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[PMID]:28525334
[Au] Autor:Markiewicz W; Jaroszewski JJ
[Ad] Endereço:.
[Ti] Título:Influence of ß2- and ß3-adrenoceptor agonists on contractile activity of the porcine myometrium in the luteal phase and the first days of pregnancy.
[So] Source:Pol J Vet Sci;20(1):111-121, 2017 Mar 28.
[Is] ISSN:1505-1773
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:This study analysed the relaxant properties of salbutamol (ß2-adrenoceptors agonist) and BRL 37344 (ß3-adrenoceptors agonist) regarding the contractility of porcine myometrium on days 10-14 of the oestrous cycle (cyclic group; n = 10) and on days 3-5 of pregnancy (early pregnant group; n = 6). The activity of myometrial strips (tension, frequency and amplitude) was recorded under isometric conditions using force transducers. The contractility was assessed further following the administration of increasing concentrations of the agonists (10-9-10-4 M), both with and without ß-adrenoceptor antagonists (butaxamine - a selective ß2- adrenoceptor antagonist, propranolol- a non-selective ß1- and ß2-adrenoceptor antagonist and bupranolol - a non-selective ß1-, ß2- and ß3-adrenoceptor antagonist) at a concentration of 10-4 M. Although neither salbutamol nor BRL 37344 caused changes in the tension, at the highest concentrations they decreased the frequency and amplitude of contractions. These changes were more evident after salbutamol treatment and in the early pregnant group. Antagonists given alone did not cause changes in the parameters examined but changed some activity of the agonists. Butoxamine reduced the decrease in frequency and amplitude induced by salbutamol and produced a decrease in the tension after BRL 37344 treatment in the early pregnant group. Propranolol reduced the decrease in frequency and amplitude induced by salbutamol in both examined groups and did not cause significant changes in BRL 37344 activity. The administration of bupranolol before salbutamol treatment caused an increase in the tension and reduced the decrease in the frequency in the cyclic group. Moreover, bupranolol eliminated a decrease in frequency and induced an increase in amplitude caused by BRL 37344 in both groups and these changes were more evident in the early pregnant group. The data indicates that both ß2- and ß3-adenoreceptors are involved in the regulation of the contractility in both groups, but the changes after agonists and antagonists treatment are more evident in the early pregnant myometrium.
[Mh] Termos MeSH primário: Agonistas de Receptores Adrenérgicos beta 2/farmacologia
Agonistas de Receptores Adrenérgicos beta 3/farmacologia
Corpo Lúteo/efeitos dos fármacos
Miométrio/fisiologia
Prenhez
Suínos/fisiologia
[Mh] Termos MeSH secundário: Albuterol/farmacocinética
Albuterol/farmacologia
Animais
Bupranolol/farmacocinética
Bupranolol/farmacologia
Butoxamina/farmacocinética
Butoxamina/farmacologia
Corpo Lúteo/fisiologia
Interações Medicamentosas
Etanolaminas/farmacocinética
Etanolaminas/farmacologia
Feminino
Gravidez
Prenhez/fisiologia
Contração Uterina/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-2 Receptor Agonists); 0 (Adrenergic beta-3 Receptor Agonists); 0 (Ethanolamines); 0NM31M53PW (Butoxamine); 5DZZ1926YW (BRL 37344); 858YGI5PIT (Bupranolol); QF8SVZ843E (Albuterol)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170520
[St] Status:MEDLINE


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[PMID]:26456674
[Au] Autor:Martin LJ; Piltonen MH; Gauthier J; Convertino M; Acland EL; Dokholyan NV; Mogil JS; Diatchenko L; Maixner W
[Ad] Endereço:Department of Psychology, McGill University, Montreal, Quebec, Canada; Alan Edwards Centre for Research on Pain, McGill University, Montreal, Quebec, Canada; Department of Psychology, University of Toronto Mississauga, Mississauga, Ontario, Canada. Electronic address: lj.martin@utoronto.ca.
[Ti] Título:Differences in the Antinociceptive Effects and Binding Properties of Propranolol and Bupranolol Enantiomers.
[So] Source:J Pain;16(12):1321-1333, 2015 Dec.
[Is] ISSN:1528-8447
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:UNLABELLED: Recent efforts have suggested that the ß-adrenergic receptor (ß-AR) system may be a novel and viable therapeutic target for pain reduction; however, most of the work to date has focused on the ß(2)-adrenergic receptor (AR). Here, we compared the antinociceptive effects of enantiomeric configurations of propranolol and bupranolol, two structurally similar nonselective ß-blocking drugs, against mouse models of inflammatory and chronic pain. In addition, we calculated in silico docking and measured the binding properties of propranolol and bupranolol for all 3 ß-ARs. Of the agents examined, S-bupranolol is superior in terms of its antinociceptive effect and exhibited fewer side effects than propranolol or its associated enantiomers. In contrast to propranolol, S-bupranolol exhibited negligible ß-AR intrinsic agonist activity and displayed a full competitive antagonist profile at ß(1)/ß(2)/ß(3)-ARs, producing a unique blockade of ß(3)-ARs. We have shown that S-bupranolol is an effective antinociceptive agent in mice without negative side effects. The distinctive profile of S-bupranolol is most likely mediated by its negligible ß-AR intrinsic agonist activity and unique blockade of ß(3)-AR. These findings suggest that S-bupranolol instead of propranolol may represent a new and effective treatment for a variety of painful conditions. PERSPECTIVE: The S enantiomer of bupranolol, a ß-receptor antagonist, shows greater antinociceptive efficacy and a superior preclinical safety profile and it should be considered as a unique ß-adrenergic receptor compound to advance future clinical pain studies.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/farmacologia
Analgésicos/farmacologia
Bupranolol/farmacologia
Nociceptividade/efeitos dos fármacos
Propranolol/farmacologia
Receptores Adrenérgicos beta/metabolismo
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/química
Analgésicos/química
Animais
Bupranolol/química
Modelos Animais de Doenças
Feminino
Masculino
Camundongos
Medição da Dor
Propranolol/química
Receptores Adrenérgicos beta/química
Estereoisomerismo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Analgesics); 0 (Receptors, Adrenergic, beta); 858YGI5PIT (Bupranolol); 9Y8NXQ24VQ (Propranolol)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:170729
[Lr] Data última revisão:
170729
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151013
[St] Status:MEDLINE


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[PMID]:25764496
[Au] Autor:Liu P; Li S; Jin Y; Qian L; Gao N; Yao SQ; Huang F; Xu QH; Cao Y
[Ad] Endereço:†Institute of Polymer Optoelectronic Materials and Devices, State Key Laboratory of Luminescent Materials and Devices, South China University of Technology, Guangzhou 510640, P. R. China.
[Ti] Título:Red-emitting DPSB-based conjugated polymer nanoparticles with high two-photon brightness for cell membrane imaging.
[So] Source:ACS Appl Mater Interfaces;7(12):6754-63, 2015 Apr 01.
[Is] ISSN:1944-8252
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:New red-emitting conjugated polymers have been successfully synthesized by incorporating classical two-photon absorption (TPA) units, electron-rich units, and a small amount of electron-deficient units along the polymer backbones. Water-dispersible nanoparticles (NPs) based on these polymers were also fabricated for applications in two-photon excitation fluorescence imaging of cell membrane. Through optimization of the polymer/matrix mass ratio and the initial feed concentration of the polymer solution, a high quantum yield (QY) of 24% was achieved for the red-emitting NPs in water. TPA cross section and two-photon action cross section values of these polymers at 750 nm reached up to 1000 GM and 190 GM per repeat unit in aqueous media, 2.5 × 10(5) GM and 4.7 × 10(4) GM per NP, respectively. Furthermore, these NPs displayed excellent photostability and biocompatibility. Their applications as two-photon excitation fluorescence probes for cell membrane imaging have been demonstrated in three different cell lines with excellent imaging contrast. These results demonstrated that these polymer NPs hold great potentials as excellent two-photon excitation fluorescence probes in various biological applications.
[Mh] Termos MeSH primário: Bupranolol/análogos & derivados
Membrana Celular/química
Corantes Fluorescentes/química
Imagem Molecular/instrumentação
Nanopartículas/química
[Mh] Termos MeSH secundário: Bupranolol/química
Linhagem Celular Tumoral
Seres Humanos
Imagem Molecular/métodos
Fótons
Polímeros/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Fluorescent Dyes); 0 (Polymers); 858YGI5PIT (Bupranolol); 99026-79-6 (2-((1-(2-chloro-5-methylphenoxy)-3-tert-butylamino-2-propoxy)succinyl)-1,3-dipalmitoylglyceroyl)
[Em] Mês de entrada:1601
[Cu] Atualização por classe:150401
[Lr] Data última revisão:
150401
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150313
[St] Status:MEDLINE
[do] DOI:10.1021/acsami.5b00223


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[PMID]:23283786
[Au] Autor:Servais AC; Fillet M
[Ad] Endereço:Department of Pharmaceutical Sciences, University of Liège, Liège, Belgium. acservais@ulg.ac.be
[Ti] Título:Enantioseparations in nonaqueous capillary electrophoresis using charged cyclodextrins.
[So] Source:Methods Mol Biol;970:297-305, 2013.
[Is] ISSN:1940-6029
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The enantioseparation of acidic and basic compounds can be successfully achieved in nonaqueous capillary electrophoresis using single-isomer charged ß-cyclodextrin (ß-CD) derivatives of opposite charge to that of the analytes. This chapter describes how to separate the enantiomers of three basic substances selected as model compounds, i.e., alprenolol, bupranolol, and terbutaline, using the negatively charged heptakis(2,3-di-O-acetyl-6-O-sulfo)-ß-CD. The enantiomers of three acidic drugs (tiaprofenic acid, suprofen, and flurbiprofen) are resolved using a monosubstituted amino ß-CD derivative, namely, 6-monodeoxy-6-mono(3-hydroxy)propylamino-ß-CD.
[Mh] Termos MeSH primário: Eletroforese Capilar/métodos
beta-Ciclodextrinas/análise
beta-Ciclodextrinas/química
[Mh] Termos MeSH secundário: Alprenolol/análise
Alprenolol/química
Bupranolol/análise
Bupranolol/química
Flurbiprofeno/análise
Flurbiprofeno/química
Propionatos/análise
Propionatos/química
Estereoisomerismo
Suprofeno/análise
Suprofeno/química
Temperatura Ambiente
Terbutalina/análise
Terbutalina/química
Raios Ultravioleta
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (6-monodeoxy-6-mono(3-hydroxy)propylamino-beta-cyclodextrin); 0 (Propionates); 0 (beta-Cyclodextrins); 1LS1T6R34C (tiaprofenic acid); 5GRO578KLP (Flurbiprofen); 858YGI5PIT (Bupranolol); 877K5MQ27W (Alprenolol); 988GU2F9PE (Suprofen); N8ONU3L3PG (Terbutaline)
[Em] Mês de entrada:1306
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130104
[St] Status:MEDLINE
[do] DOI:10.1007/978-1-62703-263-6_19


  5 / 197 MEDLINE  
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[PMID]:20550434
[Au] Autor:Mishra B; Sankar C; Mishra M
[Ad] Endereço:Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, India. bmishrabhu@rediffmail.com
[Ti] Título:Polymer based solutions of bupranolol hydrochloride for intranasal systemic delivery.
[So] Source:J Drug Target;19(3):204-11, 2011 Apr.
[Is] ISSN:1029-2330
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The present study was aimed at developing intranasal polymer based solutions as alternative route for systemic delivery of Bupranolol hydrochloride (BPH). It is a potent ß-blocker drug which upon oral administration undergoes extremely high hepatic first-pass metabolism (>90% in humans). The polymeric solutions were prepared using varying concentrations of polymers like sodium alginate, chitosan, sodium carboxymethylcellulose, methylcellulose (MC), polyvinyl alcohol, carbopol, hydroxypropyl MC, and hydroxypropyl cellulose. The prepared formulations were evaluated in terms of pH of the solution, angular viscosity, drug content, gel strength, gelation temperature, in vitro drug release, in vivo pharmacodynamic studies, histopathological, and stability studies. Except MC based solutions, a biphasic pattern of drug release was obtained in all other cases. Nasal administration of selected batches of polymeric solutions were found to be nontoxic and were able to improve drug bioavailability when compared to oral, nasal, and intravenous solution administrations of BPH.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/química
Bupranolol/química
Polímeros/química
[Mh] Termos MeSH secundário: Adesividade/efeitos dos fármacos
Administração Intranasal
Administração através da Mucosa
Antagonistas Adrenérgicos beta/farmacocinética
Antagonistas Adrenérgicos beta/farmacologia
Animais
Bupranolol/farmacocinética
Bupranolol/farmacologia
Estabilidade de Medicamentos
Feminino
Concentração de Íons de Hidrogênio/efeitos dos fármacos
Masculino
Coelhos
Soluções
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Polymers); 0 (Solutions); 858YGI5PIT (Bupranolol)
[Em] Mês de entrada:1110
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100617
[St] Status:MEDLINE
[do] DOI:10.3109/1061186X.2010.492520


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[PMID]:20424137
[Au] Autor:Hsu IR; Zuniga E; Bergman RN
[Ad] Endereço:Keck School of Medicine, University of Southern California, 1333 San Pablo Street, Los Angeles, CA 90033, USA.
[Ti] Título:Pulsatile changes in free fatty acids augment hepatic glucose production and preserves peripheral glucose homeostasis.
[So] Source:Am J Physiol Endocrinol Metab;299(1):E131-6, 2010 Jul.
[Is] ISSN:1522-1555
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Recent studies in animal and human models have revealed that free fatty acid (FFA) release from adipose tissue is oscillatory. We have shown in our laboratory that these oscillations are controlled by the sympathetic nervous system (SNS). Although FFAs have been shown to directly stimulate glucose production [endogenous glucose production (EGP)] by the liver and to reduce peripheral glucose utilization, whether the specific pattern of FFA release affects glucose metabolism is unknown. The aim of this study was to examine the effects of pulsatile vs. constant infusion of FFA on glucose homeostasis in the canine model. Euglycemic clamps with basal insulin replacement (0.1 mU.kg(-1).min(-1) insulin) were performed in dogs (n = 8) during infusion of saline (SAL) or the medium-chain fatty acid octanoate, which was given by either pulsatile infusion (PUL: 10 mmol over 2 min every 10 min) or continuous infusion (C-INF: 1 mmol/min) designed to achieve equivalent total FFA mass. Endogenous lipolytic pulses were suppressed with the beta(3)-specific adrenergic receptor antagonist bupranolol. PUL infusion elicited a pulsatile pattern of FFA in circulation with average maximum pulse height of 0.82 +/- 0.04 mM, whereas C-INF FFA levels reached 0.47 +/- 0.03 mM (fasting levels) and were maintained throughout. Glucose uptake was not affected by PUL; however, C-INF significantly reduced glucose uptake compared with both SAL and PUL. Steady-state EGP increased by >90% from basal steady state during PUL but did not change during either SAL or C-INF. Thus, pulsatile FFA infusion led to an increase in EGP while preserving glucose disposal. These data suggest that the pattern of FFA may have a role in regulation of glucose homeostasis, which may have consequences in the obese or insulin-resistant state where the SNS is known to be altered.
[Mh] Termos MeSH primário: Ácidos Graxos não Esterificados/metabolismo
Glucose/metabolismo
Fígado/metabolismo
[Mh] Termos MeSH secundário: Animais
Anti-Hipertensivos/farmacologia
Relógios Biológicos/fisiologia
Bupranolol/farmacologia
Cães
Homeostase
Masculino
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antihypertensive Agents); 0 (Fatty Acids, Nonesterified); 858YGI5PIT (Bupranolol); IY9XDZ35W2 (Glucose)
[Em] Mês de entrada:1007
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100429
[St] Status:MEDLINE
[do] DOI:10.1152/ajpendo.00427.2009


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[PMID]:19439807
[Au] Autor:Zelaszczyk D; Kozlowska H; Baranowska U; Baranowska M; Reutelsterz A; Kiec-Kononowicz K; Malinowska B; Schlicker E
[Ad] Endereço:Department of Technology and Biotechnology of Drugs, Medical College of Jagiellonian University of Cracow, Poland.
[Ti] Título:Four close bupranolol analogues are antagonists at the low-affinity state of beta1-adrenoceptors.
[So] Source:J Physiol Pharmacol;60(1):51-60, 2009 Mar.
[Is] ISSN:1899-1505
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:Bupranolol is an antagonist at the cardiostimulatory low-affinity state of b(1)-adrenoceptors and we were interested whether this effect is shared by its fluorine (GD-6), methyl (DZ-51) and isopropyl analogue (DZ-13) and by the analogue hydroxylated at the tertiary butyl moiety (DZ-52). (-)-Bupranolol and compounds (-)-GD-6, (+)-GD-6, (-)-DZ-13, (+)-DZ-13, DZ-51 and DZ-52 antagonized the CGP 12177-induced tachycardia in pithed rats with "apparent pA(2) values" of 6.1, 6.1, 4.6, 5.5, 4.6, 5.1 and 5.3, respectively. For comparison, their potencies and affinities at the high-affinity state of b(1)-adrenoceptors were determined, using the xamoterol-induced tachycardia in pithed rats and [(3)H]CGP 12177 binding to rat cerebrocortical membranes. The respective "apparent pA(2) values" in the functional experiments were 7.9, 8.1, 5.4, 8.4, 5.7, 7.3 and 6.8 and the pK(i) values in the binding experiments were 8.8, 8.4, 6.9, 8.5, 6.7, 8.4 and 8.2. In conclusion, (-)-bupranolol and its fluorine analogue (-)-GD-6 are equipotent at the low-affinity state of beta(1)-adrenoceptors. The stereoselectivity of GD-6 and DZ-13 suggests that the low-affinity state is indeed a receptor.
[Mh] Termos MeSH primário: Antagonistas de Receptores Adrenérgicos beta 1
Antagonistas Adrenérgicos beta/farmacologia
Bupranolol/farmacologia
Taquicardia/prevenção & controle
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação
Bupranolol/análogos & derivados
Córtex Cerebral/metabolismo
Masculino
Propanolaminas/farmacologia
Ratos
Ratos Wistar
Estereoisomerismo
Xamoterol/farmacologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Adrenergic beta-Antagonists); 0 (Propanolamines); 7HE0JQL703 (Xamoterol); 858YGI5PIT (Bupranolol); R89UMZ82MJ (CGP 12177)
[Em] Mês de entrada:0907
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090515
[St] Status:MEDLINE


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[PMID]:18096189
[Au] Autor:Babu RJ; Dhanasekaran M; Vaithiyalingam SR; Singh PN; Pandit JK
[Ad] Endereço:Department of Pharmacal Sciences, Harrison School of Pharmacy, Auburn University, AL 36849, USA.
[Ti] Título:Cardiovascular effects of transdermally delivered bupranolol in rabbits: effect of chemical penetration enhancers.
[So] Source:Life Sci;82(5-6):273-8, 2008 Jan 30.
[Is] ISSN:0024-3205
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Bupranolol is a promising candidate for transdermal drug delivery system (TDDS) development. The effect of permeation enhancers on the in vivo delivery and beta-blocking effect of reservoir type TDDS was studied in comparison with intravenous BPL in rabbits. The beta-blocking effect was quantified by measuring the inhibition of isoprenaline induced tachycardia in rabbits after BPL administration via transdermal and intravenous routes. The reservoir type TDDS containing a hydroxypropyl cellulose gel and polyethylene membrane was used as a control device. In comparison, the TDDS containing skin penetration enhancers, either 2-pyrrolidone or partially methylated beta cyclodextrin (PMbetaCD) were evaluated. The control device (no enhancer) produced about 52% inhibition of isoprenaline induced tachycardia at 2 h and the effect continued over 24 h application period, however, the devices with 2-pyrolidone or PMbetaCD produced about 85% inhibition of isoprenaline induced tachycardia at 3 h and the same effect continued over 24 h application period. Likewise, the AUC of these devices were significantly higher than that of control device. The intravenous bupranolol showed rapid decline in the pharmacodynamic effect with time indicating its rapid elimination. The in vivo delivery of bupranolol (as estimated by a mass balance study) from the devices made with pyrolidone or PMbetaCD was 3-fold higher than that of control. The results of this study strongly suggest that the penetration enhancers in the TDDS increased the in vivo delivery of BPL, thereby increased the beta-blocking activity of BPL by 50-60% higher than control, enabling the reduction of the TDDS patch size, accordingly.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/administração & dosagem
Bupranolol/administração & dosagem
Sistemas de Liberação de Medicamentos
Pirrolidinonas/administração & dosagem
beta-Ciclodextrinas/administração & dosagem
[Mh] Termos MeSH secundário: Administração Cutânea
Antagonistas Adrenérgicos beta/farmacocinética
Animais
Área Sob a Curva
Bupranolol/farmacocinética
Antagonismo de Drogas
Feminino
Frequência Cardíaca/efeitos dos fármacos
Injeções Intravenosas
Isoproterenol/farmacologia
Masculino
Permeabilidade/efeitos dos fármacos
Pirrolidinonas/farmacocinética
Coelhos
Pele/efeitos dos fármacos
Pele/metabolismo
Absorção Cutânea/efeitos dos fármacos
Taquicardia/induzido quimicamente
Taquicardia/tratamento farmacológico
Taquicardia/fisiopatologia
beta-Ciclodextrinas/farmacocinética
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Pyrrolidinones); 0 (beta-Cyclodextrins); 0 (methyl-beta-cyclodextrin); 858YGI5PIT (Bupranolol); KKL5D39EOL (2-pyrrolidone); L628TT009W (Isoproterenol)
[Em] Mês de entrada:0803
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:071222
[St] Status:MEDLINE


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[PMID]:17632099
[Au] Autor:Clouse AK; Riedel E; Hieble JP; Westfall TD
[Ad] Endereço:Department of Urogenital Biology, Cardiovascular and Urogenital Center of Excellence for Drug Discovery, GlaxoSmithKline Pharmaceuticals, P.O. Box 1539, 709 Swedeland Road, King of Prussia, PA 19406 USA.
[Ti] Título:The effects and selectivity of beta-adrenoceptor agonists in rat myometrium and urinary bladder.
[So] Source:Eur J Pharmacol;573(1-3):184-9, 2007 Nov 14.
[Is] ISSN:0014-2999
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Recent evidence supports a role for beta(3)-adrenoceptors in human non-pregnant and pregnant myometrium. The present study was designed to characterize the pharmacology of beta-adrenoceptors involved in the function of non-pregnant rat myometrium by comparison of the activity of several beta-adrenoceptor agonists and antagonists in isolated rat uterus and urinary bladder. Contractions of myometrial and detrusor strips were induced by adding 1 nM oxytocin and 15 mM KCl respectively. Cumulative concentration-response curves to the selective beta(3)-adrenoceptor agonists, CL 316243 and BRL 37344 and the selective beta(2)-adrenoceptor agonist ritodrine were obtained in the presence and absence of the selective beta(2)-adrenoceptor antagonist ICI 118551 and the non-selective beta-adrenoceptor antagonist bupranolol. Both BRL 37344 (pD(2)=6.79+/-0.09) and ritodrine (pD(2)=6.89+/-0.19) produced potent inhibition of oxytocin-induced contractions in myometrial strips; CL 316243 was inactive at concentrations up to 10 microM. Concentration effect curves to both BRL 37344 and ritodrine were shifted (10 to 30-fold) to the right in the presence of ICI 118551 (10 nM). BRL 37344 (pD(2)=8.51+/-0.21) and CL 316243 (pD(2)=8.61+/-0.24) produced potent inhibition of detrusor strips, while ritodrine was almost 100-fold less potent (pD(2)=5.83+/-0.17). The response to all agonists was significantly attenuated by pretreatment with bupranolol (10 microM), but only ritodrine was affected by ICI 118551 (1 microM). These results demonstrate that relaxation of rat myometrium is mediated by beta(2)-adrenoceptors while, consistent with previous reports, the beta(3)-subtype is primarily responsible for relaxation of rat detrusor.
[Mh] Termos MeSH primário: Agonistas Adrenérgicos beta/farmacologia
Contração Muscular/efeitos dos fármacos
Miométrio/efeitos dos fármacos
Bexiga Urinária/efeitos dos fármacos
[Mh] Termos MeSH secundário: Agonistas de Receptores Adrenérgicos beta 2
Antagonistas de Receptores Adrenérgicos beta 2
Agonistas de Receptores Adrenérgicos beta 3
Antagonistas de Receptores Adrenérgicos beta 3
Antagonistas Adrenérgicos beta/farmacologia
Animais
Bupranolol/farmacologia
Dioxóis/farmacologia
Relação Dose-Resposta a Droga
Etanolaminas/farmacologia
Feminino
Técnicas In Vitro
Relaxamento Muscular/efeitos dos fármacos
Miométrio/fisiologia
Ocitócicos/farmacologia
Ocitocina/farmacologia
Cloreto de Potássio/farmacologia
Propanolaminas/farmacologia
Ratos
Ratos Sprague-Dawley
Receptores Adrenérgicos beta 2/fisiologia
Receptores Adrenérgicos beta 3/fisiologia
Ritodrina/farmacologia
Bexiga Urinária/fisiologia
Contração Uterina/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-2 Receptor Agonists); 0 (Adrenergic beta-2 Receptor Antagonists); 0 (Adrenergic beta-3 Receptor Agonists); 0 (Adrenergic beta-3 Receptor Antagonists); 0 (Adrenergic beta-Agonists); 0 (Adrenergic beta-Antagonists); 0 (Dioxoles); 0 (Ethanolamines); 0 (Oxytocics); 0 (Propanolamines); 0 (Receptors, Adrenergic, beta-2); 0 (Receptors, Adrenergic, beta-3); 138908-40-4 (disodium (R,R)-5-(2-((2-(3-chlorophenyl)-2-hydroxyethyl)-amino)propyl)-1,3-benzodioxole-2,3-dicarboxylate); 46OL1UC10R (ICI 118551); 50-56-6 (Oxytocin); 5DZZ1926YW (BRL 37344); 660YQ98I10 (Potassium Chloride); 858YGI5PIT (Bupranolol); I0Q6O6740J (Ritodrine)
[Em] Mês de entrada:0803
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:070717
[St] Status:MEDLINE


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[PMID]:17280840
[Au] Autor:Evangelista S; Garbin U; Pasini AF; Stranieri C; Boccioletti V; Cominacini L
[Ad] Endereço:Preclinical Development Department, Menarini Ricerche spa, Via Sette Santi 1, 50131 Firenze, Italy. sevangelista@menarini-ricerche.it
[Ti] Título:Effect of DL-nebivolol, its enantiomers and metabolites on the intracellular production of superoxide and nitric oxide in human endothelial cells.
[So] Source:Pharmacol Res;55(4):303-9, 2007 Apr.
[Is] ISSN:1043-6618
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Nebivolol, a third generation selective beta(1)-adrenoceptor (beta(1)-AR) antagonist, has been reported to reduce intracellular oxidative stress and to induce the release of nitric oxide (NO) from the endothelium. Nebivolol is also subjected to a complex metabolic process where glucuronidation, aromatic and alicyclic hydroxylation are the major pathways leading to several metabolites. We have studied the effect of nebivolol, its enantiomers and metabolites on intracellular oxidative stress and NO availability in human umbilical vein endothelial cells (HUVECs). Furthermore, since the receptors involved in this endothelial effect of nebivolol remain controversial, we have studied this matter by the use of antagonists of beta-AR. dl-Nebivolol, d-nebivolol and l-nebivolol significantly reduced the formation of reactive oxygen species (ROS) and superoxide induced by oxidized-low density lipoprotein (ox-LDL), although the racemic and l-form were significantly more active than d-nebivolol in this activity. A marked decrease in the availability of intracellular NO was found in HUVECs exposed to ox-LDL and this parameter was normalized by the prior incubation with dl-nebivolol, d-nebivolol and l-nebivolol; the effect of racemate was mainly mimicked by its l-enantiomer. eNOS activity significantly increased by a 5-min contact of HUVECs with dl-nebivolol and l-nebivolol, but not with d-nebivolol, and a similar pattern was observed when the intracellular calcium increase was measured. The metabolites A2, A3', A12 and A14 but not A1, A3 and R 81,928, derived from different metabolic pathways, retained the antioxidant activity of the parent racemic compound dl-nebivolol, reducing the intracellular formation of ROS and superoxide. The effects of dl-nebivolol on intracellular formation of NO, eNOS activity and intracellular Ca(2+) were partially antagonized by the antagonists of beta(1-2)-AR nadolol or by the beta(3)-AR antagonist SR59230A and further antagonized by their combination or by (beta(1-2-3)-AR antagonist bupranolol. In conclusion, this study shows that the NO releasing effect of nebivolol is mainly due to its l-enantiomer; the racemate and its enantiomers possess a remarkable antioxidant activity that contributes to its effect on the cellular NO metabolism and the activation of beta(3)-AR through a calcium dependent pathway is involved in the mechanisms leading to the NO release.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/farmacologia
Antioxidantes/farmacologia
Benzopiranos/farmacologia
Células Endoteliais/efeitos dos fármacos
Etanolaminas/farmacologia
Óxido Nítrico/metabolismo
Estresse Oxidativo/efeitos dos fármacos
Superóxidos/metabolismo
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/química
Antagonistas Adrenérgicos beta/metabolismo
Antioxidantes/química
Antioxidantes/metabolismo
Benzopiranos/química
Benzopiranos/metabolismo
Biotransformação
Bupranolol/farmacologia
Cálcio/metabolismo
Células Cultivadas
Células Endoteliais/metabolismo
Ativação Enzimática/efeitos dos fármacos
Etanolaminas/química
Etanolaminas/metabolismo
Seres Humanos
Lipoproteínas LDL/metabolismo
Nadolol/farmacologia
Nebivolol
Óxido Nítrico Sintase Tipo III/metabolismo
Propanolaminas/farmacologia
Receptores Adrenérgicos beta/efeitos dos fármacos
Receptores Adrenérgicos beta/metabolismo
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (3-(2-ethylphenoxy)-1-(1,2,3,4-tetrahydronaphth-1-ylamino)-2-propanol oxalate); 0 (Adrenergic beta-Antagonists); 0 (Antioxidants); 0 (Benzopyrans); 0 (Ethanolamines); 0 (Lipoproteins, LDL); 0 (Propanolamines); 0 (Receptors, Adrenergic, beta); 0 (oxidized low density lipoprotein); 030Y90569U (Nebivolol); 11062-77-4 (Superoxides); 31C4KY9ESH (Nitric Oxide); 42200-33-9 (Nadolol); 858YGI5PIT (Bupranolol); EC 1.14.13.39 (NOS3 protein, human); EC 1.14.13.39 (Nitric Oxide Synthase Type III); SY7Q814VUP (Calcium)
[Em] Mês de entrada:0708
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:070207
[St] Status:MEDLINE



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