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Pesquisa : D02.078.370.500 [Categoria DeCS]
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  1 / 192 MEDLINE  
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[PMID]:17206612
[Au] Autor:Xie SX; Schalkhausser F; Ye QZ; Seifert R; Buschauer A
[Ad] Endereço:High Throughput Screening Laboratory, University of Kansas, Lawrence, USA.
[Ti] Título:Effects of impromidine- and arpromidine-derived guanidines on recombinant human and guinea pig histamine H1 and H2 receptors.
[So] Source:Arch Pharm (Weinheim);340(1):9-16, 2007 Jan.
[Is] ISSN:0365-6233
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Imidazolylpropylguanidines derived from impromidine and arpromidine are more potent and efficacious agonists at the guinea pig histamine H2 receptor (gpH2R) than at the human H2R (hH2R) in the GTPase assay. Additionally, such guanidines are histamine H1 receptor (H1R) antagonists with preference for the human relative to the guinea pig receptor. The purpose of this study was to examine structure-activity relationships of guanidines at human and guinea pig H1R and H2R species isoforms expressed in Sf9 insect cells. Three impromidine analogues and six arpromidine analogues exhibited agonistic activity at H2R and antagonistic activity at H1R as assessed in the steady-state GTPase assay. Species selectivity of derivatives was similar as compared with the parent compounds. None of the structural modifications examined (different aromatic ring systems and different ring substituents) was superior in terms of H2R potency and efficacy relative to impromidine and arpromidine, respectively. These data point to substantial structural constraints at the agonist binding site of H2R. Guanidines exhibited distinct structure-activity relationships for H1R antagonism in a radioligand competition binding assay and the GTPase assay and for H1R inverse agonism. Our data indicate that it is difficult to obtain guanidine-type agonists with high potency and high efficacy for hH2R, but those compounds may be useful tools for exploring the antagonist binding site and constitutive activity of H1R.
[Mh] Termos MeSH primário: Guanidinas/farmacologia
Agonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos H1/farmacologia
Imidazóis/farmacologia
Impromidina/farmacologia
Receptores Histamínicos H1/efeitos dos fármacos
Receptores Histamínicos H2/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Ligação Competitiva
Linhagem Celular
GTP Fosfo-Hidrolases/metabolismo
Subunidades alfa Gq-G11 de Proteínas de Ligação ao GTP/efeitos dos fármacos
Subunidades alfa Gq-G11 de Proteínas de Ligação ao GTP/genética
Subunidades alfa Gs de Proteínas de Ligação ao GTP/efeitos dos fármacos
Subunidades alfa Gs de Proteínas de Ligação ao GTP/genética
Guanidinas/química
Guanidinas/metabolismo
Cobaias
Agonistas dos Receptores Histamínicos/química
Agonistas dos Receptores Histamínicos/metabolismo
Antagonistas dos Receptores Histamínicos H1/química
Antagonistas dos Receptores Histamínicos H1/metabolismo
Seres Humanos
Imidazóis/química
Imidazóis/metabolismo
Impromidina/análogos & derivados
Impromidina/química
Impromidina/metabolismo
Insetos
Estrutura Molecular
Pirilamina/metabolismo
Receptores Histamínicos H1/genética
Receptores Histamínicos H1/metabolismo
Receptores Histamínicos H2/genética
Receptores Histamínicos H2/metabolismo
Proteínas Recombinantes de Fusão/efeitos dos fármacos
Relação Estrutura-Atividade
Transfecção
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Guanidines); 0 (Histamine Agonists); 0 (Histamine H1 Antagonists); 0 (Imidazoles); 0 (Receptors, Histamine H1); 0 (Receptors, Histamine H2); 0 (Recombinant Fusion Proteins); 85713MT0EH (arpromidine); 931L4X5WMM (Impromidine); EC 3.6.1.- (GTP Phosphohydrolases); EC 3.6.5.1 (GTP-Binding Protein alpha Subunits, Gq-G11); EC 3.6.5.1 (GTP-Binding Protein alpha Subunits, Gs); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:0705
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:070109
[St] Status:MEDLINE


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[PMID]:11771852
[Au] Autor:Shimada K; Abe T; Zhao Q; Mio M; Kamei C
[Ad] Endereço:Department of Pharmacology, Faculty of Pharmaceutical Sciences, Okayama University, Japan.
[Ti] Título:Effects of histamine and related compounds on the differentiation of HL-60-Eo cells into eosinophils.
[So] Source:Methods Find Exp Clin Pharmacol;23(7):383-8, 2001 Sep.
[Is] ISSN:0379-0355
[Cp] País de publicação:Spain
[La] Idioma:eng
[Ab] Resumo:The effects of histamine and related compounds on the differentiation of HL-60-Eo cells into eosinophils were studied. The histamine and H2 agonists impromidine and 4-methylhistamine caused concentration-related increases in the number of differentiated cells. On the other hand, the H1 agonists 2-methylhistamine and 2-pyndylethylamine showed no such effect. Histamine-induced eosinophil differentiation was antagonized by the H2 antagonists cimetidine and ranitidine. Histamine and H2 agonists inhibited (3H)-thymidine uptake, suggesting that these compounds caused a decrease in proliferation. Histamine as well as the H2 agonists impromidine and 4-methythistamine caused increases in cAMP level, and this effect was antagonized by ranitidine. From these findings, we concluded that both the differentiation of HL-60-Eo cells into eosinophils and proliferation of HL-60-Eo cells were mediated via H2 receptors.
[Mh] Termos MeSH primário: Eosinófilos/efeitos dos fármacos
Células HL-60/efeitos dos fármacos
Histamina/farmacologia
[Mh] Termos MeSH secundário: Diferenciação Celular/efeitos dos fármacos
Divisão Celular/efeitos dos fármacos
Cimetidina/farmacologia
AMP Cíclico/metabolismo
Relação Dose-Resposta a Droga
Eosinófilos/citologia
Eosinófilos/metabolismo
Células HL-60/citologia
Células HL-60/metabolismo
Histamina/análogos & derivados
Agonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos H1/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Seres Humanos
Impromidina/farmacologia
Metilistaminas/metabolismo
Metilistaminas/farmacologia
Ranitidina/farmacologia
Receptores Histamínicos H2/metabolismo
Timidina/farmacocinética
Fatores de Tempo
Trítio
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine Agonists); 0 (Histamine H1 Antagonists); 0 (Histamine H2 Antagonists); 0 (Methylhistamines); 0 (Receptors, Histamine H2); 10028-17-8 (Tritium); 54ST71P9EE (4-methylhistamine); 80061L1WGD (Cimetidine); 820484N8I3 (Histamine); 884KT10YB7 (Ranitidine); 931L4X5WMM (Impromidine); E0399OZS9N (Cyclic AMP); H5DHG2WBHM (2-methylhistamine); VC2W18DGKR (Thymidine)
[Em] Mês de entrada:0205
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:020105
[St] Status:MEDLINE


  3 / 192 MEDLINE  
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[PMID]:11123205
[Au] Autor:Synnerstad I; Johansson M; Nylander O; Holm L
[Ad] Endereço:Department of Physiology, Biomedical Center, Uppsala University, S-751 23 Uppsala, Sweden.
[Ti] Título:Intraluminal acid and gastric mucosal integrity: the importance of blood-borne bicarbonate.
[So] Source:Am J Physiol Gastrointest Liver Physiol;280(1):G121-9, 2001 Jan.
[Is] ISSN:0193-1857
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The acid-secreting gastric mucosa resists intraluminal acid better than the nonsecreting. Here we investigated pH at the epithelial cell surface, mucosal permeability, and blood flow during intraluminal administration of acid (100 mM) in acid-stimulated and nonstimulated gastric corpus mucosae. Surface pH (H(+)-selective microelectrodes), permeability (clearance of (51)Cr-EDTA), and mucosal blood flow (laser-Doppler flowmetry) were studied in Inactin-anesthetized rats. Acid secretion was stimulated with pentagastrin (40 microg. kg(-1). h(-1)) or impromidine (500 microg. kg(-1). h(-1)), or HCO(3)(-) (5 mmol. kg(-1). h(-1)) given intravenously. Surface pH was only slightly reduced by intraluminal acid in acid secretion-stimulated or HCO(3)(-)-treated rats but was substantially lowered in nonstimulated rats. Clearance increased threefold and blood flow increased by approximately 75% in nonstimulated rats. During stimulated acid secretion or intravenous infusion of HCO(3)(-), clearance was unchanged and blood flow increased by only approximately 30% during intraluminal acid. Increased epithelial transport of HCO(3)(-) buffering the mucus gel is most probably the explanation for the acid-secreting mucosa being less vulnerable to intraluminal acid than the nonsecreting.
[Mh] Termos MeSH primário: Equilíbrio Ácido-Base/fisiologia
Ácido Gástrico/metabolismo
Mucosa Gástrica/irrigação sanguínea
Mucosa Gástrica/metabolismo
Bicarbonato de Sódio/sangue
[Mh] Termos MeSH secundário: Animais
Permeabilidade Capilar/fisiologia
Quelantes/farmacocinética
Radioisótopos de Cromo
Ácido Edético/farmacocinética
Células Epiteliais/efeitos dos fármacos
Células Epiteliais/metabolismo
Mucosa Gástrica/efeitos dos fármacos
Agonistas dos Receptores Histamínicos/farmacologia
Concentração de Íons de Hidrogênio
Impromidina/farmacologia
Fluxometria por Laser-Doppler
Masculino
Pentagastrina/farmacologia
Ratos
Ratos Sprague-Dawley
Fluxo Sanguíneo Regional/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Chelating Agents); 0 (Chromium Radioisotopes); 0 (Histamine Agonists); 8MDF5V39QO (Sodium Bicarbonate); 931L4X5WMM (Impromidine); 9G34HU7RV0 (Edetic Acid); EF0NX91490 (Pentagastrin)
[Em] Mês de entrada:0101
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:001221
[St] Status:MEDLINE


  4 / 192 MEDLINE  
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[PMID]:10598794
[Au] Autor:Prast H; Tran MH; Lamberti C; Fischer H; Kraus M; Grass K; Philippu A
[Ad] Endereço:Institut für Pharmakologie und Toxikologie der Universität Innsbruck, Austria. Helmut.Prast@uibk.ac.at
[Ti] Título:Histaminergic neurons modulate acetylcholine release in the ventral striatum: role of H1 and H2 histamine receptors.
[So] Source:Naunyn Schmiedebergs Arch Pharmacol;360(5):552-7, 1999 Nov.
[Is] ISSN:0028-1298
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:To investigate whether H1 and H2 histamine receptors are implicated in the modulation of acetylcholine release by endogenous histamine, the ventral striatum of the conscious, freely moving rat was superfused by the push-pull superfusion technique with drugs and the release of acetylcholine was determined in the superfusate. Superfusion with the H1 receptor agonist 2-thiazolylethylamine (TEA, 50 micromol/l) enhanced the release of acetylcholine, while the H1 receptor antagonist triprolidine (50 micromol/l) reduced acetylcholine outflow and abolished the TEA-evoked release of the neurotransmitter. The inhibitory effect of triprolidine was not influenced either on simultaneous superfusion with 10 micromol/l (+/-)-7-bromo-1-(fluoresceinylthioureido)phenyl-8-hydroxy-3-methyl -2,3,4,5-tetrahydro-1H-benzazepine (SKF-83566, D1 dopamine receptor antagonist) and 50 micromol/l quinpirole (D2/D3 dopamine receptor agonist) or on superfusion with the GABAA receptor antagonist bicuculline (50 micromol/l). The H2 receptor antagonists ranitidine or famotidine (50 micromol/l each) greatly enhanced acetylcholine release rate in the ventral striatum. Presuperfusion with alpha-fluoromethylhistidine (FMH, 1 mmol/l), which inhibits neuronal synthesis of histamine, abolished the famotidine-induced release of acetylcholine. The releasing effect of famotidine was also abolished on simultaneous superfusion with 10 micromol/l SKF-83566 and 50 micromol/l quinpirole. The release of acetylcholine elicited by famotidine was reversed to a decreased acetylcholine outflow when the striatum was superfused with the GABA(A) receptor antagonist bicuculline (50 micromol/l) prior to famotidine. Superfusion with the H2 receptor agonist impromidine (1 micromol/l) decreased acetylcholine outflow, while the H2 agonist dimaprit (50 micromol/l) exerted the opposite effect. The releasing effect of dimaprit was not influenced by FMH (1 mmol/l), but it was abolished in the presence of SKF-83566 (10 micromol/l) and quinpirole (50 micromol/l). In the presence of bicuculline the release of acetylcholine by dimaprit was enhanced and prolonged. It seems possible that dimaprit and impromidine stimulate different subtypes of H2 receptors. The findings suggest that the release of acetylcholine in the striatum is modulated by neighbouring histaminergic neurons in a complex way. Stimulation of H1 histamine receptors, probably located on cholinergic neurons, enhances acetylcholine release. Stimulation by histamine of H2 receptors located on cholinergic or GABAergic neurons enhances the release of acetylcholine, while stimulation of H2 receptors located on dopaminergic neurons exerts the opposite effect.
[Mh] Termos MeSH primário: Acetilcolina/metabolismo
Neurônios/fisiologia
Receptores Histamínicos H1/fisiologia
Receptores Histamínicos H2/fisiologia
Córtex Visual/metabolismo
[Mh] Termos MeSH secundário: Animais
Bicuculina/farmacologia
Dimaprit/farmacologia
Famotidina/farmacologia
Antagonistas GABAérgicos/farmacologia
Agonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos/farmacologia
Impromidina/farmacologia
Ligantes
Masculino
Perfusão
Ranitidina/farmacologia
Ratos
Ratos Sprague-Dawley
Receptores Dopaminérgicos/metabolismo
Receptores de GABA-A/efeitos dos fármacos
Técnicas Estereotáxicas
Córtex Visual/citologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (GABA Antagonists); 0 (Histamine Agonists); 0 (Histamine Antagonists); 0 (Ligands); 0 (Receptors, Dopamine); 0 (Receptors, GABA-A); 0 (Receptors, Histamine H1); 0 (Receptors, Histamine H2); 5QZO15J2Z8 (Famotidine); 884KT10YB7 (Ranitidine); 931L4X5WMM (Impromidine); N9YNS0M02X (Acetylcholine); Y37615DVKC (Bicuculline); ZZQ699148P (Dimaprit)
[Em] Mês de entrada:0002
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:991222
[St] Status:MEDLINE


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[PMID]:10374372
[Au] Autor:Tan M; Pan Z; Wang Q; Xu Y
[Ad] Endereço:Laboratory of Blood Physiology, Hunan Medical University, Changsha, China.
[Ti] Título:Effects of different subtypes of histamine receptors on proliferation and differentiation of murine colony forming unit granulocyte-macrophage and colony forming unit megakaryocyte.
[So] Source:Chin Med J (Engl);111(2):132-5, 1998 Feb.
[Is] ISSN:0366-6999
[Cp] País de publicação:China
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To investigate the function and characteristics of histamine receptors on the hemopoietic progenitor cells. METHODS: BDF1 mice (both male and female), inbred at our university, aged 8-12 weeks, weighing 20-24 g, were used in this study. Bone marrow cells were incubated for 1 hour at 37 degrees C with 2-AT (H1 receptor agonist) or impromidine (H2 receptor agonist) alone, or in combination with the antagonists pyrilamine or cimetidine respectively. Control experiment was performed in Dulbecco's modified Eagle's Medium (DMEM) alone. Cells treated with different drugs were performed by colony forming unit-granulocyte-macrophage (CFU-GM) and colony forming unit-megakaryocyte (CFU-Meg) assay. RESULTS: When bone marrow cells were treated with 10(-8) mol/L to 10(-5) mol/L of 2-thiazolylethylamine (2-AT) which had no influence on CFU-GM and CFU-Meg proliferation, 10(-8) mol/L to 10(-5) mol/L of impromidine could increase the number of CFU-GM and CFU-Meg colonies. The effects of H2 receptor agonists on CFU-GM, CFU-Meg could be antagonized by H1 receptor agonist. CONCLUSIONS: Our findings suggest the existence of histamine H1 and H2 receptors on the hemopoietic progenitor cells and the antagonism between two different histamine receptor subtypes on the proliferation of CFU-GM and CFU-Meg.
[Mh] Termos MeSH primário: Células-Tronco Hematopoéticas/citologia
Receptores Histamínicos H1/fisiologia
Receptores Histamínicos H2/fisiologia
[Mh] Termos MeSH secundário: Animais
Células da Medula Óssea
Diferenciação Celular
Divisão Celular
Células Cultivadas
Feminino
Granulócitos/citologia
Agonistas dos Receptores Histamínicos/farmacologia
Impromidina/farmacologia
Macrófagos/citologia
Masculino
Megacariócitos/citologia
Camundongos
Camundongos Endogâmicos
Tiazóis/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine Agonists); 0 (Receptors, Histamine H1); 0 (Receptors, Histamine H2); 0 (Thiazoles); 18453-07-1 (2-(2-aminoethyl)thiazole); 931L4X5WMM (Impromidine)
[Em] Mês de entrada:9907
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:990622
[St] Status:MEDLINE


  6 / 192 MEDLINE  
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[PMID]:9792230
[Au] Autor:Coruzzi G; Poli E; Pozzoli C; Bertaccini G; Timmerman H
[Ad] Endereço:Institute of Pharmacology, University of Parma-School of Medicine, Italy.
[Ti] Título:Histamine receptor-independent muscle relaxation elicited by a series of histamine H2-receptor agonists on the isolated guinea pig duodenum: a study into the mechanism of action.
[So] Source:Gen Pharmacol;31(4):643-51, 1998 Oct.
[Is] ISSN:0306-3623
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:1. The histamine H2 receptor agonists, dimaprit, impromidine, amthamine, and several dimaprit- and impromidine-analogues were investigated for their spasmolytic activity on the guinea pig duodenum, precontracted with acetylcholine or KCl. 2. Almost all the H2 receptor agonists exerted a histamine H2 receptor-independent muscle relaxation, which was more evident on acetylcholine- than on KCl-precontracted preparations. 3. The relaxing activity of these compounds was independent of inhibitory receptors, like beta-adrenergic, GABA-ergic, serotoninergic, etc. Similarly, modifications of cyclic nucleotide metabolism and nitric oxide production did not appear to be involved. 4. The behavior of histamine H2-receptor agonists was shared only by the Na+-blocker procaine, the intracellular Ca2+-antagonist ruthenium red and, at least in terms of efficacy, by the protein kinase C inhibitor, chelerithrine. 5. This spasmolytic effect is probably due to an impairment of receptor-mediated depolarization at the plasma membrane level and/or an inhibitory activity on the protein kinase C-dependent activation of the contractile machinery. 6. Finally, our findings suggest that the histamine H2 receptor-independent muscle relaxation is a general feature shown by H2 receptor agonists endowed with different chemical structure and the putative spasmolytic "receptor" prefers a (substituted) thiazole over a (substituted) imidazole.
[Mh] Termos MeSH primário: Agonistas dos Receptores Histamínicos/farmacologia
Contração Muscular/efeitos dos fármacos
Músculo Liso/efeitos dos fármacos
Parassimpatolíticos/farmacologia
[Mh] Termos MeSH secundário: Animais
Dimaprit/análise
Dimaprit/farmacologia
Duodeno/efeitos dos fármacos
Estimulação Elétrica
Cobaias
Impromidina/análise
Impromidina/farmacologia
Técnicas In Vitro
Masculino
Relação Estrutura-Atividade
Tiazóis/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine Agonists); 0 (Parasympatholytics); 0 (Thiazoles); 142437-67-0 (amthamine); 931L4X5WMM (Impromidine); ZZQ699148P (Dimaprit)
[Em] Mês de entrada:9901
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:981029
[St] Status:MEDLINE


  7 / 192 MEDLINE  
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[PMID]:9569243
[Au] Autor:Krouwels FH; Hol BE; Lutter R; Bruinier B; Bast A; Jansen HM; Out TA
[Ad] Endereço:Department of Pulmonology, Clinical and Laboratory Immunology Unit, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands.
[Ti] Título:Histamine affects interleukin-4, interleukin-5, and interferon-gamma production by human T cell clones from the airways and blood.
[So] Source:Am J Respir Cell Mol Biol;18(5):721-30, 1998 May.
[Is] ISSN:1044-1549
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:High levels of histamine can be found in the airways of asthma patients. This study describes the effects of histamine on anti-CD3-induced production of IL-4, IL-5, and IFN-gamma by T cell clones from subjects with allergic asthma and healthy subjects. T cell clones were obtained from bronchoalveolar lavage (BAL) fluid and blood. The number of clones tested, and the percentage of clones in which histamine inhibited or enhanced cytokine production by more than 25%, were as follows: IL-4, 47, 8.5%, and 4.3%; IL-5, 43, 14%, and 30%; and IFN-gamma, 52, 40%, and 15%. Inhibition of IL-5 and IFN-gamma production was reversed by IL-2. The enhancement of IFN-gamma production was associated with an enhancement of both IL-2 production and proliferation. In 21% of the clones a combined effect consisting of inhibition of IFN-gamma production and enhancement of IL-5 production was found. This response was reversed by H2-receptor antagonists and was significantly associated with a histamine-induced increase in intracellular levels of cAMP. The role of cAMP in mediating the histamine effects was supported by the observations that the beta2-agonist salbutamol had effects similar to histamine and that high concentrations of PGE2 mimicked the inhibitory effects of histamine. Clones from BAL fluid and blood showed similar responses, as did clones from patients with asthma and from control subjects. The enhancement of IFN-gamma production by histamine, however, was found only in clones from healthy subjects. The results warrant further investigations on the role of cAMP in the regulation of cytokine production.
[Mh] Termos MeSH primário: Histamina/farmacologia
Interferon gama/biossíntese
Interleucina-4/biossíntese
Interleucina-5/biossíntese
Linfócitos T/metabolismo
[Mh] Termos MeSH secundário: Adenilil Ciclases/metabolismo
Agonistas Adrenérgicos beta/farmacologia
Albuterol/farmacologia
Asma/tratamento farmacológico
Asma/imunologia
Asma/metabolismo
Líquido da Lavagem Broncoalveolar/citologia
Células Clonais
AMP Cíclico/metabolismo
Dinoprostona/farmacologia
Ativação Enzimática/efeitos dos fármacos
Famotidina/farmacologia
Agonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos H1/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Seres Humanos
Impromidina/farmacologia
Interleucina-2/biossíntese
Pulmão/citologia
Pulmão/imunologia
Metilistaminas/farmacologia
Piperidinas/farmacologia
Piridinas/farmacologia
Ranitidina/farmacologia
Linfócitos T/efeitos dos fármacos
Triprolidina/farmacologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-Agonists); 0 (Histamine Agonists); 0 (Histamine Antagonists); 0 (Histamine H1 Antagonists); 0 (Histamine H2 Antagonists); 0 (Interleukin-2); 0 (Interleukin-5); 0 (Methylhistamines); 0 (Piperidines); 0 (Pyridines); 207137-56-2 (Interleukin-4); 2L8T9S52QM (Triprolidine); 5QZO15J2Z8 (Famotidine); 6986-90-9 (alpha-methylhistamine); 820484N8I3 (Histamine); 82115-62-6 (Interferon-gamma); 884KT10YB7 (Ranitidine); 931L4X5WMM (Impromidine); ATW1AH7OJ5 (2-(2-aminoethyl)pyridine); E0399OZS9N (Cyclic AMP); EC 4.6.1.1 (Adenylyl Cyclases); II4319BWUI (thioperamide); K7Q1JQR04M (Dinoprostone); QF8SVZ843E (Albuterol)
[Em] Mês de entrada:9806
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:980606
[St] Status:MEDLINE


  8 / 192 MEDLINE  
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[PMID]:9486484
[Au] Autor:Yanovsky Y; Haas HL
[Ad] Endereço:Department of Physiology, Heinrich-Heine-Universität, Düsseldorf, Germany.
[Ti] Título:Histamine increases the bursting activity of pyramidal cells in the CA3 region of mouse hippocampus.
[So] Source:Neurosci Lett;240(2):110-2, 1998 Jan 09.
[Is] ISSN:0304-3940
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:An excitatory action of histamine was investigated by intracellular recording in the CA3 region of hippocampal slices. Bath application of histamine or impromidine, a H2 receptor agonist, had the following effects: (1) a depolarisation in 60% and no changes in membrane potential in 40% of the CA3 pyramids; (2) single cell firing and burst activity were evoked or more than doubled when spontaneously present; (3) the bursts were prolonged and often followed by afterdischarges instead of the normal afterhyperpolarisations (AHPs); (4) synaptic stimulation evoked large bursts instead of excitatory synaptic potentials (EPSPs) and primary burst responses became prolonged. CA3 bursts may play a decisive role in memory trace formation, their facilitation and potentiation is in keeping with a positive role of the histaminergic system in attention and learning.
[Mh] Termos MeSH primário: Hipocampo/efeitos dos fármacos
Hipocampo/fisiologia
Histamina/farmacologia
Células Piramidais/efeitos dos fármacos
Células Piramidais/fisiologia
[Mh] Termos MeSH secundário: Potenciais de Ação/efeitos dos fármacos
Animais
Cimetidina/farmacologia
Estimulação Elétrica
Feminino
Hipocampo/citologia
Impromidina/farmacologia
Técnicas In Vitro
Masculino
Camundongos
Perfusão
Transmissão Sináptica/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
80061L1WGD (Cimetidine); 820484N8I3 (Histamine); 931L4X5WMM (Impromidine)
[Em] Mês de entrada:9804
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:980305
[St] Status:MEDLINE


  9 / 192 MEDLINE  
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[PMID]:9379409
[Au] Autor:Jafri MS; Moore KA; Taylor GE; Weinreich D
[Ad] Endereço:University of Maryland, School of Medicine, Department of Pharmacology and Experimental Therapeutics, Baltimore 21201-1559, USA.
[Ti] Título:Histamine H1 receptor activation blocks two classes of potassium current, IK(rest) and IAHP, to excite ferret vagal afferents.
[So] Source:J Physiol;503 ( Pt 3):533-46, 1997 Sep 15.
[Is] ISSN:0022-3751
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:1. Intracellular recordings were made in intact and acutely dissociated vagal afferent neurones (nodose ganglion cells) of the ferret to investigate the membrane effects of histamine. 2. In current-clamp or voltage-clamp recordings, histamine (10 microM) depolarized the membrane potential (10 +/- 0.8 mV; mean +/- S.E.M.; n = 27) or produced an inward current of 1.6 +/- 0.35 nA (n = 27) in approximately 80% of the neurones. 3. Histamine (10 microM) also blocked the post-spike slow after-hyperpolarization (AHP slow) present in 80% of these neurones (95 +/- 3.2%; n = 5). All neurones possessing AHPslow in ferret nodose were C fibre neurones; all AHPslow neurones had conduction velocities < or = 1 m s-1 (n = 7). 4. Both the histamine-induced inward current and the block of AHPslow were concentration dependent and each had an estimated EC50 value of 2 microM. These histamine-induced effects were mimicked by the histamine H1 receptor agonist 2-(2-aminoethyl) thiazole dihydrochloride (10 microM) and blocked by the H1 antagonists pyrilamine (100 nM) or diphenhydramine (100 nM). Schild plot analysis of the effect of pyrilamine on the histamine-induced inward current revealed a pA2 value of 9.7, consistent with that expected for an H1 receptor. Neither impromidine (10 microM) nor R(-)-alpha-methylhistamine (10 microM), selective H2 or H3 agonists, respectively, significantly affected the membrane potential, input resistance or AHPslow. 5. The reversal potential (Vrev) for the histamine-induced inward current was -84 +/- 2.1 mV (n = 4). The Vrev for the histamine response shifted in a Nernstian manner with changes in the extracellular potassium concentration. Alterations in the extracellular chloride concentration had no significant effect on the Vrev of the histamine response (n = 3). The Vrev for the AHPslow was -85 +/- 1.7 mV (n = 4). 6. These results indicate that histamine increases the excitability of ferret vagal afferent somata by interfering with two classes of potassium current: the resting or 'leak' potassium current (IK(rest)) and the potassium current underlying a post-spike slow after-hyperpolarization (IAHP). Both these effects can occur in the same neurone and involve activation of the same histamine receptor subtype, the histamine H1 receptor.
[Mh] Termos MeSH primário: Neurônios Aferentes/fisiologia
Potássio/metabolismo
Receptores Histamínicos H1/metabolismo
Nervo Vago/fisiologia
[Mh] Termos MeSH secundário: Potenciais de Ação/fisiologia
Animais
Difenidramina/farmacologia
Condutividade Elétrica
Furões
Histamina/farmacologia
Agonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos H1/farmacologia
Impromidina/farmacologia
Masculino
Metilistaminas/farmacologia
Neurônios Aferentes/química
Gânglio Nodoso/citologia
Técnicas de Patch-Clamp
Potássio/farmacocinética
Bloqueadores dos Canais de Potássio
Pirilamina/farmacologia
Tiazóis/farmacologia
Nervo Vago/citologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Histamine Agonists); 0 (Histamine H1 Antagonists); 0 (Methylhistamines); 0 (Potassium Channel Blockers); 0 (Receptors, Histamine H1); 0 (Thiazoles); 18453-07-1 (2-(2-aminoethyl)thiazole); 6986-90-9 (alpha-methylhistamine); 820484N8I3 (Histamine); 8GTS82S83M (Diphenhydramine); 931L4X5WMM (Impromidine); HPE317O9TL (Pyrilamine); RWP5GA015D (Potassium)
[Em] Mês de entrada:9711
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:971023
[St] Status:MEDLINE


  10 / 192 MEDLINE  
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[PMID]:9098743
[Au] Autor:Stenton GR; Lau HY
[Ad] Endereço:Department of Pharmacology, Faculty of Medicine, Chinese University of Hong Kong, Shatin, New Territories, Hong Kong.
[Ti] Título:Effects of histamine agonists and antagonists on rat peritoneal mast cells.
[So] Source:Inflamm Res;46 Suppl 1:S15-6, 1997 Mar.
[Is] ISSN:1023-3830
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Mh] Termos MeSH primário: Agonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos/farmacologia
Mastócitos/efeitos dos fármacos
Mastócitos/fisiologia
[Mh] Termos MeSH secundário: Animais
Dimaprit/farmacologia
Liberação de Histamina/efeitos dos fármacos
Imidazóis/farmacologia
Impromidina/farmacologia
Masculino
Cavidade Peritoneal/citologia
Ratos
Ratos Sprague-Dawley
Receptores Histamínicos H3/fisiologia
Tioureia/análogos & derivados
Tioureia/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine Agonists); 0 (Histamine Antagonists); 0 (Imidazoles); 0 (Receptors, Histamine H3); 677MJ4VPZC (imetit); 931L4X5WMM (Impromidine); GYV9AM2QAG (Thiourea); ZZQ699148P (Dimaprit)
[Em] Mês de entrada:9706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:970301
[St] Status:MEDLINE



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