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Pesquisa : D02.033.100.624.698 [Categoria DeCS]
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[PMID]:28436624
[Au] Autor:Zhang L; Chen G; Chen J; He X; Hu X
[Ad] Endereço:Department of Neurology, Sir Run Run Shaw Hospital, Zhejiang University School of Medicine, Hangzhou 310016, China.
[Ti] Título:[Mechanisms of histamine ameliorating memory impairment induced by pentylenetetrazole-kindling epilepsy in rats].
[So] Source:Zhejiang Da Xue Xue Bao Yi Xue Ban;46(1):1-6, 2017 Jan 25.
[Is] ISSN:1008-9292
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:To investigate the effects of neuronal histamine on spatial memory acquisition impairment in rats with pentylenetetrazole-kindling epilepsy, and to explore its mechanisms. A subconvulsive dose of pentylenetetrazole (35 mg/kg) was intraperitoneally injected in rats every 48 h to induce chemical kindling until fully kindled. Morris water maze was used to measure the spatial memory acquisition of the rats one week after fully pentylenetetrazole-kindled, and the histamine contents in different brain areas were measured spectrofluorometrically. Different dosages of hitidine (the precursor of histamine), pyrilamine (H1 receptor antagonist), and zolantidine (H2 receptor antagonist) were intraperitoneally injected, and their effects on spatial memory acquisition of the rats were observed. Compared with control group, escape latencies were significantly prolonged on Morris water maze training day 2 and day 3 in pentylenetetrazole-kindling epilepsy rats (all <0.05); and the histamine contents in hippocampus, thalamus and hypothalamus were decreased significantly (all <0.05). Escape latencies were markedly shortened on day 3 by intraperitoneally injected with histidine 500 mg/kg, and on day 2 and day 3 by intraperitoneally injected with histidine 1000 mg/kg in pentylenetetrazole-kindling epilepsy rats (all <0.05). The protection of histidine was reversed by zolantidine (10 and 20 mg/kg), but not by pyrilamine. Neuronal histamine can improve the spatial memory acquisition impairment in rats with pentylenetetrazole-kindling epilepsy, and the activation of H2 receptors is possibly involved in the protective effects of histamine.
[Mh] Termos MeSH primário: Transtornos da Memória/tratamento farmacológico
Receptores Histamínicos H2/efeitos dos fármacos
Receptores Histamínicos H2/fisiologia
Memória Espacial/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Benzotiazóis/farmacologia
Química Encefálica/efeitos dos fármacos
Epilepsia/induzido quimicamente
Epilepsia/complicações
Hipocampo/química
Antagonistas dos Receptores Histamínicos H1/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Histidina/farmacologia
Hipotálamo/química
Excitação Neurológica/fisiologia
Transtornos da Memória/etiologia
Pentilenotetrazol
Fenoxipropanolaminas/farmacologia
Piperidinas/farmacologia
Pirilamina/farmacologia
Ratos
Ratos Sprague-Dawley
Espectrometria de Fluorescência
Tálamo/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (Histamine H1 Antagonists); 0 (Histamine H2 Antagonists); 0 (Phenoxypropanolamines); 0 (Piperidines); 0 (Receptors, Histamine H2); 4QD397987E (Histidine); HPE317O9TL (Pyrilamine); M1108XAY01 (zolantidine); WM5Z385K7T (Pentylenetetrazole)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170425
[St] Status:MEDLINE


  2 / 134 MEDLINE  
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[PMID]:26956388
[Au] Autor:Svan A; Hedeland M; Arvidsson T; Jasper JT; Sedlak DL; Pettersson CE
[Ad] Endereço:Division of Analytical Pharmaceutical Chemistry, Uppsala University, BMC Box 574, SE-751 23, Uppsala, Sweden.
[Ti] Título:Identification of transformation products from ß-blocking agents formed in wetland microcosms using LC-Q-ToF.
[So] Source:J Mass Spectrom;51(3):207-18, 2016 Mar.
[Is] ISSN:1096-9888
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Identification of degradation products from trace organic compounds, which may retain the biological activity of the parent compound, is an important step in understanding the long-term effects of these compounds on the environment. Constructed wetlands have been successfully utilized to remove contaminants from wastewater effluent, including pharmacologically active compounds. However, relatively little is known about the transformation products formed during wetland treatment. In this study, three different wetland microcosm treatments were used to determine the biotransformation products of the ß-adrenoreceptor antagonists atenolol, metoprolol and propranolol. LC/ESI-Q-ToF run in the MS(E) and MS/MS modes was used to identify and characterize the degradation products through the accurate masses of precursor and product ions. The results were compared with those of a reference standard when available. Several compounds not previously described as biotransformation products produced in wetlands were identified, including propranolol-O-sulfate, 1-naphthol and the human metabolite N-deaminated metoprolol. Transformation pathways were significantly affected by microcosm conditions and differed between compounds, despite the compounds' structural similarities. Altogether, a diverse range of transformation products in wetland microcosms were identified and elucidated using high resolving MS. This work shows that transformation products are not always easily predicted, nor formed via the same pathways even for structurally similar compounds.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/análise
Microbiologia Ambiental
Microbiota/fisiologia
Fenoxipropanolaminas/análise
Zonas Úmidas
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/química
Antagonistas Adrenérgicos beta/metabolismo
Cromatografia Líquida/métodos
Espectrometria de Massas/métodos
Fenoxipropanolaminas/química
Fenoxipropanolaminas/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Phenoxypropanolamines)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160310
[St] Status:MEDLINE
[do] DOI:10.1002/jms.3737


  3 / 134 MEDLINE  
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[PMID]:26821612
[Au] Autor:Ghosh S; Bhaumik J; Banoth L; Banesh S; Banerjee UC
[Ad] Endereço:Department of Pharmaceutical Technology, National Institute of Pharmaceutical Education and Research, Nagar, Punjab, India.
[Ti] Título:Chemoenzymatic Route for the Synthesis of (S)-Moprolol, a Potential ß-Blocker.
[So] Source:Chirality;28(4):313-8, 2016 Apr.
[Is] ISSN:1520-636X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A biocatalytic route for the synthesis of a potential ß-blocker, (S)-moprolol is reported here. Enantiopure synthesis of moprolol is mainly dependent on the chiral intermediate, 3-(2-methoxyphenoxy)-propane-1,2-diol. Various commercial lipases were screened for the enantioselective resolution of (RS)-3-(2-methoxyphenoxy)propane-1,2-diol to produce the desired enantiomer. Among them, Aspergillus niger lipase (ANL) was selected on the basis of both stereo- and regioselectivity. The optimized values of various reaction parameters were determined such as enzyme (15 mg/mL), substrate concentration (10 mM), organic solvent (toluene), reaction temperature (30 °C), and time (18 h).The optimized conditions led to achieving >49% yield with high enantiomeric excess of (S)-3-(2-methoxyphenoxy)propane-1,2-diol. The lipase-mediated catalysis showed regioselective acylation with dual stereoselectivity. Further, the enantiopure intermediate was used for the synthesis of (S)-moprolol, which afforded the desired ß-blocker.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/química
Lipase/química
Fenoxipropanolaminas/síntese química
[Mh] Termos MeSH secundário: Acilação
Antagonistas Adrenérgicos beta/metabolismo
Biocatálise
Catálise
Lipase/metabolismo
Propanóis/química
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (3-(2-methoxyphenoxy)propane-1,2-diol); 0 (Adrenergic beta-Antagonists); 0 (Phenoxypropanolamines); 0 (Propanols); A94HCH4225 (moprolol); EC 3.1.1.3 (Lipase)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:160313
[Lr] Data última revisão:
160313
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160130
[St] Status:MEDLINE
[do] DOI:10.1002/chir.22574


  4 / 134 MEDLINE  
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[PMID]:26525191
[Au] Autor:Sadek B; Saad A; Subramanian D; Shafiullah M; Lazewska D; Kiec-Kononowiczc K
[Ad] Endereço:Department of Pharmacology & Therapeutics, College of Medicine & Health Sciences, United Arab Emirates University, Al Ain, United Arab Emirates. Electronic address: bassem.sadek@uaeu.ac.ae.
[Ti] Título:Anticonvulsant and procognitive properties of the non-imidazole histamine H3 receptor antagonist DL77 in male adult rats.
[So] Source:Neuropharmacology;106:46-55, 2016 Jul.
[Is] ISSN:1873-7064
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:It has become clear that histamine H3 receptors (H3Rs) are implicated in modulating epilepsy and memory in laboratory animals. The new non-imidazole H3R antagonist DL77 has excellent selectivity profile and shows high in-vivo potency as well as in-vitro antagonist affinity with ED50 values of 2.1 ± 0.2 mg/kg and 8.4 ± 1.3 [nM], respectively. In the present study, the anticonvulsant effects of DL77 on maximal electroshock (MES)-, pentylenetetrazole (PTZ)-, and strychnine (STR)-induced seizure models were investigated. Moreover, the procognitive properties of DL77 were tested on acquisition, consolidation and retrieval processes in a one-trial inhibitory avoidance task in male Wistar rats. The results indicate that DL77 (5, 10, and 15 mg/kg, i.p.) significantly and dose-dependently reduced MES-induced seizure duration, whereas no protection was observed in PTZ- or STR-induced seizures. Importantly, the protective action observed for DL77 in MES-induced seizure was comparable to that of the reference antiepileptic drug (AED) phenytoin (PHT), and was also reversed when rats were pretreated with the CNS penetrant pyrilamine (PYR) (10 mg/kg, i.p.), or with the selective H3R agonist R-(α)-methyl-histamine (RAMH) (10 mg/kg, i.p.). Furthermore, the procognitive studies indicate that acute pre-training systemic administration of DL77 (2.5 mg/kg, i.p.) facilitated acquisition, whereas pre-testing acute administration of DL77 (5 and 10 mg/kg, i.p.) improved retrieval. Interestingly, the procognitive effect of DL77 on retrieval was completely abrogated when rats were pretreated with the centrally-acting H2R antagonist zolantidine (ZOL) but not the centrally acting H1R antagonist PYR, indicating that histaminergic pathways through activation of H2Rs appear to be participating in neuronal circuits involved in retrieval processes. Taken together, our results show that DL77 demonstrates anticonvulsant properties in the MES-induced seizure model and improves cognitive performance through actions on different memory stages. Therefore, H3Rs may have implications for the treatment of degenerative disorders associated with impaired memory function and may represent a novel therapeutic pharmacological target to tackle cognitive problems associated with the chronic use of antiepileptic drugs. This article is part of the Special Issue entitled 'Histamine Receptors'.
[Mh] Termos MeSH primário: Anticonvulsivantes/farmacologia
Antagonistas dos Receptores Histamínicos H3/farmacologia
Nootrópicos/farmacologia
Éteres Fenílicos/farmacologia
Piperidinas/farmacologia
[Mh] Termos MeSH secundário: Animais
Aprendizagem da Esquiva/efeitos dos fármacos
Aprendizagem da Esquiva/fisiologia
Benzotiazóis/farmacologia
Modelos Animais de Doenças
Relação Dose-Resposta a Droga
Avaliação Pré-Clínica de Medicamentos
Epilepsia/tratamento farmacológico
Epilepsia/psicologia
Agonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Masculino
Memória/efeitos dos fármacos
Memória/fisiologia
Metilistaminas/farmacologia
Fenoxipropanolaminas/farmacologia
Fenitoína/farmacologia
Distribuição Aleatória
Ratos Wistar
Receptores Histamínicos H3/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1-(3-(4-tert-pentylphenoxy)propyl)piperidine); 0 (Anticonvulsants); 0 (Benzothiazoles); 0 (Histamine Agonists); 0 (Histamine H2 Antagonists); 0 (Histamine H3 Antagonists); 0 (Methylhistamines); 0 (Nootropic Agents); 0 (Phenoxypropanolamines); 0 (Phenyl Ethers); 0 (Piperidines); 0 (Receptors, Histamine H3); 6158TKW0C5 (Phenytoin); 6986-90-9 (alpha-methylhistamine); M1108XAY01 (zolantidine)
[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:151104
[St] Status:MEDLINE


  5 / 134 MEDLINE  
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[PMID]:26467607
[Au] Autor:Khan N; Saad A; Nurulain SM; Darras FH; Decker M; Sadek B
[Ad] Endereço:Department of Pharmacology and Therapeutics, College of Medicine & Health Sciences, P.O. Box 17666, Al Ain 0097, United Arab Emirates University, United Arab Emirates.
[Ti] Título:The dual-acting H3 receptor antagonist and AChE inhibitor UW-MD-71 dose-dependently enhances memory retrieval and reverses dizocilpine-induced memory impairment in rats.
[So] Source:Behav Brain Res;297:155-64, 2016 Jan 15.
[Is] ISSN:1872-7549
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Both the histamine H3 receptor (H3R) and acetylcholine esterase (AChE) are involved in the regulation of release and metabolism of acetylcholine and several other central neurotransmitters. Therefore, dual-active H3R antagonists and AChE inhibitors (AChEIs) have shown in several studies to hold promise to treat cognitive disorders like Alzheimer's disease (AD). The novel dual-acting H3R antagonist and AChEI 7-(3-(piperidin-1-yl)propoxy)-1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline (UW-MD-71) with excellent selectivity profiles over both the three other HRs as well as the AChE's isoenzyme butyrylcholinesterase (BChE) shows high and balanced in vitro affinities at both H3R and AChE with IC50 of 33.9nM and hH3R antagonism with Ki of 76.2nM, respectively. In the present study, the effects of UW-MD-71 (1.25-5mg/kg, i.p.) on acquisition, consolidation, and retrieval in a one-trial inhibitory avoidance task in male rats were investigated applying donepezil (DOZ) and pitolisant (PIT) as reference drugs. Furthermore, the effects of UW-MD-71 on memory deficits induced by the non-competitive N-methyl-d-aspartate (NMDA) antagonist dizocilpine (DIZ) were tested. Our results indicate that administration of UW-MD-71 before the test session dose-dependently increased performance and enhanced procognitive effect on retrieval. However neither pre- nor post-training acute systemic administration of UW-MD-71 facilitated acquisition or consolidation. More importantly, UW-MD-71 (2.5mg/kg, i.p.) ameliorated the DIZ-induced amnesic effects. Furthermore, the procognitive activity of UW-MD-71 in retrieval was completely reversed and partly abrogated in DIZ-induced amnesia when rats were pretreated with the centrally-acting H2R antagonist zolantidine (ZOL), but not with the CNS penetrant H1R antagonist pyrilamine (PYR). These results demonstrate the procognitive effects of UW-MD-71 in two in vivo memory models, and are to our knowledge the first demonstration in vivo that a potent dual-acting H3R antagonist and AChEI is effective in improving retrieval processes in the one-trial inhibitory avoidance task and provide evidence to such compounds to treat cognitive disorders.
[Mh] Termos MeSH primário: Inibidores da Colinesterase/farmacologia
Antagonistas dos Receptores Histamínicos H3/farmacologia
Transtornos da Memória/tratamento farmacológico
Memória/efeitos dos fármacos
Nootrópicos/farmacologia
Pirróis/farmacologia
Quinazolinas/farmacologia
[Mh] Termos MeSH secundário: Animais
Aprendizagem da Esquiva/efeitos dos fármacos
Aprendizagem da Esquiva/fisiologia
Benzotiazóis/farmacologia
Modelos Animais de Doenças
Maleato de Dizocilpina
Relação Dose-Resposta a Droga
Avaliação Pré-Clínica de Medicamentos
Indanos/farmacologia
Masculino
Memória/fisiologia
Transtornos da Memória/metabolismo
Fenoxipropanolaminas/farmacologia
Piperidinas/farmacologia
Pirilamina/farmacologia
Distribuição Aleatória
Ratos Wistar
Receptores Histamínicos H3/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (7-(3-(piperidin-1-yl)propoxy)-1,2,3,9-tetrahydropyrrolo(2,1-b)quinazoline); 0 (Benzothiazoles); 0 (Cholinesterase Inhibitors); 0 (Histamine H3 Antagonists); 0 (Indans); 0 (Nootropic Agents); 0 (Phenoxypropanolamines); 0 (Piperidines); 0 (Pyrroles); 0 (Quinazolines); 0 (Receptors, Histamine H3); 4BC83L4PIY (1-(3-(3-(4-chlorophenyl)propoxy)propyl)piperidine); 6LR8C1B66Q (Dizocilpine Maleate); 8SSC91326P (donepezil); HPE317O9TL (Pyrilamine); M1108XAY01 (zolantidine)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151016
[St] Status:MEDLINE


  6 / 134 MEDLINE  
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[PMID]:26324053
[Au] Autor:Nobuta T; Xiao G; Ghislieri D; Gilmore K; Seeberger PH
[Ad] Endereço:Max Planck Institute of Colloids and Interfaces, Am Mühlenberg 1, 14476 Potsdam, Germany. kerry.gilmore@mpikg.mpg.de peter.seeberger@mpikg.mpg.de.
[Ti] Título:Continuous and convergent access to vicinyl amino alcohols.
[So] Source:Chem Commun (Camb);51(82):15133-6, 2015 Oct 21.
[Is] ISSN:1364-548X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Five active pharmaceutical ingredients (APIs) containing the vicinyl amino alcohol moiety were synthesized using a convergent chemical assembly system. The continuous system is composed of four flow reaction modules: biphasic oxidation, Corey-Chaykovsky epoxidation, phenol alkylation, and epoxide aminolysis. Judicious choice of reagents and module order allowed for two classes of ß-amino alcohols, aryl and aryloxy, to be synthesized in good (27-69%) overall yields.
[Mh] Termos MeSH primário: Fenoxipropanolaminas/síntese química
[Mh] Termos MeSH secundário: Antiarrítmicos/síntese química
Anti-Hipertensivos/síntese química
Broncodilatadores/síntese química
Técnicas de Química Sintética
Epicloroidrina/química
Compostos de Epóxi/síntese química
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Arrhythmia Agents); 0 (Antihypertensive Agents); 0 (Bronchodilator Agents); 0 (Epoxy Compounds); 0 (Phenoxypropanolamines); 08OOR508C0 (Epichlorohydrin)
[Em] Mês de entrada:1607
[Cu] Atualização por classe:151002
[Lr] Data última revisão:
151002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150902
[St] Status:MEDLINE
[do] DOI:10.1039/c5cc06093a


  7 / 134 MEDLINE  
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[PMID]:25315344
[Au] Autor:Sun S; Fan Z; Hu L; Ma Y; Si L; Qiu J; Li G
[Ad] Endereço:School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, People's Republic of China; Department of Biotechnology and Pharmaceutical Engineering, Wuhan Polytechnic University, Wuhan, People's Republic of China.
[Ti] Título:Influence of dose and route of administration on the enantioselective pharmacokinetics of TJ0711 hydrochloride in rats.
[So] Source:Chirality;27(1):53-7, 2015 Jan.
[Is] ISSN:1520-636X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The enantioselective pharmacokinetics of TJ0711 hydrochloride were studied in rats given different doses of rac-TJ0711 hydrochloride via intravenous and oral routes. R- and S-TJ0711 hydrochloride were both rapidly absorbed, and the average AUC0-∞ of R-TJ0711 hydrochloride was greater than that of S-TJ0711 hydrochloride after intragastric administration, with an R/S AUC ratio 1.11 and 1.35 for 30 and 50 mg/kg dose group, respectively. In contrast, the average AUC0-∞ of R-TJ0711 hydrochloride was smaller than that of S-TJ0711 hydrochloride after intravenous injection, with an R/S AUC ratio 0.57 and 0.73 for 10 and 20 mg/kg dose group, respectively. R-TJ0711 hydrochloride plasma half-lives were shorter than those of S-TJ0711 hydrochloride for all groups. AUC0-4h and Cmax between the two enantiomers were significantly different after oral administration of 50 mg/kg dose of the racemate, while no significant differences between the two enantiomers were found for all the pharmacokinetic parameters of the 30 mg/kg dose group. Significant differences between the two enantiomers were detected for nearly all the pharmacokinetic parameters after intravenous administration, except for the VZ of 20 mg/kg dose group. This study suggests that dose and route of administration will influence the enantioselectivity in the pharmacokinetics of TJ0711 hydrochloride in rats.
[Mh] Termos MeSH primário: Fenoxipropanolaminas/administração & dosagem
Fenoxipropanolaminas/farmacocinética
[Mh] Termos MeSH secundário: Administração Intravenosa
Administração Oral
Animais
Relação Dose-Resposta a Droga
Masculino
Estrutura Molecular
Fenoxipropanolaminas/sangue
Ratos
Ratos Sprague-Dawley
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (1-(4-(2-methoxyethyl)phenoxy)-3-(((2-2-methoxyphenoxy)ethyl)amino)-2-propanol); 0 (Phenoxypropanolamines)
[Em] Mês de entrada:1508
[Cu] Atualização por classe:141224
[Lr] Data última revisão:
141224
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141016
[St] Status:MEDLINE
[do] DOI:10.1002/chir.22387


  8 / 134 MEDLINE  
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[PMID]:25304183
[Au] Autor:Wei H; Jin CY; Viisanen H; You HJ; Pertovaara A
[Ad] Endereço:Institute of Biomedicine/Physiology, University of Helsinki, 00014 Helsinki, Finland.
[Ti] Título:Histamine in the locus coeruleus promotes descending noradrenergic inhibition of neuropathic hypersensitivity.
[So] Source:Pharmacol Res;90:58-66, 2014 Dec.
[Is] ISSN:1096-1186
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Among brain structures receiving efferent projections from the histaminergic tuberomammillary nucleus is the pontine locus coeruleus (LC) involved in descending noradrenergic control of pain. Here we studied whether histamine in the LC is involved in descending regulation of neuropathic hypersensitivity. Peripheral neuropathy was induced by unilateral spinal nerve ligation in the rat with a chronic intracerebral and intrathecal catheter for drug administrations. Mechanical hypersensitivity in the injured limb was assessed by monofilaments. Heat nociception was assessed by determining radiant heat-induced paw flick. Histamine in the LC produced a dose-related (1-10µg) mechanical antihypersensitivity effect (maximum effect at 15min and duration of effect 30min), without influence on heat nociception. Pretreatment of LC with zolantidine (histamine H2 receptor antagonist), but not with pyrilamine (histamine H1 receptor antagonist), and spinal administration of atipamezole (an α2-adrenoceptor antagonist), prazosine (an α1-adrenoceptor antagonist) or bicuculline (a GABAA receptor antagonist) attenuated the antihypersensitivity effect of histamine. The histamine-induced antihypersensitivity effect was also reduced by pretreatment of LC with fadolmidine, an α2-adrenoceptor agonist inducing autoinhibition of noradrenergic cell bodies. Zolantidine or pyrilamine alone in the LC failed to influence pain behavior, while A-960656 (histamine H3 receptor antagonist) suppressed hypersensitivity. A plausible explanation for these findings is that histamine, due to excitatory action mediated by the histamine H2 receptor on noradrenergic cell bodies, promotes descending spinal α1/2-adrenoceptor-mediated inhibition of neuropathic hypersensitivity. Blocking the autoinhibitory histamine H3 receptor on histaminergic nerve terminals in the LC facilitates release of histamine and thereby, increases descending noradrenergic pain inhibition.
[Mh] Termos MeSH primário: Histamina/fisiologia
Hiperalgesia/fisiopatologia
Locus Cerúleo/fisiologia
Neuralgia/fisiopatologia
[Mh] Termos MeSH secundário: Neurônios Adrenérgicos/fisiologia
Antagonistas de Receptores Adrenérgicos alfa 1/farmacologia
Agonistas de Receptores Adrenérgicos alfa 2/farmacologia
Animais
Benzotiazóis/farmacologia
Bicuculina/farmacologia
Antagonistas de Receptores de GABA-A/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Temperatura Alta
Imidazóis/farmacologia
Indanos/farmacologia
Masculino
Fenoxipropanolaminas/farmacologia
Estimulação Física
Piperidinas/farmacologia
Prazosina/farmacologia
Ratos
Receptores Adrenérgicos alfa 1/fisiologia
Receptores Adrenérgicos alfa 2/fisiologia
Receptores Histamínicos/fisiologia
Nervos Espinhais/lesões
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic alpha-1 Receptor Antagonists); 0 (Adrenergic alpha-2 Receptor Agonists); 0 (Benzothiazoles); 0 (GABA-A Receptor Antagonists); 0 (Histamine H2 Antagonists); 0 (Imidazoles); 0 (Indans); 0 (Phenoxypropanolamines); 0 (Piperidines); 0 (Receptors, Adrenergic, alpha-1); 0 (Receptors, Adrenergic, alpha-2); 0 (Receptors, Histamine); 820484N8I3 (Histamine); M1108XAY01 (zolantidine); WLN5FGH1CY (radolmidine); XM03YJ541D (Prazosin); Y37615DVKC (Bicuculline)
[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:141012
[St] Status:MEDLINE


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[PMID]:24961117
[Au] Autor:Zhang XJ; Qiu J; Li G
[Ti] Título:[Antiarrhythmic effect of TJ0711].
[So] Source:Yao Xue Xue Bao;49(3):419-26, 2014 Mar.
[Is] ISSN:0513-4870
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:To study the antiarrhythmic effect of the newly developed alpha/beta-blocker TJ0711, a variety of animal models of arrhythmia were induced by CaCl2, ouabain and ischemia/reperfusion. Glass microelectrode technique was used to observe action potentials of right ventricular papillary muscle of guinea pig. The onset time of arrhythmia induced by CaCl2 was significantly prolonged by TJ0711 at 0.75, 1.5 and 3 mg x kg(-1) doses. TJ0711 (1.5 and 3 mg x kg(-1)) can significantly shorten the ventricular tachycardia (VT) and ventricular fibrillation (VF) duration, the incidence of VF and mortality were significantly reduced. On ischemia-reperfusion-induced arrhythmic model, TJ0711 (0.25, 0.5, 1 and 2 mg x kg(-1)) can significantly reduce the ventricular premature contraction (PVC), VT, VF incidence, mortality, arrhythmia score with a dose-dependent manner. At the same time, rats serum lactate dehydrogenase (LDH) and creatine kinase (CK) activities decreased significantly by TJ0711 (1 and 2 mg x kg(-1)). Ouabain could cause arrhythmia in guinea pigs, when TJ0711 (0.375, 0.75, 1.5 and 3 mg x kg(-1)) was given, the doses of ouabain inducing a variety of arrhythmia PVC, VT, VF, cardiac arrest (CA) were significantly increased with a dose-dependent manner. In the TJ0711 0.1-30 micromol x L(-1) concentration range, guinea pig right ventricular papillary muscle action potential RP (rest potential), APA (action potential amplitude) and V(max) (maximum velocity of depolarization) were not significantly affected. APD20, APD50 and APD90 had a shortening trend but no statistical difference with the increase of TJ0711 concentration. TJ0711 has antiarrhythmic effect on the sympathetic nerve excitement and myocardial cell high calcium animal arrhythmia model. Myocardial action potential zero phase conduction velocity and resting membrane potential were not inhibited by TJ0711. APD20, APD50 and APD90 were shortened by TJ0711 at high concentration. Its antiarrhythmic action mechanism may be besides the action of blocking beta1 receptor, may also have a strong selective blocking action on alpha1 receptor and reducing intracellular calcium concentration.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos alfa/farmacologia
Antagonistas Adrenérgicos beta/farmacologia
Antiarrítmicos/farmacologia
Arritmias Cardíacas
Fenoxipropanolaminas/farmacologia
[Mh] Termos MeSH secundário: Potenciais de Ação/efeitos dos fármacos
Antagonistas Adrenérgicos alfa/administração & dosagem
Antagonistas Adrenérgicos beta/administração & dosagem
Animais
Antiarrítmicos/administração & dosagem
Arritmias Cardíacas/sangue
Arritmias Cardíacas/induzido quimicamente
Arritmias Cardíacas/etiologia
Arritmias Cardíacas/patologia
Arritmias Cardíacas/fisiopatologia
Cloreto de Cálcio
Creatina Quinase/sangue
Relação Dose-Resposta a Droga
Feminino
Cobaias
Ventrículos do Coração/citologia
Lactato Desidrogenases/sangue
Masculino
Traumatismo por Reperfusão Miocárdica/complicações
Miócitos Cardíacos/efeitos dos fármacos
Miócitos Cardíacos/fisiologia
Ouabaína
Músculos Papilares/citologia
Fenoxipropanolaminas/administração & dosagem
Distribuição Aleatória
Ratos
Ratos Sprague-Dawley
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (1-(4-(2-methoxyethyl)phenoxy)-3-(((2-2-methoxyphenoxy)ethyl)amino)-2-propanol); 0 (Adrenergic alpha-Antagonists); 0 (Adrenergic beta-Antagonists); 0 (Anti-Arrhythmia Agents); 0 (Phenoxypropanolamines); 5ACL011P69 (Ouabain); EC 1.1.- (Lactate Dehydrogenases); EC 2.7.3.2 (Creatine Kinase); M4I0D6VV5M (Calcium Chloride)
[Em] Mês de entrada:1602
[Cu] Atualização por classe:140625
[Lr] Data última revisão:
140625
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140626
[St] Status:MEDLINE


  10 / 134 MEDLINE  
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[PMID]:23598647
[Au] Autor:Serafim KR; Kishi MS; Canto-de-Souza A; Mattioli R
[Ad] Endereço:Laboratório de Neurociências, Departamento de Fisioterapia, Centro de Ciências Biológicas e da Saúde, Universidade Federal de São Carlos, São Carlos, SP, Brasil.
[Ti] Título:H1 but not H2 histamine antagonist receptors mediate anxiety-related behaviors and emotional memory deficit in mice subjected to elevated plus-maze testing.
[So] Source:Braz J Med Biol Res;46(5):440-6, 2013 May.
[Is] ISSN:1414-431X
[Cp] País de publicação:Brazil
[La] Idioma:eng
[Ab] Resumo:This study investigated the role of H1 and H2 receptors in anxiety and the retrieval of emotional memory using a Trial 1/Trial 2 (T1/T2) protocol in an elevated plus-maze (EPM). Tests were performed on 2 consecutive days, designated T1 and T2. Before T1, the mice received intraperitoneal injections of saline (SAL), 20 mg/kg zolantidine (ZOL, an H2 receptor antagonist), or 8.0 or 16 mg/kg chlorpheniramine (CPA, an H1 receptor antagonist). After 40 min, they were subjected to the EPM test. In T2 (24 h later), each group was subdivided into two additional groups, and the animals from each group were re-injected with SAL or one of the drugs. In T1, the Student t-test showed no difference between the SAL and ZOL or 8 mg/kg CPA groups with respect to the percentages of open arm entries (%OAE) and open arm time (%OAT). However, administration of CPA at the highest dose of 16 mg/kg decreased %OAE and %OAT, but not locomotor activity, indicating anxiogenic-like behavior. Emotional memory, as revealed by a reduction in open arm exploration between the two trials, was observed in all experimental groups, indicating that ZOL and 8 mg/kg CPA did not affect emotional memory, whereas CPA at the highest dose affected acquisition and consolidation, but not retrieval of memory. Taken together, these results suggest that H1 receptor, but not H2, is implicated in anxiety-like behavior and in emotional memory acquisition and consolidation deficits in mice subjected to EPM testing.
[Mh] Termos MeSH primário: Ansiedade/induzido quimicamente
Benzotiazóis/farmacologia
Clorfeniramina/farmacologia
Antagonistas dos Receptores Histamínicos H1/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Transtornos da Memória/induzido quimicamente
Fenoxipropanolaminas/farmacologia
Piperidinas/farmacologia
Receptores Histamínicos H1/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Masculino
Aprendizagem em Labirinto
Camundongos
Microinjeções
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (Histamine H1 Antagonists); 0 (Histamine H2 Antagonists); 0 (Phenoxypropanolamines); 0 (Piperidines); 0 (Receptors, Histamine H1); 3U6IO1965U (Chlorpheniramine); M1108XAY01 (zolantidine)
[Em] Mês de entrada:1403
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130420
[St] Status:MEDLINE



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