih IS; Thanacoody RH; McKay GA; Thomas SH
[Ad] Endereço:School of Clinical and Laboratory Sciences, University of Newcastle, Newcastle-upon-Tyne, Newcastle, UK.
[Ti] Título:Comparison of the effects of thioridazine and mesoridazine on the QT interval in healthy adults after single oral doses.
[So] Source:Clin Pharmacol Ther;82(5):548-54, 2007 Nov.
[Is] ISSN:1532-6535
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:We compared the effects of single doses of thioridazine and mesoridazine on the heart rate-corrected QT (QTc) interval in healthy adult volunteers. QTc intervals and plasma concentrations of thioridazine, mesoridazine, and metabolites were measured after single oral doses of thioridazine hydrochloride 50 mg, mesoridazine besylate 50 mg, or placebo in a double-blind, crossover study. Mean maximum increases in the QTc interval following thioridazine (37.3+/-4.1 ms, P=0.023) and mesoridazine (46.6+/-7.4 ms, P=0.021) were similar and significantly greater than following placebo (12.9+/-8.1 ms). The area under the effect-time curve over 8 h following drug administration was similar between the two drugs (129.3+/-22.1 vs 148.3+/-43.0 ms h). In conclusion, thioridazine and mesoridazine are associated with similar effects on the QTc interval.
[Mh] Termos MeSH primário: Antipsicóticos/efeitos adversos
Antagonistas de Dopamina/efeitos adversos
Sistema de Condução Cardíaco/efeitos dos fármacos
Mesoridazina/efeitos adversos
Tioridazina/efeitos adversos
[Mh] Termos MeSH secundário: Administração Oral
Adulto
Antipsicóticos/administração & dosagem
Antipsicóticos/sangue
Antipsicóticos/farmacocinética
Área Sob a Curva
Estudos Cross-Over
Antagonistas de Dopamina/administração & dosagem
Antagonistas de Dopamina/sangue
Antagonistas de Dopamina/farmacocinética
Método Duplo-Cego
Eletrocardiografia
Feminino
Seres Humanos
Síndrome do QT Longo/induzido quimicamente
Síndrome do QT Longo/fisiopatologia
Masculino
Mesoridazina/administração & dosagem
Mesoridazina/sangue
Mesoridazina/farmacocinética
Meia-Idade
Valores de Referência
Tioridazina/administração & dosagem
Tioridazina/sangue
Tioridazina/farmacocinética
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Dopamine Antagonists); 5XE4NWM740 (Mesoridazine); N3D6TG58NI (Thioridazine)
[Em] Mês de entrada:0711
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:070406
[St] Status:MEDLINE


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[PMID]:17345072
[Au] Autor:Dorado P; Berecz R; Peñas-Lledó EM; de la Rubia A; Llerena A
[Ti] Título:No effect of the CYP1A2*1F genotype on thioridazine, mesoridazine, sulforidazine plasma concentrations in psychiatric patients.
[So] Source:Eur J Clin Pharmacol;63(5):527-8, 2007 May.
[Is] ISSN:0031-6970
[Cp] País de publicação:Germany
[La] Idioma:eng
[Mh] Termos MeSH primário: Antipsicóticos/farmacocinética
Mesoridazina/sangue
Fenotiazinas/sangue
Tioridazina/farmacocinética
[Mh] Termos MeSH secundário: Alelos
Antipsicóticos/administração & dosagem
Citocromo P-450 CYP1A2
Debrisoquina/metabolismo
Relação Dose-Resposta a Droga
Genótipo
Seres Humanos
Transtornos Mentais
Reação em Cadeia da Polimerase
Polimorfismo Genético
Polimorfismo de Fragmento de Restrição
Fumar
Tioridazina/administração & dosagem
[Pt] Tipo de publicação:CLINICAL TRIAL; LETTER; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Phenothiazines); 5XE4NWM740 (Mesoridazine); B7599I244X (sulforidazine); EC 1.14.14.1 (Cytochrome P-450 CYP1A2); N3D6TG58NI (Thioridazine); X31CDK040E (Debrisoquin)
[Em] Mês de entrada:0708
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:070309
[St] Status:MEDLINE


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[PMID]:17042915
[Au] Autor:Limberis JT; Su Z; Cox BF; Gintant GA; Martin RL
[Ad] Endereço:Department of Integrative Pharmacology, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064-6119, USA. james.limberis@abbott.com
[Ti] Título:Altering extracellular potassium concentration does not modulate drug block of human ether-a-go-go-related gene (hERG) channels.
[So] Source:Clin Exp Pharmacol Physiol;33(11):1059-65, 2006 Nov.
[Is] ISSN:0305-1870
[Cp] País de publicação:Australia
[La] Idioma:eng
[Ab] Resumo:1. Drug-induced block of the rapidly activating delayed rectifier K+ current (I(Kr)), encoded by human ether-a-go-go-related gene (hERG), has been linked to acquired long QT syndrome (aLQTS). Hypokalaemia is a recognized risk factor in aLQTS. To further understand why hypokalaemia is a risk factor in aLQTS, we examined the effect of [K+]o on drug block of the hERG potassium channel stably expressed in human embryonic kidney (HEK-293) cells using whole-cell voltage-clamp techniques. 2. The effects of selected [K+]o (1-20 mmol/L) on hERG block with four structurally diverse compounds (dofetilide, mesoridazine, quinidine and terfenadine) from different therapeutic classes were evaluated. Reducing [K+]o from 20 to 1 mmol/L had little effect on IC50 values for hERG current block for all four compounds. For example, evaluating quinidine in external potassium concentrations of 20, 10, 5 and 1 mmol/L resulted in IC50 values of 1.82 +/- 0.33, 2.04 +/- 0.28, 1.57 +/- 0.52 and 1.14 +/- 0.21 mmol/L, respectively. No statistically significant difference (P > 0.35, anova) was observed between drug block of hERG in different external potassium concentrations. These data are in contrast with previously reported results examining hERG channel modulation expressed in AT-1 cells under similar experimental conditions. 3. These results demonstrate that [K+]o does not directly modulate drug block of hERG channels expressed in an HEK-293 cell line. The enhanced risk of Torsades de Pointes associated with hypokalaemia in aLQTS may be due to reduction of other (non-hERG) potassium currents, further reducing the repolarization reserve, and not due to direct modulation of hERG block by [K+]o.
[Mh] Termos MeSH primário: Canais de Potássio Éter-A-Go-Go/metabolismo
Rim/efeitos dos fármacos
Bloqueadores dos Canais de Potássio/farmacologia
Potássio/farmacologia
[Mh] Termos MeSH secundário: Linhagem Celular
Canal de Potássio ERG1
Seres Humanos
Rim/citologia
Mesoridazina/farmacologia
Fenetilaminas/farmacologia
Quinidina/farmacologia
Sulfonamidas/farmacologia
Terfenadina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ERG1 Potassium Channel); 0 (Ether-A-Go-Go Potassium Channels); 0 (KCNH2 protein, human); 0 (Phenethylamines); 0 (Potassium Channel Blockers); 0 (Sulfonamides); 5XE4NWM740 (Mesoridazine); 7BA5G9Y06Q (Terfenadine); ITX08688JL (Quinidine); R4Z9X1N2ND (dofetilide); RWP5GA015D (Potassium)
[Em] Mês de entrada:0702
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:061018
[St] Status:MEDLINE


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[PMID]:15357957
[Au] Autor:Choi S; Haggart D; Toll L; Cuny GD
[Ad] Endereço:Laboratory for Drug Discovery in Neurodegeneration, Harvard Center for Neurodegeneration and Repair, Brigham & Women's Hospital, 65 Landsdowne Street, Cambridge, MA 02139, USA.
[Ti] Título:Synthesis, receptor binding and functional studies of mesoridazine stereoisomers.
[So] Source:Bioorg Med Chem Lett;14(17):4379-82, 2004 Sep 06.
[Is] ISSN:0960-894X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The four stereoisomers of mesoridazine were synthesized and evaluated in D2, 5-HT1A, 5-HT2A, 5-HT2C, D1, and D3 receptor binding and functional assays. Two isomers demonstrated potent D2 receptor binding (Ki < 3 nM) and functional antagonism (IC50 < or = 10 nM) activities. These two isomers also showed moderate affinity for the 5-HT2A and D3 receptors. A third isomer was devoid of significant D2 receptor binding, but did have moderate affinity for the 5-HT2A and D3 receptors. The fourth isomer demonstrated poor affinity for all the receptors tested. Most significantly, the stereochemistry of the sulfoxide moiety played a dominant role in the observed structure-activity relationship (SAR).
[Mh] Termos MeSH primário: Mesoridazina/síntese química
Mesoridazina/metabolismo
Receptores de Dopamina D2/metabolismo
Receptores de Serotonina/metabolismo
[Mh] Termos MeSH secundário: Seres Humanos
Ligação Proteica/fisiologia
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Receptors, Dopamine D2); 0 (Receptors, Serotonin); 5XE4NWM740 (Mesoridazine)
[Em] Mês de entrada:0502
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:040911
[St] Status:MEDLINE


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Fotocópia
[PMID]:15290689
[Au] Autor:Morrow RJ; Millership JS; Collier PS
[Ad] Endereço:Queens University Belfast, School of Pharmacy, Belfast, UK. r.morrow@qub.ac.uk
[Ti] Título:Diastereotopic analysis of mesoridazine besylate (Serentil).
[So] Source:Chirality;16(8):534-40, 2004 Oct.
[Is] ISSN:0899-0042
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:NMR studies were conducted with the aim of determining the diastereoisomeric ratio of a commercially supplied sample of mesoridazine (MES) and to compare the results with a freshly synthesised sample of MES. The results indicated that the commercially supplied MES consisted almost entirely of one diastereoisomeric pair, which was in agreement with previous findings reported by Eap et al. The synthesised sample of MES was analysed by NMR in two stages: 1) as the initial product isolated as the free base from the direct synthesis, and 2) as the free base isolated from the crystallised besylate salt of the synthetic product. The NMR results show that the initial synthetic product consisted of two equal pairs of diastereoisomers. The diastereoisomeric pairs were further separated by the addition of the chiral shift reagent (R)-(-)-N-(3,5 dinitrobenzoyl)-alpha-benzylamine to reveal equal quantities of all four enantiomers, clearly observed at the methyl sulfoxide proton peak of the NMR scan. The sample obtained from the crystallisation of MES besylate, however, indicated a significant difference, with a diastereoisomeric ratio of 75:25. The results suggest that MES besylate undergoes preferential crystallisation of one pair of diastereoisomers, with the other pair remaining in solution.
[Mh] Termos MeSH primário: Mesoridazina/química
[Mh] Termos MeSH secundário: Cristalização
Espectroscopia de Ressonância Magnética
Mesoridazina/síntese química
Metilação
Estrutura Molecular
Estereoisomerismo
Tioridazina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
5XE4NWM740 (Mesoridazine); N3D6TG58NI (Thioridazine)
[Em] Mês de entrada:0411
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:040804
[St] Status:MEDLINE



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