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[PMID]:27417385
[Au] Autor:Bruchatá K; Némethy A; Cizmáriková R; Racanská E; Habala L
[Ad] Endereço:Faculty of Pharmacy, Department of Chemical Theory of Drugs, Comenius University in Bratislava, Bratislava, Slovakia.
[Ti] Título:Synthesis and In Vitro Pharmacological Evaluation of 5-(Alkoxymethyl)-2-(3-alkylamino-2-hydroxypropoxy)phenylethanones Related to Acebutolol and Celiprolol.
[So] Source:Arch Pharm (Weinheim);349(9):733-40, 2016 Sep.
[Is] ISSN:1521-4184
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The structure-activity relationships of 13 analogs of aryloxyaminopropanol type derived from 2-hydroxyphenylethanone as potential ß-blockers are described. The synthesized compounds possess an isopropyl or a tert-butyl group in the hydrophilic part of the molecule and an alkoxymethyl substitution in the lipophilic moiety. The target compounds were prepared by an established four-step method and their structures were confirmed by interpretation of their UV, IR, (1) H NMR and (13) C NMR spectra, and by elemental analysis. The ß-adrenolytic efficacy of the prepared racemic compounds was determined on isolated guinea pig atria (ß1 ) and trachea (ß2 ) and expressed as pA2 values against isoprenaline tachycardia. The assumed cardioselectivity was expressed as ß1 /ß2 ratio and the values of compounds with an alkoxy group (CH3 O, iC3 H5 O, C5 H11 O, CH2 CHCH2 O, CH3 OCH2 CH2 O) in the lipophilic part and with tert-butyl in the hydrophilic part of the molecule were found to be comparable or higher than those of the standards acebutolol and celiprolol. All evaluated substances at a concentration of 10(-7) mol/dm(3) showed also negative chronotropic effects.
[Mh] Termos MeSH primário: Acebutolol/análogos & derivados
Acebutolol/farmacologia
Celiprolol/análogos & derivados
Celiprolol/farmacologia
Propanolaminas/química
Propanolaminas/farmacologia
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/síntese química
Antagonistas Adrenérgicos beta/farmacologia
Animais
Cobaias
Átrios do Coração/efeitos dos fármacos
Frequência Cardíaca/efeitos dos fármacos
Histamina/farmacologia
Isoproterenol/farmacologia
Propanolaminas/síntese química
Relação Estrutura-Atividade
Traqueia/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Propanolamines); 67P356D8GH (Acebutolol); 820484N8I3 (Histamine); DRB57K47QC (Celiprolol); L628TT009W (Isoproterenol)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170315
[Lr] Data última revisão:
170315
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160716
[St] Status:MEDLINE
[do] DOI:10.1002/ardp.201600136


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[PMID]:26817868
[Au] Autor:Nijim Y; Adawi A; Bisharat B; Bowirrat A
[Ad] Endereço:From the Head of Pediatric and Neonatal Department (YN); Pediatric and Neonatal Department, EMMS Nazareth-The Nazareth Hospital, Nazareth (AA); Director of EMMS Nazareth Hospital, Galilee Medical School - Bar Ilan University (BB); and Clinical Neuroscience and Population Genetics-EMMS, Nazareth Hospital, Nazareth, Israel (AB).
[Ti] Título:First Case Report of Smith-Magenis Syndrome (SMS) Among the Arab Community in Nazareth: View and Overview.
[So] Source:Medicine (Baltimore);95(3):e2362, 2016 Jan.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Smith-Magenis syndrome (SMS0) is a complex and rare genetic multisystem disorder characterized by a variable pattern of cognitive deficits accompanied by a1 distinctive behavioral phenotype. SMS is characterized by subtle facial dysmorphology, short stature, sleep disturbances, and neurobehavioral abnormalities. Little is known about the manifestation of his unique case among Arab population and its strategic treatment.This study comes to present a case of SMS in an Arab newborn male who was born in spontaneous delivery on June 29, 2015, with tachypnea, tracheomalacia, and mild hypotonia. The newborn was admitted on the Neonatal Intensive Care Unit (NICU), and various laboratory examinations and clinical examinations were performed.Throughout his hospitalization, feeding difficulties appeared and thus a peripheral venous catheter was inserted in the left leg.After 22 days of follow-up and hospitalizations, the patient status improved and he was discharged with recommendations to be in follow up in pediatric outpatient clinic.However, notwithstanding the different investigations, intermittent tachypnea continued at a rate of 72 to 77 breaths/min. Search for diagnosis begin intensively owing to persistence of tachypnia, mild hypotonia, feeding difficulties, sleep disturbances, and mild dysmorphic facial features. Suspicions of genetic abnormalities were considered and blood samples were sent for chromosome analysis and for fluorescent in situ hybridization (FISH) testing.The genetic results revealed the following: cytogenetic findings: 46, XY, del(17)(p11.2) and the FISH results: del(17)(p11.2p11.2) (D17S29). The chromosome diagnosis revealed an interstitial deletion of 17p11.2 and the diagnosis of the SMS was confirmed.Accurate clinical diagnosis, therapeutic assessments and a holistic management plans, including multidiscipline therapeutic strategies, periodic neuro-developmental assessments, and an early intervention programs, are recommended.However, cytogenetic analysis or FISH using an RAI1-specific probe is the most frequently used technique for DS. Sleep and behavioral disturbances treatment include a combination of the daytime dose of acebutolol with an evening oral dose of melatonin. Melatonin as chronobiotic, antioxidant, and analgesic agent showed to be effective in different primary sleep disorders and in those associated with neurobehavioral disorders. Based on the beneficial effect of melatonin, it will be useful to use serum levels of melatonin as a follow-up test.
[Mh] Termos MeSH primário: Árabes/genética
Síndrome de Smith-Magenis/genética
[Mh] Termos MeSH secundário: Acebutolol/uso terapêutico
Antagonistas de Receptores Adrenérgicos beta 1
Antioxidantes/uso terapêutico
Deleção Cromossômica
Combinação de Medicamentos
Seres Humanos
Hibridização in Situ Fluorescente
Recém-Nascido
Israel/epidemiologia
Masculino
Melatonina/uso terapêutico
Fenótipo
Distribuição Espacial da População
Síndrome de Smith-Magenis/diagnóstico
Síndrome de Smith-Magenis/tratamento farmacológico
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Antioxidants); 0 (Drug Combinations); 67P356D8GH (Acebutolol); JL5DK93RCL (Melatonin)
[Em] Mês de entrada:1606
[Cu] Atualização por classe:170502
[Lr] Data última revisão:
170502
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:160129
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000002362


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[PMID]:26423291
[Au] Autor:Khalit WN; Tay KS
[Ad] Endereço:Environmental Research Group, Department of Chemistry, Faculty of Science, University of Malaya, 50603, Kuala Lumpur, Malaysia.
[Ti] Título:Aqueous chlorination of acebutolol: kinetics, transformation by-products, and mechanism.
[So] Source:Environ Sci Pollut Res Int;23(3):2521-9, 2016 Feb.
[Is] ISSN:1614-7499
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:This study investigated the reaction kinetics and the transformation by-products of acebutolol during aqueous chlorination. Acebutolol is one of the commonly used ß-blockers for the treatment of cardiovascular diseases. It has been frequently detected in the aquatic environment. In the kinetics study, the second-order rate constant for the reaction between acebutolol and chlorine (k app) was determined at 25 ± 0.1 °C. The degradation of acebutolol by free available chlorine was highly pH dependence. When the pH increased from 6 to 8, it was found that the k app for the reaction between acebutolol and free available chlorine was increased from 1.68 to 11.2 M(-1) min(-1). By comparing with the reported k app values, the reactivity of acebutolol toward free available chlorine was found to be higher than atenolol and metoprolol but lower than nadolol and propranolol. Characterization of the transformation by-products formed during the chlorination of acebutolol was carried out using liquid chromatography-quadrupole time-of-flight high-resolution mass spectrometry. Seven major transformation by-products were identified. These transformation by-products were mainly formed through dealkylation, hydroxylation, chlorination, and oxidation reactions.
[Mh] Termos MeSH primário: Acebutolol/química
Antagonistas de Receptores Adrenérgicos beta 1/química
Anti-Hipertensivos/química
Poluentes Químicos da Água/química
Purificação da Água
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/química
Atenolol/química
Cloro/química
Cromatografia Líquida
Halogenação
Cinética
Espectrometria de Massas
Oxirredução
Propranolol/química
Água/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Adrenergic beta-Antagonists); 0 (Antihypertensive Agents); 0 (Water Pollutants, Chemical); 059QF0KO0R (Water); 4R7X1O2820 (Chlorine); 50VV3VW0TI (Atenolol); 67P356D8GH (Acebutolol); 9Y8NXQ24VQ (Propranolol)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:171103
[Lr] Data última revisão:
171103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151002
[St] Status:MEDLINE
[do] DOI:10.1007/s11356-015-5470-y


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[PMID]:26408002
[Au] Autor:Muta K; Fukami T; Nakajima M
[Ad] Endereço:Drug Metabolism and Toxicology, Faculty of Pharmaceutical Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan.
[Ti] Título:A proposed mechanism for the adverse effects of acebutolol: CES2 and CYP2C19-mediated metabolism and antinuclear antibody production.
[So] Source:Biochem Pharmacol;98(4):659-70, 2015 Dec 15.
[Is] ISSN:1873-2968
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Acebutolol, a ß-adrenergic receptor-blocker, occasionally causes drug-induced lupus erythematosus (DILE). Acebutolol is mainly metabolized to diacetolol. Because metabolic activation has been considered to be related to acebutolol-induced toxicity, we sought to identify the enzymes that are responsible for acebutolol metabolism and investigate their involvement in acebutolol-induced toxicity. By using human liver microsomes (HLM) or intestinal microsomes and recombinant enzymes, we found that diacetolol was produced via hydrolysis by carboxylesterase 2 (CES2) and subsequent acetylation by N-acetyltransferase 2 (NAT2). When acetolol, a hydrolytic metabolite of acebutolol, was incubated with HLM and an NADPH-generating system, a metabolite conjugated with N-acetylcystein was generated. This metabolite was found to be formed by CYP2C19 based on studies with a panel of recombinant cytochrome P450 enzymes and an inhibition study using HLM with tranylcypromine, a CYP2C19 inhibitor. Because antinuclear antibody (ANA) production is associated with DILE, we investigated whether ANA was detected in plasma from mice treated with acebutolol. Administration of acebutolol (100mg/kg, p.o.) to female C57BL/6 mice for 30 days resulted in ANA production in plasma in seven of thirteen mice. The number of mice that showed ANA production was larger in mice co-treated with pregnenolone 16α-carbonitrile, an inducer of P450s, whereas it was lower in mice co-treated with tri-o-tolylphosphate or 1-aminobenzotriazole, which are inhibitors of esterases or P450s, respectively. These results suggested that the hydrolysis and oxidation of acebutolol was associated with ANA production. In summary, this study demonstrated that metabolic activation may be a causal factor of adverse reactions of acebutolol.
[Mh] Termos MeSH primário: Acebutolol/efeitos adversos
Acebutolol/metabolismo
Anticorpos Antinucleares/metabolismo
Carboxilesterase/metabolismo
Citocromo P-450 CYP2C19/metabolismo
[Mh] Termos MeSH secundário: Adulto
Animais
Relação Dose-Resposta a Droga
Feminino
Seres Humanos
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Microssomos Hepáticos/efeitos dos fármacos
Microssomos Hepáticos/metabolismo
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antibodies, Antinuclear); 67P356D8GH (Acebutolol); EC 1.14.14.1 (CYP2C19 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP2C19); EC 3.1.1.1 (CES2 protein, human); EC 3.1.1.1 (Carboxylesterase)
[Em] Mês de entrada:1603
[Cu] Atualização por classe:161126
[Lr] Data última revisão:
161126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150927
[St] Status:MEDLINE


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[PMID]:25981230
[Au] Autor:Basagni B; Navarrete E; Bertoni D; Cattran C; Mapelli D; Oddy M; De Tanti A
[Ad] Endereço:Centro Cardinal Ferrari (Servizio di Neuropsicologia), via IV Novembre, 21, 43012, Fontanellato, Parma, Italy. bbasagni@gmail.com.
[Ti] Título:The Italian version of the Brain Injury Rehabilitation Trust (BIRT) personality questionnaires: five new measures of personality change after acquired brain injury.
[So] Source:Neurol Sci;36(10):1793-8, 2015 Oct.
[Is] ISSN:1590-3478
[Cp] País de publicação:Italy
[La] Idioma:eng
[Ab] Resumo:The aim of this study was to describe the translation and adaptation of the BIRT personality questionnaires for the Italian population. This included the replication of validity testing and the collection of normative data. Following translation and adaptation according to cross-cultural guidelines, the questionnaires were administered as a pre-test to a sample of 20 healthy subjects and then to 10 patients. The questionnaires were then administered to 120 healthy subjects equally distributed by sex, education, and age, to collect normative data from an Italian population. The questionnaires were easily administered to both healthy subjects and patients. Statistical analysis on normative data was conducted to find the mean value for each questionnaire. This study lays the foundations for using a new instrument to assess behavioral changes after acquired brain injury on the Italian population.
[Mh] Termos MeSH primário: Lesões Encefálicas/diagnóstico
Lesões Encefálicas/psicologia
Linguagem
Testes de Personalidade
[Mh] Termos MeSH secundário: Acebutolol
Adulto
Lesões Encefálicas/reabilitação
Feminino
Seres Humanos
Masculino
Meia-Idade
Traduções
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
67P356D8GH (Acebutolol)
[Em] Mês de entrada:1606
[Cu] Atualização por classe:171013
[Lr] Data última revisão:
171013
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150519
[St] Status:MEDLINE
[do] DOI:10.1007/s10072-015-2251-9


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[PMID]:25977108
[Au] Autor:Banoth L; Thakur NS; Bhaumik J; Banerjee UC
[Ad] Endereço:Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research (NIPER), Punjab, India.
[Ti] Título:Biocatalytic Approach for the Synthesis of Enantiopure Acebutolol as a ß1-Selective Blocker.
[So] Source:Chirality;27(6):382-91, 2015 Jun.
[Is] ISSN:1520-636X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A new chemoenzymatic route is reported to synthesize acebutolol, a selective ß1 adrenergic receptor blocking agent in enantiopure (R and S) forms. The enzymatic kinetic resolution strategy was used to synthesize enantiopure intermediates (R)- and (S)-N-(3-acetyl-4-(3-chloro-2-hydroxypropoxy)phenyl)butyramide from the corresponding racemic alcohols. The results showed that out of eleven commercially available lipase preparations, two enzyme preparations (Lipase A, Candida antarctica, CLEA [CAL CLEA] and Candida rugosa lipase, 62316 [CRL 62316]) act in enantioselective manner. Under optimized conditions the enantiomeric excess of both (R)- and (S)-N-(3-acetyl-4-(3-chloro-2-hydroxypropoxy)phenyl)butyramide were 99.9 and 96.8%, respectively. N-alkylation of both the (R) and (S) intermediates with isopropylamine gave enantiomerically pure (R and S)- acebutolol with a yield 68 and 72%, respectively. This study suggests a high yielding, easy and environmentally green approach to synthesize enantiopure acebutolol.
[Mh] Termos MeSH primário: Acebutolol/síntese química
Antagonistas de Receptores Adrenérgicos beta 1/síntese química
[Mh] Termos MeSH secundário: Biocatálise
Modelos Biológicos
Estrutura Molecular
Estereoisomerismo
Especificidade por Substrato
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 67P356D8GH (Acebutolol)
[Em] Mês de entrada:1602
[Cu] Atualização por classe:150527
[Lr] Data última revisão:
150527
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150516
[St] Status:MEDLINE
[do] DOI:10.1002/chir.22444


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[PMID]:25958323
[Au] Autor:Abuzooda T; Amini A; Abdel-Rehim M
[Ad] Endereço:Department of Analytical Chemistry, Stockholm University, 106 91 Stockholm, Sweden.
[Ti] Título:Graphite-based microextraction by packed sorbent for online extraction of ß-blockers from human plasma samples.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;992:86-90, 2015 Jun 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In the present work a new graphitic material (Carbon-XCOS) was used as a sorbent for microextraction by packed sorbent (MEPS). The ß-blockers metoprolol and acebutolol in plasma samples were extracted and detected online using Carbon-MEPS syringe and liquid chromatography and tandem mass spectrometry (LC-MS/MS). Factors affecting the MEPS performance such as conditioning, washing and elution solutions were investigated. The validation of the bioanalytical method was performed using human plasma. The standard curve ranged from 10 to 2000nM and the lower limit of quantification (LLOQ) was set to 10nM. The method validation showed good accuracy and precision for the quality control (QC) samples at three concentration levels (30, 800 and 1600nM). The accuracy values of the QC samples were in the range of 86-108% (n=18). The precision values of intra- and inter-day for QC samples ranged from 4.4% to 14.4% (RSD) for the both studied analytes. The coefficient of determination (R(2)) values were ≥0.999 (n=3).
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/sangue
Antagonistas Adrenérgicos beta/isolamento & purificação
Grafite/química
Microextração em Fase Sólida/métodos
[Mh] Termos MeSH secundário: Acebutolol/sangue
Acebutolol/isolamento & purificação
Cromatografia Líquida
Seres Humanos
Limite de Detecção
Modelos Lineares
Metoprolol/sangue
Metoprolol/isolamento & purificação
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 67P356D8GH (Acebutolol); 7782-42-5 (Graphite); GEB06NHM23 (Metoprolol)
[Em] Mês de entrada:1602
[Cu] Atualização por classe:150524
[Lr] Data última revisão:
150524
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150511
[St] Status:MEDLINE


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[PMID]:25857877
[Au] Autor:Ogrodowczyk M; Dettlaff K; Kachlicki P; Marciniec B
[Ad] Endereço:Poznan University of Medical Sciences, Department of Pharmaceutical Chemistry, Grunwaldzka 6, 60-780 Poznan, Poland.
[Ti] Título:Identification of Radiodegradation Products of Acebutolol and Alprenolol by HPLC/MS/MS.
[So] Source:J AOAC Int;98(1):46-50, 2015 Jan-Feb.
[Is] ISSN:1060-3271
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Two therapeutically active compounds from the group of ß-blockers, acebutolol (AC) and alprenolol (AL), in solid form were subjected to ionizing radiation emitted by a beam of high energy electrons from an accelerator with a standard sterilization dose of 25 kGy and in higher doses of 50-400 kGy. The effects of irradiation were detected by chromatographic methods (TLC, HPLC) and a hyphenated method (HPLC/MS/MS). No significant changes in the physicochemical properties of both compounds studied irradiated with 25 kGy were noted, but upon irradiation with the highest dose (400 kGy) the loss of AC and AL content determined by HPLC was 2.79 and 9.12%, respectively. The product of AC decomposition and the two products of AL decomposition were separated and identified by HPLC/MS/MS. It has been established that radiodegradation of AC and AL takes place by oxidation, leading to formation of the products of radiolysis, most probably alcohol derivatives of the ß-blockers studied. The additional product that appears on radiodegradation of AL is probably formed as a result of two simultaneous reactions: oxidation and CH2 group elimination.
[Mh] Termos MeSH primário: Acebutolol/química
Alprenolol/química
Cromatografia Líquida de Alta Pressão/métodos
Radiação Ionizante
Espectrometria de Massas em Tandem/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
67P356D8GH (Acebutolol); 877K5MQ27W (Alprenolol)
[Em] Mês de entrada:1510
[Cu] Atualização por classe:150410
[Lr] Data última revisão:
150410
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150411
[St] Status:MEDLINE
[do] DOI:10.5740/jaoacint.14-096


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[PMID]:25643948
[Au] Autor:Verstraelen J; Reichl S
[Ad] Endereço:Institut für Pharmazeutische Technologie, Technische Universität Braunschweig, Braunschweig, Germany.
[Ti] Título:Upregulation of P-glycoprotein expression by ophthalmic drugs in different corneal in-vitro models.
[So] Source:J Pharm Pharmacol;67(5):605-15, 2015 May.
[Is] ISSN:2042-7158
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: The purpose of this study was to analyse P-glycoprotein (P-gp) expression in different human in-vitro cornea models (HCE-T epithelial model and Hemicornea construct) after stimulation with P-gp substrates (rhodamine 123, levofloxacin and acebutolol). METHODS: The influence of P-gp substrates on mRNA expression was analysed using reverse transcriptase polymerase chain reaction (PCR) and real-time PCR. The effect of stimulation on the transporter functionality was estimated with a digoxin efflux assay. The Caco-2 cell line was used as positive control. KEY FINDINGS: The reverse transcriptase PCR results showed an increase in band intensity compared with the control medium for all substrates. The real-time PCR for the Caco-2 and HCE-T epithelial model yielded a similar outcome, in which all tested substrates upregulated P-gp. In contrast, the Hemicornea construct showed no significant increase in the mRNA expression after stimulation. Both in-vitro models possessed similar drug transport profiles after stimulation. A significantly increased efflux of digoxin was measured after 24 and 72 h of stimulation with levofloxacin and acebutolol. CONCLUSIONS: The expression and functionality of the P-gp in corneal tissue can be influenced through time exposure with specific substrates. However, the exact mechanism still requires further elucidation.
[Mh] Termos MeSH primário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/biossíntese
Acebutolol/farmacologia
Córnea/efeitos dos fármacos
Córnea/metabolismo
Levofloxacino/farmacologia
Soluções Oftálmicas/farmacologia
Regulação para Cima/efeitos dos fármacos
[Mh] Termos MeSH secundário: Células Cultivadas
Seres Humanos
Técnicas In Vitro
Rodamina 123/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Ophthalmic Solutions); 1N3CZ14C5O (Rhodamine 123); 67P356D8GH (Acebutolol); 6GNT3Y5LMF (Levofloxacin)
[Em] Mês de entrada:1605
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150204
[St] Status:MEDLINE
[do] DOI:10.1111/jphp.12357


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[PMID]:25196119
[Au] Autor:Swidan MM; Sakr TM; Motaleb MA; El-Bary AA; El-Kolaly MT
[Ad] Endereço:Labeled Compound Department, Hot Labs Center, Atomic Energy Authority, PO13759, Cairo, Egypt.
[Ti] Título:Radioiodinated acebutolol as a new highly selective radiotracer for myocardial perfusion imaging.
[So] Source:J Labelled Comp Radiopharm;57(10):593-9, 2014 Aug.
[Is] ISSN:1099-1344
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Acebutolol was successfully labeled with (125) I via direct electrophilic substitution reaction. Radioiodinated acebutolol was prepared with a maximum radiochemical yield of 96.5 ± 0.3% and in vitro stability up to 72 h. The in vivo biological distribution of radioiodinated acebutolol showed high heart uptake of 37.8 ± 0.14% injected activity/g organ with low lungs and liver uptakes at 5 min post-injection. In vivo receptor blocking study was carried out in mice to evaluate its selectivity to heart. Radioiodinated acebutolol showed fast heart accumulation with high heart/liver ratio, which provides the ability for fast myocardial imaging with significant decrease in the radiation hazards risk on patients. So, radioiodinated acebutolol could be displayed as a radiotracer drug of choice in case of emergency patients for myocardial perfusion imaging.
[Mh] Termos MeSH primário: Acebutolol/farmacocinética
Imagem de Perfusão do Miocárdio/métodos
Compostos Radiofarmacêuticos/farmacocinética
[Mh] Termos MeSH secundário: Acebutolol/síntese química
Animais
Radioisótopos do Iodo/química
Radioisótopos do Iodo/farmacocinética
Masculino
Camundongos
Compostos Radiofarmacêuticos/síntese química
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Iodine Radioisotopes); 0 (Radiopharmaceuticals); 67P356D8GH (Acebutolol)
[Em] Mês de entrada:1511
[Cu] Atualização por classe:140925
[Lr] Data última revisão:
140925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140909
[St] Status:MEDLINE
[do] DOI:10.1002/jlcr.3223



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