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[PMID]:27353308
[Au] Autor:Nautiyal KM; Tritschler L; Ahmari SE; David DJ; Gardier AM; Hen R
[Ad] Endereço:Department of Psychiatry, Columbia University, New York, NY, USA.
[Ti] Título:A Lack of Serotonin 1B Autoreceptors Results in Decreased Anxiety and Depression-Related Behaviors.
[So] Source:Neuropsychopharmacology;41(12):2941-2950, 2016 Nov.
[Is] ISSN:1740-634X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The effects of serotonin (5-HT) on anxiety and depression are mediated by a number of 5-HT receptors, including autoreceptors that act to inhibit 5-HT release. While the majority of anxiety and depression-related research has focused on the 5-HT receptor, the 5-HT receptor has a lesser known role in modulating emotional behavior. 5-HT receptors are inhibitory GPCRs located on the presynaptic terminal of both serotonin and non-serotonin neurons, where they act to inhibit neurotransmitter release. The autoreceptor population located on the axon terminals of 5-HT neurons is a difficult population to study due to their diffuse localization throughout the brain that overlaps with 5-HT heteroreceptors (receptors located on non-serotonergic neurons). In order to study the contribution of 5-HT autoreceptors to anxiety and depression-related behaviors, we developed a genetic mouse model that allows for selective ablation of 5-HT autoreceptors. Mice lacking 5-HT autoreceptors displayed the expected increases in extracellular serotonin levels in the ventral hippocampus following administration of a selective serotonin reuptake inhibitor. In behavioral studies, they displayed decreased anxiety-like behavior in the open field and antidepressant-like effects in the forced swim and sucrose preference tests. These results suggest that strategies aimed at blocking 5-HT autoreceptors may be useful for the treatment of anxiety and depression.
[Mh] Termos MeSH primário: Ansiedade/metabolismo
Autorreceptores/metabolismo
Depressão/metabolismo
Hipocampo/metabolismo
Receptor 5-HT1B de Serotonina/deficiência
[Mh] Termos MeSH secundário: Animais
Animais Recém-Nascidos
Ansiedade/genética
Autorreceptores/genética
Depressão/genética
Modelos Animais de Doenças
Comportamento Exploratório/fisiologia
Preferências Alimentares/efeitos dos fármacos
Hipocampo/efeitos dos fármacos
Isótopos de Iodo/farmacocinética
Masculino
Aprendizagem em Labirinto/efeitos dos fármacos
Aprendizagem em Labirinto/fisiologia
Camundongos
Camundongos Endogâmicos C57BL
Camundongos Transgênicos
Pindolol/análogos & derivados
Pindolol/farmacocinética
Receptor 5-HT1B de Serotonina/genética
Receptores 5-HT1 de Serotonina/genética
Receptores 5-HT1 de Serotonina/metabolismo
Antagonistas da Serotonina/farmacocinética
Proteínas da Membrana Plasmática de Transporte de Serotonina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Autoreceptors); 0 (Iodine Isotopes); 0 (Receptor, Serotonin, 5-HT1B); 0 (Receptors, Serotonin, 5-HT1); 0 (Serotonin Antagonists); 0 (Serotonin Plasma Membrane Transport Proteins); 4K0SD5SNFS (cyanopindolol); BJ4HF6IU1D (Pindolol)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171101
[Lr] Data última revisão:
171101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160630
[St] Status:MEDLINE
[do] DOI:10.1038/npp.2016.109


  2 / 3608 MEDLINE  
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[PMID]:26825432
[Au] Autor:Wang Y; Dong X
[Ad] Endereço:a Department of Pharmacology , Shanxi Medical University , Taiyuan, Shanxi Province , People's Republic of China and.
[Ti] Título:Nebivolol ameliorates asymmetric dimethylarginine-induced vascular response in rat aorta via ß3 adrenoceptor-mediated mechanism.
[So] Source:Clin Exp Hypertens;38(2):252-9, 2016.
[Is] ISSN:1525-6006
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Asymmetric dimethylarginine (ADMA), an endogenous nitric oxide synthase (NOS) inhibitor, induces endothelial dysfunction. Nebivolol, a highly selective ß1-adrenergic receptor (AR) blocker, is the only beta-blocker known to induce vascular production of nitric oxide. OBJECTIVE: The present study was designed to evaluate the effect and mechanism of nebivolol on ADMA-induced vascular response in rat aorta in vitro. METHODS: In vitro, the effects of nebivolol and ADMA on resting tone or contraction induced by phenylephrine (PE, 10(-6 )mol/L) and relaxation induced by acetylcholine (Ach, 10(-10)-10(-5 )mol/L) were evaluated. RESULTS: ADMA in a concentration-dependent manner increased the resting and PE-induced tone and reduced Ach-induced relaxation. Nebivolol inhibited the ADMA-induced enhancements in tone and reversed the effects of ADMA on Ach-induced relaxation. These effects of nebivolol were blocked by selective ß3 receptor blocker cyanopindolol (1 µM), but not by selective ß2 receptor blocker butoxamine (50 µM). CONCLUSIONS: Nebivolol ameliorates the ADMA-induced vascular responses in rat aorta, at least in part, by mechanisms involving ß3 adrenoceptor.
[Mh] Termos MeSH primário: Agonistas de Receptores Adrenérgicos beta 1/farmacologia
Aorta/efeitos dos fármacos
Arginina/análogos & derivados
Inibidores Enzimáticos/farmacologia
Nebivolol/farmacologia
Receptores Adrenérgicos beta 3/metabolismo
[Mh] Termos MeSH secundário: Agonistas de Receptores Adrenérgicos alfa 1/farmacologia
Antagonistas de Receptores Adrenérgicos beta 2/farmacologia
Antagonistas de Receptores Adrenérgicos beta 3/farmacologia
Animais
Aorta/metabolismo
Arginina/farmacologia
Butoxamina/farmacologia
Técnicas In Vitro
Óxido Nítrico/metabolismo
Óxido Nítrico Sintase/antagonistas & inibidores
Fenilefrina/farmacologia
Pindolol/análogos & derivados
Pindolol/farmacologia
Ratos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic alpha-1 Receptor Agonists); 0 (Adrenergic beta-1 Receptor Agonists); 0 (Adrenergic beta-2 Receptor Antagonists); 0 (Adrenergic beta-3 Receptor Antagonists); 0 (Enzyme Inhibitors); 0 (Receptors, Adrenergic, beta-3); 030Y90569U (Nebivolol); 0NM31M53PW (Butoxamine); 1WS297W6MV (Phenylephrine); 31C4KY9ESH (Nitric Oxide); 4K0SD5SNFS (cyanopindolol); 63CV1GEK3Y (N,N-dimethylarginine); 94ZLA3W45F (Arginine); BJ4HF6IU1D (Pindolol); EC 1.14.13.39 (Nitric Oxide Synthase)
[Em] Mês de entrada:1610
[Cu] Atualização por classe:170103
[Lr] Data última revisão:
170103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160131
[St] Status:MEDLINE
[do] DOI:10.3109/10641963.2015.1081233


  3 / 3608 MEDLINE  
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[PMID]:26762097
[Au] Autor:Agapova OY; Skoblov YS; Zykov KA; Rvacheva AV; Beilina VB; Masenko VP; Chazova IE
[Ti] Título:[Radioligand Method of Assessment of ß-Adrenoceptor's Activity on Human T-Lymphocytes].
[So] Source:Bioorg Khim;41(5):592-8, 2015 Sep-Oct.
[Is] ISSN:0132-3423
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:We proposed a new method of evaluation of beta-receptor's activity on the surface of human T-lymphocytes based on the radioligand method. Optimal conditions for evaluation of specific binding to ß2-adrenoceptors of 0.5 fmol ligand per 1 million cells using [125I]-cyanopindolol were found. The possibility of using of ß2-adrenoceptor's activity assessment in clinical settings was demonstrated on human T-lymphocyte.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta
Pindolol/análogos & derivados
Receptores Adrenérgicos beta/metabolismo
Linfócitos T/metabolismo
[Mh] Termos MeSH secundário: Células Cultivadas
Seres Humanos
Radioisótopos do Iodo
Ligantes
Ligação Proteica
Ensaio Radioligante
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Iodine Radioisotopes); 0 (Ligands); 0 (Receptors, Adrenergic, beta); 4K0SD5SNFS (cyanopindolol); BJ4HF6IU1D (Pindolol)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:161126
[Lr] Data última revisão:
161126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160115
[St] Status:MEDLINE


  4 / 3608 MEDLINE  
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[PMID]:26385885
[Au] Autor:Sato T; Baker J; Warne T; Brown GA; Leslie AG; Congreve M; Tate CG
[Ad] Endereço:MRC Laboratory of Molecular Biology, Cambridge Biomedical Campus, Cambridge, United Kingdom (T.S., T.W., A.G.W.L., C.G.T.); Heptares Therapeutics Ltd, Welwyn Garden City, United Kingdom (G.A.B., M.C.); School of Life Sciences, University of Nottingham, Medical School, Queen's Medical Centre, Notting
[Ti] Título:Pharmacological Analysis and Structure Determination of 7-Methylcyanopindolol-Bound ß1-Adrenergic Receptor.
[So] Source:Mol Pharmacol;88(6):1024-34, 2015 Dec.
[Is] ISSN:1521-0111
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Comparisons between structures of the ß1-adrenergic receptor (AR) bound to either agonists, partial agonists, or weak partial agonists led to the proposal that rotamer changes of Ser(5.46), coupled to a contraction of the binding pocket, are sufficient to increase the probability of receptor activation. (RS)-4-[3-(tert-butylamino)-2-hydroxypropoxy]-1H-indole-2-carbonitrile (cyanopindolol) is a weak partial agonist of ß1AR and, based on the hypothesis above, we predicted that the addition of a methyl group to form 4-[(2S)-3-(tert-butylamino)-2-hydroxypropoxy]-7-methyl-1H-indole-2-carbonitrile (7-methylcyanopindolol) would dramatically reduce its efficacy. An eight-step synthesis of 7-methylcyanopindolol was developed and its pharmacology was analyzed. 7-Methylcyanopindolol bound with similar affinity to cyanopindolol to both ß1AR and ß2AR. As predicted, the efficacy of 7-methylcyanopindolol was reduced significantly compared with cyanopindolol, acting as a very weak partial agonist of turkey ß1AR and an inverse agonist of human ß2AR. The structure of 7-methylcyanopindolol-bound ß1AR was determined to 2.4-Å resolution and found to be virtually identical to the structure of cyanopindolol-bound ß1AR. The major differences in the orthosteric binding pocket are that it has expanded by 0.3 Å in 7-methylcyanopindolol-bound ß1AR and the hydroxyl group of Ser(5.46) is positioned 0.8 Å further from the ligand, with respect to the position of the Ser(5.46) side chain in cyanopindolol-bound ß1AR. Thus, the molecular basis for the reduction in efficacy of 7-methylcyanopindolol compared with cyanopindolol may be regarded as the opposite of the mechanism proposed for the increase in efficacy of agonists compared with antagonists.
[Mh] Termos MeSH primário: Pindolol/análogos & derivados
Receptores Adrenérgicos beta 1/química
Receptores Adrenérgicos beta 1/metabolismo
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação/fisiologia
Células CHO
Cricetinae
Cricetulus
Seres Humanos
Pindolol/química
Pindolol/metabolismo
Pindolol/farmacologia
Ligação Proteica/fisiologia
Estrutura Secundária de Proteína
Relação Estrutura-Atividade
Turquia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Receptors, Adrenergic, beta-1); 4K0SD5SNFS (cyanopindolol); BJ4HF6IU1D (Pindolol)
[Em] Mês de entrada:1602
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150920
[St] Status:MEDLINE
[do] DOI:10.1124/mol.115.101030


  5 / 3608 MEDLINE  
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[PMID]:25892302
[Au] Autor:Nautiyal KM; Tanaka KF; Barr MM; Tritschler L; Le Dantec Y; David DJ; Gardier AM; Blanco C; Hen R; Ahmari SE
[Ad] Endereço:Department of Psychiatry, Columbia University, New York, NY 10032, USA; Division of Integrative Neuroscience, the New York State Psychiatric Institute, New York, NY 10032, USA.
[Ti] Título:Distinct Circuits Underlie the Effects of 5-HT1B Receptors on Aggression and Impulsivity.
[So] Source:Neuron;86(3):813-26, 2015 May 06.
[Is] ISSN:1097-4199
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Impulsive and aggressive behaviors are both modulated by serotonergic signaling, specifically through the serotonin 1B receptor (5-HT1BR). 5-HT1BR knockout mice show increased aggression and impulsivity, and 5-HT1BR polymorphisms are associated with aggression and drug addiction in humans. To dissect the mechanisms by which the 5-HT1BR affects these phenotypes, we developed a mouse model to spatially and temporally regulate 5-HT1BR expression. Our results demonstrate that forebrain 5-HT1B heteroreceptors expressed during an early postnatal period contribute to the development of the neural systems underlying adult aggression. However, distinct heteroreceptors acting during adulthood are involved in mediating impulsivity. Correlating with the impulsivity, dopamine in the nucleus accumbens is elevated in the absence of 5-HT1BRs and normalized following adult rescue of the receptor. Overall, these data show that while adolescent expression of 5-HT1BRs influences aggressive behavior, a distinct set of 5-HT1B receptors modulates impulsive behavior during adulthood.
[Mh] Termos MeSH primário: Agressão/fisiologia
Encéfalo/anatomia & histologia
Regulação da Expressão Gênica no Desenvolvimento/fisiologia
Comportamento Impulsivo/fisiologia
Receptor 5-HT1B de Serotonina/metabolismo
[Mh] Termos MeSH secundário: Actinas/genética
Actinas/metabolismo
Animais
Animais Recém-Nascidos
Encéfalo/crescimento & desenvolvimento
Encéfalo/metabolismo
Comportamento de Escolha/fisiologia
Condicionamento Operante/efeitos dos fármacos
Condicionamento Operante/fisiologia
Dopamina/metabolismo
Inibidores da Captação de Dopamina/farmacologia
Doxiciclina/farmacologia
Regulação da Expressão Gênica no Desenvolvimento/efeitos dos fármacos
Regulação da Expressão Gênica no Desenvolvimento/genética
Isótopos de Iodo/farmacocinética
Camundongos
Camundongos Transgênicos
Pindolol/análogos & derivados
Pindolol/farmacocinética
Piperazinas/farmacologia
Ligação Proteica/efeitos dos fármacos
Receptor 5-HT1B de Serotonina/genética
Serotonina/metabolismo
Antagonistas da Serotonina/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Actins); 0 (Dopamine Uptake Inhibitors); 0 (Iodine Isotopes); 0 (Piperazines); 0 (Receptor, Serotonin, 5-HT1B); 0 (Serotonin Antagonists); 333DO1RDJY (Serotonin); 4K0SD5SNFS (cyanopindolol); 90X28IKH43 (vanoxerine); BJ4HF6IU1D (Pindolol); N12000U13O (Doxycycline); VTD58H1Z2X (Dopamine)
[Em] Mês de entrada:1507
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150421
[St] Status:MEDLINE


  6 / 3608 MEDLINE  
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[PMID]:25689398
[Au] Autor:Liu Y; Zhou X; Zhu D; Chen J; Qin B; Zhang Y; Wang X; Yang D; Meng H; Luo Q; Xie P
[Ad] Endereço:Department of Neurology, The First Affiliated Hospital of Chongqing Medical University, Chongqing, China; Institute of Neuroscience, Chongqing Medical University, Chongqing, China; Chongqing Key Laboratory of Neurobiology, Chongqing Medical University, Chongqing, China.
[Ti] Título:Is pindolol augmentation effective in depressed patients resistant to selective serotonin reuptake inhibitors? A systematic review and meta-analysis.
[So] Source:Hum Psychopharmacol;30(3):132-42, 2015 May.
[Is] ISSN:1099-1077
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: This systematic review and meta-analysis was conducted to assess the use of pindolol augmentation in depressed patients resistant to selective serotonin reuptake inhibitor (SSRI) therapy. METHODS: A comprehensive search of PubMed, Cochrane, Embase, Web of Science, and PsychINFO databases from 1970 through December 2013 was conducted. Only randomized controlled trials (RCTs) studied on unipolar SSRI-resistant depressed adults were included. The primary outcome was mean change scores of depressive symptom on the depression rating scales, assessed with standardized mean differences. RESULTS: Five RCTs consisting of 154 patients met all inclusion and exclusion criteria. The overall pooled effect size in the primary and secondary efficacy analysis showed no significant effects of pindolol plus SSRI therapy (standardized mean difference = -0.43, p = 0.24; OR = 1.92, p = 0.39, respectively). In terms of acceptability, there was no statistical difference in either tolerability or safety between the two groups (OR = 0.46, p = 0.40; OR = 0.90, p = 0.94, respectively). These estimates remained robust through several sensitivity and subgroup analyses, except 7.5 mg-qd pindolol augmentation did show a significant benefit over 2.5-mg tid pindolol augmentation. CONCLUSIONS: Pindolol augmentation may not be suitable for treatment-resistant depression patients with SSRI-resistant depression. However, once-daily high-dose pindolol (7.5 mg qd) appears to show a promising benefit in these patients.
[Mh] Termos MeSH primário: Transtorno Depressivo Resistente a Tratamento/tratamento farmacológico
Pindolol/uso terapêutico
Inibidores da Captação de Serotonina/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Transtorno Depressivo Resistente a Tratamento/fisiopatologia
Quimioterapia Combinada
Seres Humanos
Pindolol/administração & dosagem
Pindolol/efeitos adversos
Escalas de Graduação Psiquiátrica
Ensaios Clínicos Controlados Aleatórios como Assunto
Inibidores da Captação de Serotonina/administração & dosagem
Inibidores da Captação de Serotonina/efeitos adversos
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Serotonin Uptake Inhibitors); BJ4HF6IU1D (Pindolol)
[Em] Mês de entrada:1601
[Cu] Atualização por classe:150422
[Lr] Data última revisão:
150422
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150218
[St] Status:MEDLINE
[do] DOI:10.1002/hup.2465


  7 / 3608 MEDLINE  
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[PMID]:25610919
[Au] Autor:Cumba LR; Smith JP; Brownson DA; Iniesta J; Metters JP; do Carmo DR; Banks CE
[Ad] Endereço:Faculty of Science and Engineering, School of Chemistry and the Environment, Division of Chemistry and Environmental Science, Manchester Metropolitan University, Chester Street, Manchester M1 5GD, UK. c.banks@mmu.ac.uk.
[Ti] Título:Electroanalytical detection of pindolol: comparison of unmodified and reduced graphene oxide modified screen-printed graphite electrodes.
[So] Source:Analyst;140(5):1543-50, 2015 Mar 07.
[Is] ISSN:1364-5528
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Recent work has reported the first electroanalytical detection of pindolol using reduced graphene oxide (RGO) modified glassy carbon electrodes [S. Smarzewska and W. Ciesielski, Anal. Methods, 2014, 6, 5038] where it was reported that the use of RGO provided significant improvements in the electroanalytical signal in comparison to a bare (unmodified) glassy carbon electrode. We demonstrate, for the first time, that the electroanalytical quantification of pindolol is actually possible using bare (unmodified) screen-printed graphite electrodes (SPEs). This paper addresses the electroanalytical determination of pindolol utilising RGO modified SPEs. Surprisingly, it is found that bare (unmodified) SPEs provide superior electrochemical signatures over that of RGO modified SPEs. Consequently the electroanalytical sensing of pindolol is explored at bare unmodified SPEs where a linear range between 0.1 µM-10.0 µM is found to be possible whilst offering a limit of detection (3σ) corresponding to 0.097 µM. This provides a convenient yet analytically sensitive method for sensing pindolol. The optimised electroanalytical protocol using the unmodified SPEs, which requires no pre-treatment (electrode polishing) or electrode modification step (such as with the use of RGO), was then further applied to the determination of pindolol in urine samples. This work demonstrates that the use of RGO modified SPEs have no significant benefits when compared to the bare (unmodified) alternative and that the RGO free electrode surface can provide electro-analytically useful performances.
[Mh] Termos MeSH primário: Técnicas Biossensoriais/métodos
Técnicas Eletroquímicas/métodos
Eletrodos
Grafite/química
Óxidos/química
Pindolol/urina
[Mh] Termos MeSH secundário: Seres Humanos
Limite de Detecção
Microscopia Eletrônica de Varredura
Oxirredução
Análise Espectral Raman
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Oxides); 7782-42-5 (Graphite); BJ4HF6IU1D (Pindolol)
[Em] Mês de entrada:1509
[Cu] Atualização por classe:150216
[Lr] Data última revisão:
150216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150123
[St] Status:MEDLINE
[do] DOI:10.1039/c4an02005g


  8 / 3608 MEDLINE  
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[PMID]:25220702
[Au] Autor:Mallmann ES; Paixão L; Ribeiro MF; Spritzer PM
[Ad] Endereço:Gynecological Endocrinology Unit, Division of Endocrinology, Hospital de Clínicas de Porto Alegre (HCPA), Rua Ramiro Barcelos, 2350, 90035-003 Porto Alegre, Brazil; Division of Gynecology and Obstetrics, Hospital Presidente Vargas, Avenida Independência 661, 90035-070 Porto Alegre, Brazil.
[Ti] Título:Serotonergic 5-HT2A/2C receptors are involved in prolactin secretion in hyperestrogenic rats.
[So] Source:Neurosci Lett;582:71-4, 2014 Oct 17.
[Is] ISSN:1872-7972
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Serotonin (5-HT) has been shown to participate in prolactin secretion through a complex process resulting in both positive and negative effects. Estrogen has also been recognized as being involved in this serotonergic effect on prolactin release. Therefore, the aim of the present study was to assess whether estradiol modulates serotonergic involvement in prolactin secretion though 5-HT1A and/or 5-HT2A/2C receptors. Ovariectomized female Wistar rats, treated for 2 weeks with estrogen to induce a hyperprolactinemic status (hyperestrogenic rats) or with sunflower oil vehicle (hypoestrogenic rats), were injected daily with normal saline solution or 6-chloro-2-(1-piperazinyl)pyrazine (MK-212), an 5-HT2A/2C receptor agonist, for 4 days. Other groups of ovariectomized animals received 8-hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT) or pindolol, an agonist and antagonist of the 5-HT1A receptor respectively, on the last day of treatment with estrogen or vehicle. Prolactin levels were compared among groups in each experiment under the distinct drug treatments. MK-212 was found to increase prolactin concentrations both in hyper- and hypoestrogenic females compared to controls (p<0.05). In contrast, prolactin levels remained similar to those of controls both in hyperestrogenic animals treated with 8-OH-DPAT and pindolol and in hypoestrogenic rats administered the same treatments. In conclusion, our findings indicate the involvement of 5-HT2A/2C receptors on prolactin release through serotonergic pathways in female animals, especially in hyperestrogenic states.
[Mh] Termos MeSH primário: Estradiol/farmacologia
Estrogênios/farmacologia
Prolactina/secreção
Receptor 5-HT2A de Serotonina/metabolismo
Receptor 5-HT2C de Serotonina/metabolismo
[Mh] Termos MeSH secundário: 8-Hidroxi-2-(di-n-propilamino)tetralina/farmacologia
Animais
Feminino
Pindolol/farmacologia
Prolactina/sangue
Pirazinas/farmacologia
Ratos Wistar
Antagonistas da Serotonina/farmacologia
Agonistas de Receptores de Serotonina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Estrogens); 0 (Pyrazines); 0 (Receptor, Serotonin, 5-HT2A); 0 (Receptor, Serotonin, 5-HT2C); 0 (Serotonin Antagonists); 0 (Serotonin Receptor Agonists); 4TI98Z838E (Estradiol); 62C3N7238U (6-chloro-2-(1-piperazinyl)pyrazine); 78950-78-4 (8-Hydroxy-2-(di-n-propylamino)tetralin); 9002-62-4 (Prolactin); BJ4HF6IU1D (Pindolol)
[Em] Mês de entrada:1505
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140916
[St] Status:MEDLINE


  9 / 3608 MEDLINE  
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[PMID]:25148727
[Au] Autor:Briuglia ML; Urquhart AJ; Lamprou DA
[Ad] Endereço:Strathclyde Institute of Pharmacy and Biomedical Sciences (SIPBS), University of Strathclyde, 161 Cathedral Street, Glasgow, G4 0RE Scotland, UK.
[Ti] Título:Sustained and controlled release of lipophilic drugs from a self-assembling amphiphilic peptide hydrogel.
[So] Source:Int J Pharm;474(1-2):103-11, 2014 Oct 20.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Materials which undergo self-assembly to form supramolecular structures can provide alternative strategies to drug loading problems in controlled release application. RADA 16 is a simple and versatile self-assembling peptide with a designed structure formed of two distinct surfaces, one hydrophilic and one hydrophobic that are positioned in such a well-ordered fashion allowing precise assembly into a predetermined organization. A "smart" architecture in nanostructures can represent a good opportunity to use RADA16 as a carrier system for hydrophobic drugs solving problems of drugs delivery. In this work, we have investigated the diffusion properties of Pindolol, Quinine and Timolol maleate from RADA16 in PBS and in BSS-PLUS at 37°C. A sustained, controlled, reproducible and efficient drug release has been detected for all the systems, which allows to understand the dependence of release kinetics on the physicochemical characteristics of RADA16 structural and chemical properties of the selected drugs and the nature of solvents used. For the analysis various physicochemical characterization techniques were used in order to investigate the state of the peptide before and after the drugs were added. Not only does RADA16 optimise drug performance, but it can also provide a solution for drug delivery issues associated with lipophilic drugs.
[Mh] Termos MeSH primário: Hidrogel de Polietilenoglicol-Dimetacrilato/química
Peptídeos/química
Pindolol/farmacocinética
Quinina/farmacocinética
Tensoativos/química
Timolol/farmacocinética
[Mh] Termos MeSH secundário: Difusão
Interações Hidrofóbicas e Hidrofílicas
Estrutura Molecular
Pindolol/química
Quinina/química
Timolol/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Peptides); 0 (Surface-Active Agents); 25852-47-5 (Hydrogel, Polyethylene Glycol Dimethacrylate); 817W3C6175 (Timolol); A7V27PHC7A (Quinine); BJ4HF6IU1D (Pindolol)
[Em] Mês de entrada:1508
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140824
[St] Status:MEDLINE


  10 / 3608 MEDLINE  
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[PMID]:25135059
[Au] Autor:Putt TL; Duffull SB; Schollum JB; Walker RJ
[Ad] Endereço:Department of Medicine, University of Otago, Dunedin, New Zealand.
[Ti] Título:GFR may not accurately predict aspects of proximal tubule drug handling.
[So] Source:Eur J Clin Pharmacol;70(10):1221-6, 2014 Oct.
[Is] ISSN:1432-1041
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:PURPOSE: Dose modification in renal impairment has traditionally been based on changes in estimated glomerular filtration rate (eGFR; estimated by creatinine clearance). However, many drugs are eliminated by tubular anionic and cationic transport where changes in eGFR may not necessarily reflect changes in tubular function. This study investigated the relationship between GFR and renal tubular function with reference to drug handling by using accepted drug probes. METHODS: Three drug probes, (51)Cr-EDTA, fluconazole, and pindolol, were administered to patients who had varying degrees of renal impairment. Blood sampling, assays, and a pharmacokinetic analysis were performed for all drug probes and endogenous urate. Measured GFR ((51)Cr-EDTA clearance; mGFR) was compared to tubular anionic transport (urate clearance), tubular reabsorption (fluconazole clearance), and tubular cationic transport (S-pindolol clearance). RESULTS: A moderately strong association was demonstrated between the measured isotopic GFR and creatinine clearance (R(2) = 0.78). A moderate positive correlation was found between mGFR and proximal tubular anion transport and reabsorption (R(2) = 0.40-0.44, p < 0.0001). In contrast, cationic secretion correlated poorly with mGFR (R(2) = 0.11, p = 0.036). CONCLUSIONS: Given that drug dosing schedules utilise eGFR values as the basis for modifying drug dosing, our results would suggest that a recommendation of a dose reduction according to eGFR alone should be treated with caution.
[Mh] Termos MeSH primário: Taxa de Filtração Glomerular
Túbulos Renais Proximais/metabolismo
Insuficiência Renal/fisiopatologia
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Transporte Biológico/fisiologia
Relação Dose-Resposta a Droga
Ácido Edético/farmacocinética
Feminino
Fluconazol/farmacocinética
Seres Humanos
Testes de Função Renal/métodos
Masculino
Meia-Idade
Pindolol/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
8VZV102JFY (Fluconazole); 9G34HU7RV0 (Edetic Acid); BJ4HF6IU1D (Pindolol)
[Em] Mês de entrada:1505
[Cu] Atualização por classe:170920
[Lr] Data última revisão:
170920
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140820
[St] Status:MEDLINE
[do] DOI:10.1007/s00228-014-1733-7



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