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1.
Rev. psicol. trab. organ. (1999) ; 38(3): 129-147, dic. 2022. tab, graf
Artigo em Inglês | IBECS | ID: ibc-212971

RESUMO

Human Resources Analytics (HRA) is drawing more attention every year, and will be crucial to human resource development. However, the literature around the topic would appear to be more promotional than descriptive. With this in mind, we conducted a systematic literature review and content analysis with the following objectives: first, to address the current state of HRA and second, to propose a framework for the development of HRA as a sustainable practice. We analyzed 79 articles from research databases and found 34 empirical studies for subsequent content analysis. While the main results reflect the relative newness of the field of HRA, with the majority of the empirical articles focusing on financial aspects, they also reveal the growing importance given to ethics. Finally, we propose a framework for the development of sustainable HRA based on the triple bottom line and discuss the implications of our findings for researchers and practitioners.(AU)


La analítica de recursos humanos (ARH) atrae cada vez más atención en los últimos años y será crucial para el desarrollo del ámbito de los recursos humanos. No obstante, la literatura sobre el tema parece ser más promocional que descriptiva. Para comprobar esto, llevamos a cabo una revisión sistemática de la literatura y un análisis de contenido con los siguientes objetivos: primero, abordar el estado actual la ARH y segundo, proponer un marco para el desarrollo de la AHR como una práctica sostenible. Analizamos 79 artículos de investigación incluidos en las más prestigiosas bases de datos y encontramos 34 estudios empíricos para su posterior análisis de contenido. Los principales resultados reflejan la relativa novedad del campo de la ARH, estando centrados la mayoría de los artículos en los aspectos financieros. No obstante, también se observa la creciente importancia dada a la ética. Finalmente, proponemos un marco para el desarrollo de una ARH basada en la triple cuenta de resultados (económica, social y medioambiental, y se discuten las implicaciones prácticas y teóricas de nuestros hallazgos.(AU)


Assuntos
Humanos , Emprego , Desenvolvimento Sustentável , Big Data , Inteligência Artificial , Indicadores de Desenvolvimento Sustentável , Ética , Psicologia , Psicologia Industrial , Organizações
2.
J Med Chem ; 64(6): 3439-3448, 2021 03 25.
Artigo em Inglês | MEDLINE | ID: mdl-33721487

RESUMO

The identification of LSN3318839, a positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R), is described. LSN3318839 increases the potency and efficacy of the weak metabolite GLP-1(9-36)NH2 to become a full agonist at the GLP-1R and modestly potentiates the activity of the highly potent full-length ligand, GLP-1(7-36)NH2. LSN3318839 preferentially enhances G protein-coupled signaling by the GLP-1R over ß-arrestin recruitment. Ex vivo experiments show that the combination of GLP-1(9-36)NH2 and LSN3318839 produces glucose-dependent insulin secretion similar to that of GLP-1(7-36)NH2. Under nutrient-stimulated conditions that release GLP-1, LSN3318839 demonstrates robust glucose lowering in animal models alone or in treatment combination with sitagliptin. From a therapeutic perspective, the biological properties of LSN3318839 support the concept that GLP-1R potentiation is sufficient for reducing hyperglycemia.


Assuntos
Regulação Alostérica/efeitos dos fármacos , Receptor do Peptídeo Semelhante ao Glucagon 1/agonistas , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Administração Oral , Animais , Glicemia/análise , Descoberta de Drogas , Receptor do Peptídeo Semelhante ao Glucagon 1/química , Receptor do Peptídeo Semelhante ao Glucagon 1/metabolismo , Humanos , Hipoglicemiantes/administração & dosagem , Camundongos , Modelos Moleculares , Ratos Sprague-Dawley
3.
Rev. neurol. (Ed. impr.) ; 70(2): 37-44, 16 ene., 2020. tab, graf
Artigo em Espanhol | IBECS | ID: ibc-187246

RESUMO

Introducción: La importancia de conocer el patrón de evolución de los déficits cognitivos en los primeros meses tras un traumatismo craneoencefálico (TCE) ha fomentado el desarrollo de numerosos estudios longitudinales. Sin embargo, los resultados de la mayoría de ellos deberían tomarse con cautela debido a la falta de un control adecuado del efecto de la práctica, que puede llevar a sobreestimar la recuperación genuina de los procesos cognitivos. Objetivo: Describir los cambios cognitivos entre las fases aguda y subaguda del TCE controlando el efecto de la práctica. Pacientes y métodos: Veintidós pacientes realizaron dos evaluaciones neuropsicológicas tras el TCE (inmediata y tras seis meses) mediante los siguientes tests: Trail Making Test (A, B, B/A y B-A), test de Stroop (P, C, PC e interferencia), clave de números, búsqueda de símbolos, dígitos directos e inversos, fluidez verbal y memoria inmediata. Para controlar el efecto de la práctica se realizó una transformación de las puntuaciones aplicando el procedimiento propuesto por Calamia et al. Resultados: Antes de controlar el efecto de la práctica, se evidenció una mejoría en las puntuaciones de todos los tests (p > 0,001). Sin embargo, tras él, la mejoría permaneció sólo en el Trail Making Test-B, B/A y B-A, la clave de números, la búsqueda de símbolos, el test de Stroop PC y los dígitos inversos. Conclusiones: La falta de control del efecto de la práctica en estudios longitudinales puede generar interpretaciones erróneas sobre el perfil de evolución de los déficits cognitivos. El patrón de recuperación tras un TCE varía en función del proceso cognitivo


Introduction: The importance of knowing the pattern of evolution of cognitive deficits in the first months after a traumatic brain injury (TBI) has encouraged the development of numerous longitudinal studies. However, the results of most of them should be taken with caution due to the lack of adequate control of practice effects that can lead to overestimating the genuine recovery of cognitive processes. Aim. To describe the cognitive changes between the acute and subacute phases of the TBI controlling the effect of the practice. Patients and methods: Twenty-two patients were assessed in two different time points after TBI (immediately and after six months) using the following tests: Trail Making Test (A, B, B/A, B-A), Stroop Test (W, C, CW, interference), Digit Symbol-Coding, Symbol Search, Digits Forward and Backward, Verbal Fluency and Short-term Memory. To control for the practice effects, a transformation of the scores was performed applying the procedure proposed by Calamia et al. Results: Before controlling the practice effects, the scores of all tests improved (p > 0.001). However, afterward, the improvement remained only in the Trail Making Test-B, B/A and B-A, Digit Symbol-Coding, Symbol Search, Stroop CW and Digits Backward. Conclusions: The lack of control of practice effects in longitudinal studies can generate misleading interpretations about the evolution of cognitive deficits. The pattern of recovery after a TBI varies depending on the cognitive process


Assuntos
Humanos , Feminino , Adulto , Pessoa de Meia-Idade , Disfunção Cognitiva/etiologia , Lesões Encefálicas Traumáticas/complicações , Testes Neuropsicológicos , Lesões Encefálicas Traumáticas/diagnóstico , Lesões Encefálicas Traumáticas/fisiopatologia , Lesões Encefálicas Traumáticas/psicologia , Memória/fisiologia , Estudos Longitudinais
4.
Artigo em Inglês | MEDLINE | ID: mdl-31121842

RESUMO

Women continue to lag behind for accessing managerial positions, partially due to discrimination at work. One of the main roots of such discrimination is gender stereotyping, so we aim to comprehend those biased procedures. First, we have analyzed those highlighted gender lawsuit cases in the scientific literature that have dealt with stereotypes both in the American and the European work contexts. Second, meta-analytic studies regarding organizational consequences of gender stereotypes have been synthetized. Third, gender stereotypes have been grouped by means of a content analysis of the existing literature after processing 61 articles systematically retrieved from WOS, SCOPUS, and PsycINFO databases. As a result, a taxonomy of gender stereotypes has been achieved evidencing that descriptive and prescriptive stereotypes have an impact on decision-making procedures through the apparently perception of women as less suitable for managerial positions. Moreover, we offer a deep explanation of the gender discrimination phenomenon under the umbrella of psychosocial theories, and some measures for successfully overcoming management stereotyping, showing that organizational culture can be improved from both the perspective of equal employment opportunities and the organizational justice frameworks for reaching a balanced and healthier workplace.


Assuntos
Cultura Organizacional , Estereotipagem , Tomada de Decisões , Europa (Continente) , Feminino , Humanos , Masculino , Justiça Social , Estados Unidos , Local de Trabalho
5.
Psicothema (Oviedo) ; 30(3): 344-350, ago. 2018. tab
Artigo em Inglês | IBECS | ID: ibc-175904

RESUMO

BACKGROUND: Interest in measuring the perception of organizational justice has been growing in recent years due to its proven ability to produce significant organizational outcomes such as well-being and emotional exhaustion. In Spain, the Organizational Justice Scale (OJS) can be highlighted as an instrument which has shown good psychometric properties in previous research in the hotel industry. This study provides further evidence of the characteristics of the OJS using a large multi-sectorial sample. METHOD: Participants comprised 849 employees from different occupational sectors. The structure of the OJS was studied by means of an exploratory and confirmatory factor analysis splitting the sample up into two random subsamples. The reliability and validity of each dimension was also analyzed. RESULTS:Results indicated a three-factorial structure: distributive, procedural, and interactional, offering adequate reliability and validity. As expected, positive correlations were found between perception of organizational justice and well-being, and negative correlations with respect to emotional exhaustion. CONCLUSIONS: OJS is an appropriate tool for use by researchers and practitioners in the study of the perception of organizational justice in Spain, additionally ensuring adequate validity and reliability


ANTECEDENTES: el interés por la medición de la percepción de justicia organizacional ha aumentado en los últimos años debido a su demostrada relación con resultados organizacionales significativos, como el bienestar y el agotamiento emocional. En España, se puede destacar la Escala de Justicia Organizacional (OJS) como un instrumento que ha mostrado buenas propiedades psicométricas en estudios previos en el sector hotelero. Este estudio complementa la evidencia de las características de la OJS utilizando una amplia muestra multisectorial. MÉTODO: los participantes fueron 849 empleados de diferentes sectores ocupacionales. La estructura de la OJS se estudió mediante análisis factorial exploratorio y confirmatorio dividiendo la muestra en dos submuestras aleatorias. Además, se analizó la fiabilidad y validez de cada dimensión. RESULTADOS: los resultados indicaron que la escala está constituida por tres factores (distributiva, procedimental y en la interacción), con una fiabilidad y validez adecuadas. Por otra parte, como era de esperar, se encontraron correlaciones positivas entre la percepción de justicia organizacional y el bienestar, y negativas con el agotamiento emocional. CONCLUSIONES: la OJS es una herramienta adecuada para su uso por parte de académicos y profesionales en el estudio de la percepción de justicia organizacional en España, garantizando una validez y fiabilidad adecuadas


Assuntos
Humanos , Masculino , Feminino , Adulto , Cultura Organizacional , Justiça Social , Reprodutibilidade dos Testes , Psicometria , Espanha
6.
Psicothema ; 30(3): 344-350, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30009759

RESUMO

BACKGROUND: Interest in measuring the perception of organizational justice has been growing in recent years due to its proven ability to produce significant organizational outcomes such as well-being and emotional exhaustion. In Spain, the Organizational Justice Scale (OJS) can be highlighted as an instrument which has shown good psychometric properties in previous research in the hotel industry. This study provides further evidence of the characteristics of the OJS using a large multi-sectorial sample. METHOD: Participants comprised 849 employees from different occupational sectors. The structure of the OJS was studied by means of an exploratory and confirmatory factor analysis splitting the sample up into two random subsamples. The reliability and validity of each dimension was also analyzed. RESULTS: Results indicated a three-factorial structure: distributive, procedural, and interactional, offering adequate reliability and validity. As expected, positive correlations were found between perception of organizational justice and well-being, and negative correlations with respect to emotional exhaustion. CONCLUSIONS: OJS is an appropriate tool for use by researchers and practitioners in the study of the perception of organizational justice in Spain, additionally ensuring adequate validity and reliability.


Assuntos
Cultura Organizacional , Justiça Social , Adulto , Feminino , Humanos , Masculino , Psicometria , Reprodutibilidade dos Testes , Espanha
7.
Neurocir.-Soc. Luso-Esp. Neurocir ; 27(2): 75-86, mar.-abr. 2016. ilus, tab
Artigo em Espanhol | IBECS | ID: ibc-150774

RESUMO

Se presenta una propuesta de programa de formación en Neurocirugía basado en competencias y adaptado al marco del proyecto de Troncalidad. Esta propuesta ha sido elaborada por un grupo de neurocirujanos comisionados por la Sociedad Española de Neurocirugía (SENEC) y podría ser modificada para generar una versión definitiva que estaría operativa coincidiendo con implantación del sistema troncal. El presente escrito pretende facilitar el examen del nuevo programa adjuntado en la versión on-line de nuestra revista. Duración del programa: El periodo total de formación es de 6 años; los 2 primeros se enmarcan en el tronco de Cirugía y los restantes 4 se adscriben al periodo específico. Estructura del programa: Se trata de un programa basado en competencias referidas al mapa utilizado por el Accreditation Council for Graduate Medical Education (ACGME) en los EE. UU. que incluye los siguientes dominios competenciales: Conocimiento médico, Cuidado del paciente, Comunicación, Profesionalismo, Aprendizaje basado en la práctica y perfeccionamiento, Sistemas de Salud, Colaboración interprofesional y Desarrollo profesional y personal. El mapa de subcompetencias en los dominios de Conocimiento y Cuidado del paciente (incluidas las competencias quirúrgicas) se adaptó del propuesto por la AANS y el CNS (anexo 1 del programa). Se utiliza además un mapa de subcompetencias para las rotaciones troncales. Métodos de instrucción: El aprendizaje del residente se basa en el estudio personal (autoaprendizaje) apoyado en el uso eficiente de las fuentes de información y una práctica clínica supervisada, incluyendo además la instrucción en bioética, gestión clínica, investigación y técnicas docentes Métodos de evaluación: La propuesta de evaluación del residente incluye, entre otros instrumentos, test teóricos de conocimiento, evaluación objetiva y estructurada del nivel de competencia clínica con enfermo real o estandarizado, escalas globales de competencia, evaluación 360°, «audits» de registros clínicos, señalizadores del progreso del residente («milestones») y autoevaluación (anexo 2). Además, el residente evalúa periódicamente la dedicación docente de los neurocirujanos del servicio y otros docentes implicados en las rotaciones, y valora anualmente el funcionamiento global del programa. Los resultados de las evaluaciones se registran, junto con otros datos de interés, en el Libro del Residente. Comité nacional de programa: Se propone la creación de un Comité de Programa adscrito directamente a la SENEC (Comisión Nacional) que, aparte de generar la versión definitiva del programa, se ocupe de monitorizar su implementación (nivel de adherencia al mismo y funcionamiento en los diferentes servicios), asuma la creación de bancos de preguntas y la administración centralizada de los test de conocimiento (en el ecuador de la residencia y/o al final de la misma) y centralice información recabada por los tutores que podría ser utilizada para la de reacreditación de los servicios


A programme proposal for competency-based Neurosurgery training adapted to the specialization project is presented. This proposal has been developed by a group of neurosurgeons commissioned by the SENEC (Spanish Society of Neurosurgery) and could be modified to generate a final version that could come into force coinciding with the implementation of the specialization programme. This document aims to facilitate the test of the new programme included in the online version of our journal. Duration of the programme: Total training period is 6 years; initial 2 years belong to the surgery specialization and remaining 4 years belong to core specialty period. Structure of the programme: It is a competency-based programmed based on the map used by the US Accreditation Council for Graduate Medical Education (ACGME) including the following domains of clinical competency: Medical knowledge, patient care, communication skills, professionalism, practice-based learning and improvement, health systems, interprofessional collaboration and professional and personal development. Subcompetencies map in the domains of Knowledge and Patient care (including surgical competencies) was adapted to the one proposed by AANS and CNS (annex 1 of the programme). A subcompetency map was also used for the specialization rotations. Instruction methods: Resident's training is based on personal study (self-learning) supported by efficient use of information sources and supervised clinical practice, including bioethical instruction, clinical management, research and learning techniques. Evaluation methods: Resident evaluation proposal includes, among other instruments, theoretical knowledge tests, objective and structured evaluation of the level of clinical competency with real or standardised patients, global competency scales, 360-degree evaluation, clinical record audits, milestones for residents progress and self-assessment (annex 2). Besides, residents periodically assess the teaching commitment of the department's neurosurgeons and other professors participating in rotations, and annually assess the overall operation of the programme. Results of evaluations are registered, together with other relevant data, in the Resident's Book. Programme's National Committee: The creation of a Programme Committee directly attached to the SENEC (National Commission) that, aside from generating a final version of the programme, monitors its implementation (level of adherence and operation in the different departments), assumes the creation of test banks and the centralized administration of knowledge tests (in the middle of the residency and/or at the end of it) and centralizes information collected by tutors that could be used for re-accreditation of the services, is proposed


Assuntos
Humanos , Neurocirurgia/educação , Educação Médica/tendências , Internato e Residência/organização & administração , Competência Profissional , Educação de Pós-Graduação em Medicina/tendências , Avaliação Educacional/métodos
8.
Neurocirugia (Astur) ; 27(2): 75-86, 2016.
Artigo em Espanhol | MEDLINE | ID: mdl-26944384

RESUMO

A programme proposal for competency-based Neurosurgery training adapted to the specialization project is presented. This proposal has been developed by a group of neurosurgeons commissioned by the SENEC (Spanish Society of Neurosurgery) and could be modified to generate a final version that could come into force coinciding with the implementation of the specialization programme. This document aims to facilitate the test of the new programme included in the online version of our journal. DURATION OF THE PROGRAMME: Total training period is 6 years; initial 2 years belong to the surgery specialization and remaining 4 years belong to core specialty period. STRUCTURE OF THE PROGRAMME: It is a competency-based programmed based on the map used by the US Accreditation Council for Graduate Medical Education (ACGME) including the following domains of clinical competency: Medical knowledge, patient care, communication skills, professionalism, practice-based learning and improvement, health systems, interprofessional collaboration and professional and personal development. Subcompetencies map in the domains of Knowledge and Patient care (including surgical competencies) was adapted to the one proposed by AANS and CNS (annex 1 of the programme). A subcompetency map was also used for the specialization rotations. INSTRUCTION METHODS: Resident's training is based on personal study (self-learning) supported by efficient use of information sources and supervised clinical practice, including bioethical instruction, clinical management, research and learning techniques. EVALUATION METHODS: Resident evaluation proposal includes, among other instruments, theoretical knowledge tests, objective and structured evaluation of the level of clinical competency with real or standardised patients, global competency scales, 360-degree evaluation, clinical record audits, milestones for residents progress and self-assessment (annex 2). Besides, residents periodically assess the teaching commitment of the department's neurosurgeons and other professors participating in rotations, and annually assess the overall operation of the programme. Results of evaluations are registered, together with other relevant data, in the Resident's Book. PROGRAMME'S NATIONAL COMMITTEE: The creation of a Programme Committee directly attached to the SENEC (National Commission) that, aside from generating a final version of the programme, monitors its implementation (level of adherence and operation in the different departments), assumes the creation of test banks and the centralized administration of knowledge tests (in the middle of the residency and/or at the end of it) and centralizes information collected by tutors that could be used for re-accreditation of the services, is proposed.


Assuntos
Competência Clínica , Currículo , Internato e Residência , Neurocirurgia/educação , Espanha
9.
Rev. psicol. trab. organ. (1999) ; 31(3): 155-164, dic. 2015.
Artigo em Inglês | IBECS | ID: ibc-146249

RESUMO

The recruitment process aims to request relevant information from applicants, but sometimes this could be used to discriminate. Based mainly on the legal framework and the Rational Bias, the present paper explores the use of potentially discriminatory content against women in Spanish companies according to the enforcement of the equal employment opportunity legislation in 2007, and its relationship with organizational results. We have performed a comparative study between 2005 and 2009 implementing a combination of qualitative and quantitative analysis. All the websites of the Spanish Stock Exchange were analyzed. Results show that companies did include potentially discriminatory questions in application forms, even after the law enforcement, but not in recruitment statements. Regarding organizational results, small but significant relationships between legal fulfillment and annual returns were found, but these results could have been influenced by factors attributable to the economic crisis. To conclude, we provide recommendations regarding desirable policies and organizational practices in the context of the area being studied (AU)


El proceso de reclutamiento es una fase importante del proceso de selección, donde se solicita información personal de los candidatos. Pero esta información podría ser utilizada de forma discriminatoria en la toma de decisiones. Basándonos en la Teoría del Sesgo Racional y en la legislación vigente en materia de igualdad, en este estudio se explora el posible uso discriminatorio contra las mujeres en las empresas que cotizan en la bolsa española, así como su relación con los resultados organizacionales. Hemos realizado un estudio comparativo entre los años 2005 y 2009 del contenido de las hojas de solicitud de empleo en las webs de todas las empresas que cotizaban en bolsa en esos años. Combinando técnicas cualitativas y cuantitativas, los resultados mostraron que las empresas incluían contenido potencialmente discriminatorio tanto antes como después de la Ley de Igualdad entre Mujeres y Hombres de 2007. Asimismo, hemos encontrado relación entre los resultados anuales de las empresas y el cumplimiento estricto de la legislación. Finalmente, incluimos recomendaciones de buenas prácticas para la política organizacional durante el reclutamiento (AU)


Assuntos
Feminino , Humanos , Masculino , Seleção de Pessoal/organização & administração , Seleção de Pessoal/normas , Seleção de Pessoal , Sexismo/psicologia , Sexismo/estatística & dados numéricos , Internet/normas , Webcasts como Assunto/tendências , Seleção de Pessoal/métodos , Seleção de Pessoal/tendências , Internet/organização & administração , Internet
10.
Bioorg Med Chem Lett ; 23(23): 6463-6, 2013 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-24140446

RESUMO

We have explored the decahydroisoquinoline scaffold, bearing a phenyl tetrazole, as GluK1 antagonists with potential as oral analgesics. We have established the optimal linker atom between decahydroisoquinoline and phenyl rings and demonstrated an improvement of both the affinity for the GluK1 receptor and the selectivity against the related GluA2 receptor with proper phenyl substitution. In this Letter, we also disclose in vivo data that led to the discovery of LY545694·HCl, a compound with oral efficacy in two persistent pain models.


Assuntos
Isoquinolinas/farmacologia , Dor/tratamento farmacológico , Pró-Fármacos/farmacologia , Receptores de Ácido Caínico/antagonistas & inibidores , Tetrazóis/farmacologia , Administração Oral , Sequência de Aminoácidos , Animais , Modelos Animais de Doenças , Isoquinolinas/química , Masculino , Dados de Sequência Molecular , Pró-Fármacos/química , Ratos , Ratos Sprague-Dawley , Receptores de Ácido Caínico/química , Relação Estrutura-Atividade , Tetrazóis/química
11.
Bioorg Med Chem Lett ; 23(23): 6459-62, 2013 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-24119554

RESUMO

The synthesis and structure-activity relationship of decahydroisoquinoline derivatives with various benzoic acid substitutions as GluK1 antagonists are described. Potent and selective antagonists were selected for a tailored prodrug approach in order to facilitate the evaluation of the new compounds in pain models after oral administration. Several diester prodrugs allowed for acceptable amino acid exposure and moderate efficacy in vivo.


Assuntos
Isoquinolinas/farmacologia , Dor/tratamento farmacológico , Pró-Fármacos/farmacologia , Receptores de Ácido Caínico/antagonistas & inibidores , Administração Oral , Sequência de Aminoácidos , Animais , Modelos Animais de Doenças , Haplorrinos , Isoquinolinas/química , Dados de Sequência Molecular , Pró-Fármacos/química , Receptores de Ácido Caínico/química , Relação Estrutura-Atividade
12.
J Med Chem ; 48(13): 4200-3, 2005 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-15974569

RESUMO

Amino acids 5 and 7, two potent and selective competitive GluR5 KA receptor antagonists, exhibited high GluR5 receptor affinity over other glutamate receptors. Their ester prodrugs 6 and 8 were orally active in three models of pain: reversal of formalin-induced paw licking, carrageenan-induced thermal hyperalgesia, and capsaicin-induced mechanical hyperalgesia.


Assuntos
Aminoácidos/farmacologia , Analgésicos/química , Analgésicos/farmacologia , Dor/tratamento farmacológico , Receptores de Ácido Caínico/antagonistas & inibidores , Analgésicos/farmacocinética , Animais , Disponibilidade Biológica , Linhagem Celular , Modelos Animais de Doenças , Humanos , Hiperalgesia/tratamento farmacológico , Ratos , Receptores de AMPA/metabolismo , Proteínas Recombinantes/metabolismo , Medula Espinal/fisiopatologia , Ácido alfa-Amino-3-hidroxi-5-metil-4-isoxazol Propiônico/metabolismo
13.
J Med Chem ; 45(20): 4383-6, 2002 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-12238915

RESUMO

Amino diacid 3, a highly selective competitive GluR5 kainate receptor antagonist, exhibited high GluR5 receptor affinity and selectivity over other glutamate receptors. Its diethyl ester prodrug 4 was orally active in two models of migraine: the neurogenic dural plasma protein extravasation model and the nucleus caudalis c-fos expression model. These data suggest that a GluR5 kainate receptor antagonist might be an efficacious antimigraine therapy with a novel mechanism of action.


Assuntos
Ácidos Carboxílicos/síntese química , Ésteres/síntese química , Antagonistas de Aminoácidos Excitatórios/síntese química , Isoquinolinas/síntese química , Transtornos de Enxaqueca/tratamento farmacológico , Pró-Fármacos/síntese química , Receptores de Ácido Caínico/antagonistas & inibidores , Doença Aguda , Administração Oral , Animais , Disponibilidade Biológica , Cálcio/metabolismo , Ácidos Carboxílicos/química , Ácidos Carboxílicos/farmacologia , Linhagem Celular , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Ésteres/química , Ésteres/farmacologia , Antagonistas de Aminoácidos Excitatórios/química , Antagonistas de Aminoácidos Excitatórios/farmacologia , Humanos , Isoquinolinas/química , Isoquinolinas/farmacologia , Pró-Fármacos/química , Pró-Fármacos/farmacologia , Ensaio Radioligante , Ratos , Ratos Wistar
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