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[PMID]:26383739
[Au] Autor:Ita KB; Popova IE
[Ad] Endereço:a College of Pharmacy, Touro University , Mare Island-Vallejo , CA , USA and.
[Ti] Título:Influence of sonophoresis and chemical penetration enhancers on percutaneous transport of penbutolol sulfate.
[So] Source:Pharm Dev Technol;21(8):990-995, 2016 Dec.
[Is] ISSN:1097-9867
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The effect of ultrasound and chemical penetration enhancers on transcutaneous flux of penbutolol sulfate across split-thickness porcine skin was investigated. Penbutolol sulfate is a potent, noncardioselective beta-blocker, which is used for the management of hypertension. The drug is one of the most lipid soluble of the ß-adrenoceptor antagonists used clinically. It has an n-octanol/pH 7.4 buffer partition coefficient of 179 compared to a value of 22 for propranolol. The amount of penbutolol sulfate transported across the skin is low. In this project, we studied the effect of sonophoresis and chemical penetration enhancers on transdermal delivery of penbutolol sulfate. Low-frequency sonophoresis at a frequency of 20 kHz increased transcutaneous flux of penbutolol sulfate by 3.5-fold (27.37 ± µg cm h ) compared to passive delivery (7.82 ± 1.72 µg cm h ). We also investigated the effect of 50% ethanol, 1% limonene and 2% isopropyl myristate (IPM) on transcutaneous permeation of penbutolol sulfate. IPM, ethanol and limonene at the concentration of 1%, 50% and 2%, respectively, increased the steady-state flux values of penbutolol sulfate 2.2- (17.07 ± 3.24 µg cm h ), 2.6 - (19.40 ± 6.40 µg cm h ) and 3.4-times (26.38 ± 5.01 µg cm h ) compared to passive delivery (7.76 ± 2.9 µg cm h ). The results demonstrate that although there were slight increases in flux values, ultrasound, ethanol, limonene and IPM did not significantly enhance the transdermal delivery of penbutolol sulfate. Future studies will examine ways of optimizing sonophoretic and chemical enhancer parameters to achieve flux enhancement.
[Mh] Termos MeSH primário: Portadores de Fármacos/química
Pembutolol/administração & dosagem
Pembutolol/química
Pele/metabolismo
[Mh] Termos MeSH secundário: Administração Cutânea
Antagonistas Adrenérgicos beta/administração & dosagem
Antagonistas Adrenérgicos beta/química
Animais
Cicloexenos/química
Sistemas de Liberação de Medicamentos/métodos
Etanol/química
Miristatos/química
Permeabilidade
Absorção Cutânea
Solubilidade
Suínos
Terpenos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Cyclohexenes); 0 (Drug Carriers); 0 (Myristates); 0 (Terpenes); 0RE8K4LNJS (isopropyl myristate); 3K9958V90M (Ethanol); 78W62V43DY (Penbutolol); 9MC3I34447 (limonene)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170314
[Lr] Data última revisão:
170314
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150919
[St] Status:MEDLINE


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[PMID]:25434124
[Au] Autor:Zheng L; Wu Y; Zhao Y; Li L; Ma Y
[Ti] Título:[Simultaneous determination of 18 ß-agonist residues in feed using QuEChERS sample preparation and high performance liquid chromatography-tandem mass spectrometry].
[So] Source:Se Pu;32(8):867-73, 2014 Aug.
[Is] ISSN:1000-8713
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:A multi-residue method was developed for the simultaneous determination of 18 ß-agonist residues (clenbuterol, ractopamine, penbutolol, tulobuterol, etc) in feed by using QuEChERS sample preparation and high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). The feed samples were dispersed by water, then the analytes were extracted with acetonitrile containing 4% (v/v) ammonia and cleaned up by QuEChERS method with 25 mg octadecylsilyl (C18) and 50 mg primary secondary amine (PSA) adsorbents. The separation of compounds was carried on an Agilent ZORBAX Eclipse XDB-C,8 column (50 mm x 4. 6 mm, 1. 8 µm) by a gradient elution using methanol-0. 1% (v/v) formic acid aqueous solution as mobile phase. The analytes were detected by tandem mass spectrometry under multiple reaction monitoring (MRM) mode with positive electrospray ionization (ESI+) and quantified by the matrix-matched external standard method. The results showed that the calibration curves of the 18 ß-agonists were linear in the range of 5 - 200 µg/L with correlation coefficients of 0. 9912-0. 9995. The average recoveries of the 18 analytes at three spiked levels of 0.05, 0.1 and 0. 5 mg/kg ranged from 78. 4% to 107. 1% with the relative standard deviations (RSDs) of 3.5%-12.3%. The limit of quantification (LOQ, S/N≥10) was 0. 05 mg/kg for each analyte. The developed method is simple and sensitive, and can be applied as a screen and confirmatory method for the analysis of ß-agonists in feed.
[Mh] Termos MeSH primário: Agonistas Adrenérgicos beta/análise
Ração Animal/análise
Cromatografia Líquida de Alta Pressão
Resíduos de Drogas/análise
Espectrometria de Massas em Tandem
[Mh] Termos MeSH secundário: Clembuterol
Pembutolol
Fenetilaminas
Terbutalina/análogos & derivados
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-Agonists); 0 (Phenethylamines); 57370OZ3P1 (ractopamine); 591I9SU0F7 (tulobuterol); 78W62V43DY (Penbutolol); N8ONU3L3PG (Terbutaline); XTZ6AXU7KN (Clenbuterol)
[Em] Mês de entrada:1509
[Cu] Atualização por classe:161018
[Lr] Data última revisão:
161018
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141202
[St] Status:MEDLINE


  3 / 176 MEDLINE  
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[PMID]:19555303
[Au] Autor:Ita KB; Banga AK
[Ad] Endereço:Department of Pharmaceutical Sciences, College of Pharmacy, Touro University, Mare Island-Vallejo, California 94592, USA. Kevin.ita@touro.edu
[Ti] Título:In vitro transdermal iontophoretic delivery of penbutolol sulfate.
[So] Source:Drug Deliv;16(1):11-4, 2009 Jan.
[Is] ISSN:1521-0464
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Iontophoretic transport of penbutolol sulfate across porcine ear skin was studied. Passive transdermal flux of the drug in phosphate-buffered saline was 7.65 microg/cm(2) hr. There was statistically significant flux enhancement when direct current iontophoresis was applied. Iontophoresis (0.11 mA/cm(2), 0.17 mA/cm(2), and 0.22 mA/cm(2)) for 6 hr, resulted in net transport of 87.36 microg/cm(2), 137.51 microg/cm(2), and 201.12 microg/cm(2) of penbutolol sulfate, respectively. After 24 hr, cumulative amount of penbutolol transported were 201.63, 300.76, and 359.98 microg/cm(2), respectively. There was a 2.20- (0.11 mA/cm(2)), 3.26- (0.17 m/Acm(2)), and 4.28-fold (0.22 mA/cm(2)) enhancement in transcutaneous steady-state flux values compared to passive delivery. Steady-state fluxes of penbutolol sulfate also increased proportionally to current density. Steady-state fluxes calculated from the linear portion of the cumulative amount versus time curves for penbutolol sulfate were 16.68, 24.97, and 32.76 microg/cm(2)/hr at current densities of 0.11, 0.17, and 0.22 mA/cm(2). This study provides initial evidence for the potential use of iontophoresis for enhanced transdermal delivery of penbutolol sulfate.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/administração & dosagem
Iontoforese/métodos
Pembutolol/administração & dosagem
Absorção Cutânea
[Mh] Termos MeSH secundário: Administração Cutânea
Antagonistas Adrenérgicos beta/farmacocinética
Animais
Transporte Biológico
Sistemas de Liberação de Medicamentos
Técnicas In Vitro
Pembutolol/farmacocinética
Suínos
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 78W62V43DY (Penbutolol)
[Em] Mês de entrada:0909
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090627
[St] Status:MEDLINE
[do] DOI:10.1080/10717540802396976


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[PMID]:11734181
[Au] Autor:Courade JP; Chassaing C; Bardin L; Alloui A; Eschalier A
[Ad] Endereço:Laboratoire de Pharmacologie Médicale, Faculté de Médecine, EMI 9904 INSERM/Université d'Auvergne, BP 38, 30, Place Henri Dunant, 63001 cedex 1, Clermont-Ferrand, France.
[Ti] Título:5-HT receptor subtypes involved in the spinal antinociceptive effect of acetaminophen in rats.
[So] Source:Eur J Pharmacol;432(1):1-7, 2001 Nov 30.
[Is] ISSN:0014-2999
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The present study was designed to investigate which subtype of spinal 5-HT receptors were involved in acetaminophen-induced antinociception using the paw-pressure test. Propacetamol (prodrug of acetaminophen, 400 mg/kg, injected intravenously, corresponding to 200 mg/kg of acetaminophen) produced a significant antinociceptive effect in this test. This effect was at least partially inhibited by intrathecal (i.t.) pretreatment with the 5-HT(1B) (penbutolol), 5-HT(2A) (ketanserin), 5-HT(2C) (mesulergine) receptor antagonists, but not by the 5-HT(1A) (N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclohexanecarboxamide trihydrochloride, WAY 100635) and 5-HT(3) (granisetron) receptor antagonists. This profile was very close to that obtained recently with 5-HT, which suggests an implication of 5-HT in the spinal antinociceptive effect of acetaminophen. These results, the lack of binding of acetaminophen to 5-HT receptors and the increase of central 5-HT levels induced by this drug suggest that acetaminophen-induced antinociception could be indirectly mediated by 5-HT.
[Mh] Termos MeSH primário: Acetaminofen/farmacologia
Analgésicos/farmacologia
Receptores de Serotonina/fisiologia
[Mh] Termos MeSH secundário: Animais
Ergolinas/farmacologia
Granisetron/farmacologia
Injeções Espinhais
Ketanserina/farmacologia
Masculino
Limiar da Dor/efeitos dos fármacos
Pembutolol/farmacologia
Piperazinas/farmacologia
Piridinas/farmacologia
Ratos
Ratos Sprague-Dawley
Receptor 5-HT1B de Serotonina
Receptor 5-HT2A de Serotonina
Receptor 5-HT2C de Serotonina
Receptores de Serotonina/efeitos dos fármacos
Receptores 5-HT1 de Serotonina
Receptores 5-HT3 de Serotonina
Antagonistas da Serotonina/farmacologia
Fatores de Tempo
Vocalização Animal/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Analgesics); 0 (Ergolines); 0 (Piperazines); 0 (Pyridines); 0 (Receptor, Serotonin, 5-HT1B); 0 (Receptor, Serotonin, 5-HT2A); 0 (Receptor, Serotonin, 5-HT2C); 0 (Receptors, Serotonin); 0 (Receptors, Serotonin, 5-HT1); 0 (Receptors, Serotonin, 5-HT3); 0 (Serotonin Antagonists); 362O9ITL9D (Acetaminophen); 71IH826FEG (N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide); 78W62V43DY (Penbutolol); 97F9DE4CT4 (Ketanserin); SML95FK06I (mesulergine); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:0202
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:011206
[St] Status:MEDLINE


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[PMID]:11417867
[Au] Autor:Funato K; Imai T; Nakashima K; Otagiri M
[Ad] Endereço:Aventis Pharma Ltd., Kawagoe, Saitama, Japan.
[Ti] Título:High-performance liquid chromatography with chemiluminescence detection of penbutolol and its hydroxylated metabolite in rat plasma.
[So] Source:J Chromatogr B Biomed Sci Appl;757(2):229-35, 2001 Jun 15.
[Is] ISSN:1387-2273
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:This paper describes a new method of high-performance liquid chromatography with chemiluminescence detection for the analysis of penbutolol (PB) and its main metabolite, 4-hydroxy penbutolol (4-OH PB) in rat plasma. 4-Dimethylaminosulfonyl-7-(N-chloroformylmethyl-N-methyl) amino-2,1,3-benzoxadiazole (DBD-COCl) was used as a fluorogenic labeling reagent. A mixture of hydrogen peroxide and bis[4-nitro-2-(3,6,9-trioxadecyloxycarbonyl)phenyl]oxalate (TDPO) in acetonitrile was used as a post-column chemiluminogenic reagent. The derivatives of PB and 4-OH PB with DBD-COCI were separated by isocratic effluent with 0.01 M imidazole buffer (pH 7.0)-acetonitrile within 10 min. The detection limits of the proposed method for PB and 4-OH PB were 9.9 and 15 fmol on column, respectively. After intravenous administration of PB in rats, its plasma concentration profiles of PB and 4-OH PB were determined by the proposed method. PB was demonstrated to be rapidly metabolized to 4-OH PB at the same rate as cardiac output.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Pembutolol/sangue
[Mh] Termos MeSH secundário: Animais
Calibragem
Hidroxilação
Indicadores e Reagentes
Medições Luminescentes
Ratos
Reprodutibilidade dos Testes
Espectrometria de Fluorescência
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Indicators and Reagents); 78W62V43DY (Penbutolol)
[Em] Mês de entrada:0112
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:010622
[St] Status:MEDLINE


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[PMID]:10942852
[Au] Autor:Rabiner EA; Gunn RN; Castro ME; Sargent PA; Cowen PJ; Koepp MJ; Meyer JH; Bench CJ; Harrison PJ; Pazos A; Sharp T; Grasby PM
[Ad] Endereço:MRC Cyclotron Unit, Hammersmith Hospital, Imperial College School of Medicine, London, United Kingdom. ilan@cu.rpms.ac.uk
[Ti] Título:beta-blocker binding to human 5-HT(1A) receptors in vivo and in vitro: implications for antidepressant therapy.
[So] Source:Neuropsychopharmacology;23(3):285-93, 2000 Sep.
[Is] ISSN:0893-133X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A novel strategy for improving the treatment of depressive illness is augmentation of antidepressants with a 5-HT1(1A) autoreceptor antagonist. However, trials using the 5-HT1(1A)/beta-blocker pindolol are proving inconsistent. We report how positron emission tomography (PET) and in vitro autoradiography can inform trials of antidepressant augmentation. We show that in healthy volunteers, in vivo, pindolol (n = 10) and penbutolol (n = 4), but not tertatolol (n = 4) occupy the human 5-HT(1A) receptors, at clinical doses. Pindolol, as well as the beta-blockers penbutolol and tertatolol, has high affinity for human 5-HT(1A) receptors in post-mortem brain slices (n = 4). Pindolol shows preference for 5-HT(1A) autoreceptors versus the post-synaptic receptors both in vitro and in vivo. Our data reveal that pindolol doses used in antidepressant trials so far are suboptimal for significant occupancy at the 5-HT(1A) autoreceptor. Penbutolol or higher doses of pindolol are candidates for testing as antidepressant augmenting regimes in future clinical trials.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/metabolismo
Antidepressivos/metabolismo
Receptores de Serotonina/metabolismo
Tiofenos
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/farmacologia
Adulto
Idoso
Autorradiografia
Autorreceptores/metabolismo
Química Encefálica/efeitos dos fármacos
Feminino
Seres Humanos
Técnicas In Vitro
Masculino
Meia-Idade
Pembutolol/metabolismo
Pembutolol/farmacologia
Pindolol/metabolismo
Pindolol/farmacologia
Piperazinas/metabolismo
Propanolaminas/metabolismo
Propanolaminas/farmacologia
Piridinas/metabolismo
Receptores de Neurotransmissores/efeitos dos fármacos
Receptores de Neurotransmissores/metabolismo
Receptores 5-HT1 de Serotonina
Antagonistas da Serotonina/metabolismo
Tomografia Computadorizada de Emissão
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Antidepressive Agents); 0 (Autoreceptors); 0 (Piperazines); 0 (Propanolamines); 0 (Pyridines); 0 (Receptors, Neurotransmitter); 0 (Receptors, Serotonin); 0 (Receptors, Serotonin, 5-HT1); 0 (Serotonin Antagonists); 0 (Thiophenes); 71IH826FEG (N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide); 78W62V43DY (Penbutolol); 9ZO341YQXP (tertatolol); BJ4HF6IU1D (Pindolol)
[Em] Mês de entrada:0010
[Cu] Atualização por classe:150311
[Lr] Data última revisão:
150311
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:000816
[St] Status:MEDLINE


  7 / 176 MEDLINE  
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[PMID]:10899952
[Au] Autor:Castro ME; Harrison PJ; Pazos A; Sharp T
[Ad] Endereço:University Department of Clinical Pharmacology, Radcliffe Infirmary, Oxford, England.
[Ti] Título:Affinity of (+/-)-pindolol, (-)-penbutolol, and (-)-tertatolol for pre- and postsynaptic serotonin 5-HT(1A) receptors in human and rat brain.
[So] Source:J Neurochem;75(2):755-62, 2000 Aug.
[Is] ISSN:0022-3042
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:There is considerable interest in the use of drugs that selectively block presynaptic (somatodendritic) serotonin 5-HT(1A) receptors for the adjunctive treatment of major depressive disorder. The 5-HT(1A)/beta-adrenoceptor ligands (+/-)-pindolol, (-)-tertatolol, and (-)-penbutolol are currently under clinical investigation, and knowledge of their affinity at different populations of central 5-HT(1A) receptors is needed. Here we have determined the affinity of these drugs for presynaptic and postsynaptic 5-HT(1A) receptors in postmortem human and rat brain using receptor autoradiography and the selective 5-HT(1A) radioligand [(3)H]WAY-100635. The binding of [(3)H]WAY-100635 was specific and saturable and showed high affinity in the rat dorsal raphe nucleus and hippocampus (K(D) = 1.5-1.7 nM). In competition studies, the three compounds had nanomolar affinity and produced monophasic displacement of [(3)H]WAY-100635 binding in all regions of both species. (-)-Penbutolol and (-)-tertatolol had similar affinity for pre-and postsynaptic 5-HT(1A) receptors in both rat and human brain. However, in the human, but not the rat, the affinity of (+/-)-pindolol in dorsal raphe nucleus (K(i) = 8.9 +/- 1. 1 nM) was slightly but significantly higher than that in hippocampus (K(i) = 14.4 +/- 1.5 nM in CA1). In summary, our data show that (+/-)-pindolol, (-)-tertatolol, and (-)-penbutolol are all high-affinity ligands at native human and rat 5-HT(1A) receptors. (-)-Penbutolol and (-)-tertatolol do not discriminate between the pre- and postsynaptic 5-HT(1A) sites tested in either species, but (+/-)-pindolol showed a slightly higher affinity for the presynaptic site in human brain. Further work is needed to establish whether the latter difference is clinically relevant.
[Mh] Termos MeSH primário: Antiarrítmicos/farmacocinética
Encéfalo/metabolismo
Pembutolol/farmacocinética
Pindolol/farmacocinética
Propanolaminas/farmacocinética
Receptores Pré-Sinápticos/metabolismo
Receptores de Serotonina/metabolismo
Sinapses/metabolismo
Tiofenos
[Mh] Termos MeSH secundário: Idoso
Animais
Autorradiografia
Giro Denteado/metabolismo
Feminino
Hipocampo/metabolismo
Seres Humanos
Masculino
Piperazinas/farmacocinética
Piridinas/farmacocinética
Ensaio Radioligante
Núcleos da Rafe/metabolismo
Ratos
Ratos Sprague-Dawley
Receptores 5-HT1 de Serotonina
Antagonistas da Serotonina/farmacocinética
Trítio
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Arrhythmia Agents); 0 (Piperazines); 0 (Propanolamines); 0 (Pyridines); 0 (Receptors, Presynaptic); 0 (Receptors, Serotonin); 0 (Receptors, Serotonin, 5-HT1); 0 (Serotonin Antagonists); 0 (Thiophenes); 10028-17-8 (Tritium); 71IH826FEG (N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide); 78W62V43DY (Penbutolol); 9ZO341YQXP (tertatolol); BJ4HF6IU1D (Pindolol)
[Em] Mês de entrada:0008
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:000719
[St] Status:MEDLINE


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[PMID]:10415377
[Au] Autor:Hjorth S; Auerbach SB
[Ad] Endereço:Department of Pharmacology, University of Göteborg, Göteborg, Sweden.
[Ti] Título:Autoreceptors remain functional after prolonged treatment with a serotonin reuptake inhibitor.
[So] Source:Brain Res;835(2):224-8, 1999 Jul 24.
[Is] ISSN:0006-8993
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Serotonin (5-hydroxytryptamine, 5-HT) autoreceptors may desensitize during prolonged administration of antidepressant drugs. If autoreceptors desensitize, their inhibitory influence on extracellular 5-HT should be attenuated. To test this hypothesis, the selective serotonin reuptake inhibitor (SSRI) citalopram (10 mg kg(-1), s.c., b.i.d.) or saline was administered for 14 days to rats. After a 24-h washout period, rats were anesthetized, and implanted with dialysis probes for determination of 5-HT in the frontal cortex (FCx) and dorsal hippocampus (DH). In response to citalopram (5 mg kg(-1), s.c.) challenge, there were moderate increases in 5-HT in the FCx and DH of both the chronic citalopram and saline pretreatment groups. After subsequent administration of the 5-HT(1A/1B) autoreceptor antagonist, (-)-penbutolol, there were further increases in 5-HT in the FCx and DH of the saline pretreatment group. Moreover, contrary to the expected effect if autoreceptors were desensitized, the potentiation produced by (-)-penbutolol was greater in the FCx and DH of the chronic citalopram group as compared to rats pretreated with saline. These results suggest that autoreceptors still restrain the increase in 5-HT produced by an SSRI after prolonged administration.
[Mh] Termos MeSH primário: Autorreceptores/efeitos dos fármacos
Citalopram/farmacologia
Inibidores da Captação de Serotonina/farmacologia
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/farmacologia
Animais
Masculino
Microdiálise
Pembutolol/farmacologia
Ratos
Ratos Sprague-Dawley
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Autoreceptors); 0 (Serotonin Uptake Inhibitors); 0DHU5B8D6V (Citalopram); 78W62V43DY (Penbutolol)
[Em] Mês de entrada:9909
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:990723
[St] Status:MEDLINE


  9 / 176 MEDLINE  
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[PMID]:10369467
[Au] Autor:Gartside SE; Clifford EM; Cowen PJ; Sharp T
[Ad] Endereço:Oxford University Department of Clinical Pharmacology, Radcliffe Infirmary.
[Ti] Título:Effects of (-)-tertatolol, (-)-penbutolol and (+/-)-pindolol in combination with paroxetine on presynaptic 5-HT function: an in vivo microdialysis and electrophysiological study.
[So] Source:Br J Pharmacol;127(1):145-52, 1999 May.
[Is] ISSN:0007-1188
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The antidepressant efficacy of selective serotonin reuptake inhibitors (SSRIs) might be enhanced by co-administration of 5-HT1A receptor antagonists. Thus, we have recently shown that the selective 5-HT1A receptor antagonist, WAY 100635, blocks the inhibitory effect of an SSRI on 5-HT cell firing, and enhances its ability to elevate extracellular 5-HT in the forebrain. Here we determined whether the beta-adrenoceptor/5-HT1A receptor ligands (+/-)-pindolol, (-)-tertatolol and (-)-penbutolol, interact with paroxetine in a similar manner. Both (-)-tertatolol (2.4 mg kg(-1) i.v.) and (-)-penbutolol (2.4 mg kg(-1) i.v.) enhanced the effect of paroxetine (0.8 mg kg(-1) i.v.) on extracellular 5-HT in the frontal cortex, whilst (+/-)-pindolol (4 mg kg(-1) i.v.) did not. (-)-Tertatolol (2.4 mg kg(-1) i.v.) alone caused a slight increase in 5-HT however, (-)-penbutolol (2.4 mg kg(-1) i.v.) alone had no effect. In electrophysiological studies (-)-tertatolol (2.4 mg kg(-1) i.v.) alone had no effect on 5-HT cell firing but blocked the inhibitory effect of paroxetine. In contrast, (-)-penbutolol (0.1-0.8 mg kg(-1) i.v.) itself inhibited 5-HT cell firing, and this effect was reversed by WAY 100635 (0.1 mg kg(-1) i.v.). We have recently shown that (+/-)-pindolol inhibits 5-HT cell firing via a WAY 100635-sensitive mechanism. Our data suggest that (-)-tertatolol enhances the effect of paroxetine on forebrain 5-HT via blockade of 5-HT1A autoreceptors which mediate paroxetine-induced inhibition of 5-HT cell firing. In comparison, the mechanisms by which (-)-penbutolol enhances the effect of paroxetine on extracellular 5-HT is unclear, since (-)-penbutolol itself appears to have agonist properties at the 5-HT1A autoreceptor. Indeed, the agonist action of (+/-)-pindolol at 5-HT1A autoreceptors probably explains its inability to enhance the effect of paroxetine on 5-HT in the frontal cortex. Overall, our data suggest that both (-)-tertatolol and (-)-penbutolol are superior to (+/-)-pindolol in terms of enhancing the effect of an SSRI on extracellular 5-HT. Both (-)-tertatolol and (-)-penbutolol are worthy of investigation for use as adjuncts to SSRIs in the treatment of major depression.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/farmacologia
Antidepressivos/farmacologia
Receptores Pré-Sinápticos/fisiologia
Receptores de Serotonina/fisiologia
Inibidores da Captação de Serotonina/farmacologia
Serotonina/fisiologia
Tiofenos
[Mh] Termos MeSH secundário: Animais
Sinergismo Farmacológico
Eletrofisiologia
Técnicas In Vitro
Masculino
Potenciais da Membrana
Microdiálise
Paroxetina/farmacologia
Técnicas de Patch-Clamp
Pembutolol/farmacologia
Pindolol/farmacologia
Propanolaminas/farmacologia
Prosencéfalo/efeitos dos fármacos
Prosencéfalo/metabolismo
Núcleos da Rafe/efeitos dos fármacos
Núcleos da Rafe/metabolismo
Ratos
Ratos Sprague-Dawley
Receptores Pré-Sinápticos/efeitos dos fármacos
Receptores de Serotonina/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Antidepressive Agents); 0 (Propanolamines); 0 (Receptors, Presynaptic); 0 (Receptors, Serotonin); 0 (Serotonin Uptake Inhibitors); 0 (Thiophenes); 333DO1RDJY (Serotonin); 41VRH5220H (Paroxetine); 78W62V43DY (Penbutolol); 9ZO341YQXP (tertatolol); BJ4HF6IU1D (Pindolol)
[Em] Mês de entrada:9909
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:990616
[St] Status:MEDLINE


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Fotocópia
[PMID]:10067289
[Au] Autor:Korovina EP
[Ti] Título:[Beta-adrenergic blockers and calcium antagonists in hypertrophic cardiomyopathy].
[Ti] Título:Beta-adrenoblokatory i antagonisti kal'tsiia pri gipertroficheskoi kardiomiopatii..
[So] Source:Klin Med (Mosk);76(12):30-5, 1998.
[Is] ISSN:0023-2149
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:Effects of beta-blockers (propranolol, penbutolol) and calcium antagonists (nifedipine, verapamil, diltiazem) were studied in 73 patients with hypertrophic cardiomyopathy (HC). Clinical data, ECG and echo-CG findings were assessed. It was found that beta-adrenoblockers and calcium antagonists improve quality of life in one-third of the patients. Penbutolol and nifedipine did so in half of the patients. Neither beta-adrenoblockers nor calcium antagonists decrease myocardial hypertrophy. Calcium antagonists may result in lowering of myocardial contractility while beta-adrenoblockers may increase the ejection fraction. Diltiazem produced a positive effect on diastolic function but had many side effects. Nifedipine increased lethality compared with verapamil and propranolol.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/uso terapêutico
Bloqueadores dos Canais de Cálcio/uso terapêutico
Cardiomiopatia Hipertrófica/tratamento farmacológico
[Mh] Termos MeSH secundário: Adolescente
Antagonistas Adrenérgicos beta/administração & dosagem
Antagonistas Adrenérgicos beta/farmacologia
Adulto
Idoso
Bloqueadores dos Canais de Cálcio/administração & dosagem
Bloqueadores dos Canais de Cálcio/farmacologia
Cardiomiopatia Hipertrófica/fisiopatologia
Diltiazem/administração & dosagem
Diltiazem/farmacologia
Diltiazem/uso terapêutico
Feminino
Hemodinâmica/efeitos dos fármacos
Seres Humanos
Masculino
Meia-Idade
Nifedipino/administração & dosagem
Nifedipino/farmacologia
Nifedipino/uso terapêutico
Pembutolol/administração & dosagem
Pembutolol/farmacologia
Pembutolol/uso terapêutico
Propranolol/administração & dosagem
Propranolol/farmacologia
Propranolol/uso terapêutico
Fatores de Tempo
Verapamil/administração & dosagem
Verapamil/farmacologia
Verapamil/uso terapêutico
[Pt] Tipo de publicação:CLINICAL TRIAL; COMPARATIVE STUDY; ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Calcium Channel Blockers); 78W62V43DY (Penbutolol); 9Y8NXQ24VQ (Propranolol); CJ0O37KU29 (Verapamil); EE92BBP03H (Diltiazem); I9ZF7L6G2L (Nifedipine)
[Em] Mês de entrada:9903
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:990306
[St] Status:MEDLINE



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