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[PMID]:26461804
[Au] Autor:Saxena M; Bhunia SS; Saxena AK
[Ad] Endereço:a Department of Chemistry , Amity University , Lucknow , India.
[Ti] Título:Molecular modelling studies on 2-substituted octahydropyrazinopyridoindoles for histamine H2 receptor antagonism.
[So] Source:SAR QSAR Environ Res;26(7-9):739-55, 2015.
[Is] ISSN:1029-046X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The human histamine H2 receptor (hH2HR) is a G-protein coupled receptor protein with seven transmembrane (TM)-spanning helices primarily involved in regulation of gastric acid secretion. Antagonists targeting hH2HR are useful in the treatment of hyperacidic conditions such as peptic ulcers, gastresophageal reflux disease and gastrointestinal bleeding. We have previously reported the antagonism of 2-substituted pyrazinopyridoindoles at the human histamine H1 receptor and mode of binding of these compounds at the hH1HR using in silico methods. Interestingly, some of the compounds in the series also showed promising activity towards hH2HR that prompted us to investigate the mode of binding of these compounds at hH2HR. In the absence of the crystal structure of hH2HR a homology model has been constructed using multiple sequence alignment, using the X-ray crystal structures of Turkey ß1-adrenergic receptor (tß1AR), Human histamine H1 receptor (hH1HR), Human ß2-adrenergic receptor (hß2AR) and Human D3 dopamine receptor (hD3R). The important residues for binding were depicted in TMIII, TMV, TMVI and TMVII by the homology modelled hH2HR for 2-substituted pyrazinopyridoindoles. A comparative study for deducing the selectivity regarding the binding towards hH1HR and hH2HR has been carried out, which may be useful in designing of selective hH1HR/hH2HR antagonists in these classes of compounds.
[Mh] Termos MeSH primário: Antagonistas dos Receptores Histamínicos H2/química
Receptores Histamínicos H2/química
[Mh] Termos MeSH secundário: Cimetidina/química
Simulação por Computador
Famotidina/química
Seres Humanos
Indóis/química
Metiamida/química
Simulação de Acoplamento Molecular
Pirazinas/química
Piridinas/química
Ranitidina/química
Homologia de Sequência de Aminoácidos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine H2 Antagonists); 0 (Indoles); 0 (Pyrazines); 0 (Pyridines); 0 (Receptors, Histamine H2); 3K7670861M (Metiamide); 5QZO15J2Z8 (Famotidine); 80061L1WGD (Cimetidine); 884KT10YB7 (Ranitidine)
[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:151014
[St] Status:MEDLINE
[do] DOI:10.1080/1062936X.2015.1088572


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[PMID]:17332265
[Au] Autor:Preuss H; Ghorai P; Kraus A; Dove S; Buschauer A; Seifert R
[Ad] Endereço:Department of Pharmaceutical/Medicinal Chemistry II, Institute of Pharmacy, University of Regensburg, Regensburg, Germany.
[Ti] Título:Constitutive activity and ligand selectivity of human, guinea pig, rat, and canine histamine H2 receptors.
[So] Source:J Pharmacol Exp Ther;321(3):983-95, 2007 Jun.
[Is] ISSN:0022-3565
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Previous studies revealed pharmacological differences between human and guinea pig histamine H(2) receptors (H(2)Rs) with respect to the interaction with guanidine-type agonists. Because H(2)R species variants are structurally very similar, comparative studies are suited to relate different properties of H(2)R species isoforms to few molecular determinants. Therefore, we systematically compared H(2)Rs of human (h), guinea pig (gp), rat (r), and canine (c). Fusion proteins of hH(2)R, gpH(2)R, rH(2)R, and cH(2)R, respectively, and the short splice variant of G(salpha), G(salphaS), were expressed in Sf9 insect cells. In the membrane steady-state GTPase activity assay, cH(2)R-G(salphaS) but neither gpH(2)R-G(salphaS) nor rH(2)R-G(salphaS) showed the hallmarks of increased constitutive activity compared with hH(2)R-G(salphaS), i.e., increased efficacies of partial agonists, increased potencies of agonists with the extent of potency increase being correlated with the corresponding efficacies at hH(2)R-G(salphaS), increased inverse agonist efficacies, and decreased potencies of antagonists. Furthermore, in membranes expressing nonfused H(2)Rs without or together with mammalian G(salphaS) or H(2)R-G(salpha) fusion proteins, the highest basal and GTP-dependent increases in adenylyl cyclase activity were observed for cH(2)R. An example of ligand selectivity is given by metiamide, acting as an inverse agonist at hH(2)R-G(salphaS), gpH(2)R-G(salphaS), and rH(2)R-G(salphaS) in the GTPase assay in contrast to being a weak partial agonist with decreased potency at cH(2)R-G(salphaS). In conclusion, the cH(2)R exhibits increased constitutive activity compared with hH(2)R, gpH(2)R, and rH(2)R, and there is evidence for ligand-specific conformations in H(2)R species isoforms.
[Mh] Termos MeSH primário: Agonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Receptores Histamínicos H2/metabolismo
[Mh] Termos MeSH secundário: Adenilil Ciclases/metabolismo
Animais
Baculoviridae/genética
Linhagem Celular
Membrana Celular/efeitos dos fármacos
Membrana Celular/metabolismo
Cães
GTP Fosfo-Hidrolases/metabolismo
Subunidades alfa Gs de Proteínas de Ligação ao GTP/genética
Subunidades alfa Gs de Proteínas de Ligação ao GTP/metabolismo
Cobaias
Histamina/farmacologia
Seres Humanos
Ligantes
Metiamida/farmacologia
Ratos
Receptores Histamínicos H2/genética
Proteínas Recombinantes de Fusão/metabolismo
Proteínas Recombinantes/metabolismo
Especificidade da Espécie
Spodoptera
Transfecção
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine Agonists); 0 (Histamine H2 Antagonists); 0 (Ligands); 0 (Receptors, Histamine H2); 0 (Recombinant Fusion Proteins); 0 (Recombinant Proteins); 3K7670861M (Metiamide); 820484N8I3 (Histamine); EC 3.6.1.- (GTP Phosphohydrolases); EC 3.6.5.1 (GTP-Binding Protein alpha Subunits, Gs); EC 4.6.1.1 (Adenylyl Cyclases)
[Em] Mês de entrada:0707
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:070303
[St] Status:MEDLINE


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[PMID]:15231494
[Au] Autor:Matsumoto I; Inoue Y; Tsuchiya K; Shimada T; Aikawa T
[Ad] Endereço:Dept. of Physiology, Nagasaki Univ. School of Medicine, Nagasaki 852-8523, Japan. matu-itu@net.nagasaki-u.ac.jp
[Ti] Título:Degranulation of mast cells located in median eminence in response to compound 48/80 evokes adrenocortical secretion via histamine and CRF in dogs.
[So] Source:Am J Physiol Regul Integr Comp Physiol;287(4):R969-80, 2004 Oct.
[Is] ISSN:0363-6119
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The effect of intracerebroventricular infusion of compound 48/80 (C48/80), a mast cell secretagogue, on adrenal cortisol secretion was investigated in dogs under pentobarbital sodium anesthesia. A marked increase in adrenal cortisol secretion was elicited by C48/80 along with a concomitant increase in the plasma levels of cortisol and immunoreactive ACTH, but neither arterial blood pressure and heart rate nor the plasma histamine level altered significantly. Pretreatment with either anti-CRF antiserum or pyrilamine maleate (H(1) histamine-receptor antagonist) significantly attenuated the C48/80-evoked increase in cortisol secretion, but pretreatment with metiamide (H(2)-receptor antagonist) significantly potentiated it. Significant attenuation of the C48/80-evoked increase in cortisol also occurred in dogs given ketotifen, a mast cell stabilizing drug, before pharmacologic challenge. In the pars tuberalis and median eminence (ME), mast cells were highly concentrated in close association with the primary plexus of the hypophysial portal system. Degranulated mast cells were extensively found in the ME of C48/80-treated animals. These results suggest that mast cells located in these regions liberated histamine within the brain as a result of degranulation induced by C48/80 and that this led to activation of the hypothalamic-pituitary-adrenocortical axis.
[Mh] Termos MeSH primário: Córtex Suprarrenal/secreção
Degranulação Celular/efeitos dos fármacos
Hormônio Liberador da Corticotropina/fisiologia
Histamina/fisiologia
Eminência Mediana/citologia
Eminência Mediana/efeitos dos fármacos
p-Metoxi-N-metilfenetilamina/farmacologia
[Mh] Termos MeSH secundário: Córtex Suprarrenal/efeitos dos fármacos
Hormônio Adrenocorticotrópico/farmacologia
Animais
Cromatografia em Camada Delgada
Cães
Relação Dose-Resposta a Droga
Epinefrina/farmacologia
Feminino
Hemodinâmica/efeitos dos fármacos
Histamina/sangue
Antagonistas dos Receptores Histamínicos H1/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Hidrocortisona/sangue
Hidrocortisona/secreção
Injeções Intraventriculares
Cetotifeno/farmacologia
Masculino
Metiamida/farmacologia
Pirilamina/farmacologia
Circulação Esplâncnica/fisiologia
p-Metoxi-N-metilfenetilamina/administração & dosagem
p-Metoxi-N-metilfenetilamina/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine H1 Antagonists); 0 (Histamine H2 Antagonists); 3K7670861M (Metiamide); 4091-50-3 (p-Methoxy-N-methylphenethylamine); 820484N8I3 (Histamine); 9002-60-2 (Adrenocorticotropic Hormone); 9015-71-8 (Corticotropin-Releasing Hormone); HPE317O9TL (Pyrilamine); WI4X0X7BPJ (Hydrocortisone); X49220T18G (Ketotifen); YKH834O4BH (Epinephrine)
[Em] Mês de entrada:0410
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:040703
[St] Status:MEDLINE


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[PMID]:11191621
[Au] Autor:Scaccianoce S; Lombardo K; Nicolai R; Affricano D; Angelucci L
[Ad] Endereço:Department of Human Physiology and Pharmacology, University La Sapienza, Rome, Italy. scaccianoce@uniroma1.it
[Ti] Título:Studies on the involvement of histamine in the hypothalamic-pituitary-adrenal axis activation induced by nerve growth factor.
[So] Source:Life Sci;67(26):3143-52, 2000 Nov 17.
[Is] ISSN:0024-3205
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Nerve growth factor (NGF) has been shown to stimulate the hypothalamic-pituitary-adrenocortical (HPA) axis. Since NGF induces the release of histamine from mast cells and in consideration of the fact that histamine is an HPA axis activator, we investigated whether NGF adrenocortical stimulation is mediated by histamine. To accomplish with it, the H1 histamine antagonist promethazine and the H2 antagonists metiamide and zolantidine were used in freely-moving cannulated rats. The increase in plasma corticosterone concentration induced by histamine administration was prevented completely by promethazine pretreatment but was unaffected by the H2 antagonists. Neither H1 nor H2 antagonists affected the adrenocortical stimulation induced by NGF administration. Moreover, since mast cells are reportedly present in the rat adrenal gland and the locally released histamine mediates the release of adrenaline which, in turn, stimulates glucocorticoid synthesis and secretion, we studied the effect of NGF on basal and ACTH-stimulated corticosterone release from in vitro isolated quartered adrenal glands and collagenase-dispersed adrenal cells. The results from these in vitro experiments have indicated that NGF modified neither spontaneous nor stimulated corticosterone release. Altogether these observations suggest that endogenous histamine is unlikely to be involved in HPA axis stimulation by NGF and reinforce the previously proposed concept of an active participation of NGF in the control of adrenocortical activity.
[Mh] Termos MeSH primário: Histamina/fisiologia
Sistema Hipotálamo-Hipofisário/fisiologia
Fator de Crescimento Neural/fisiologia
Sistema Hipófise-Suprarrenal/fisiologia
[Mh] Termos MeSH secundário: Glândulas Suprarrenais/metabolismo
Animais
Benzotiazóis
Cateterismo
Corticosterona/metabolismo
Antagonistas dos Receptores Histamínicos H1/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Masculino
Metiamida/farmacologia
Camundongos
Fenoxipropanolaminas
Piperidinas/farmacologia
Prometazina/farmacologia
Ratos
Ratos Wistar
Tiazóis/farmacologia
[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 (Thiazoles); 3K7670861M (Metiamide); 820484N8I3 (Histamine); 9061-61-4 (Nerve Growth Factor); FF28EJQ494 (Promethazine); M1108XAY01 (zolantidine); W980KJ009P (Corticosterone)
[Em] Mês de entrada:0101
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:010224
[St] Status:MEDLINE


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[PMID]:10567937
[Au] Autor:Wolff JC; Barr L; Moss P
[Ad] Endereço:SmithKline Beecham Pharmaceuticals, New Frontiers Science Park North, Third Avenue, Harlow, Essex CM19 5AW, UK. Jean-Claude_Wolff-1@sbphrd.com
[Ti] Título:New ultraviolet signal actuated switching valve for the measurement of low level impurities by liquid chromatography/mass spectrometry.
[So] Source:Rapid Commun Mass Spectrom;13(23):2376-81, 1999.
[Is] ISSN:0951-4198
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A new ultraviolet (UV) signal actuated switching valve for diverting the main matrix compound to waste, preventing it entering the ion source of the mass spectrometer is described. Sensitivity for trace impurities eluting after the drug substance cimetidine or related compounds could be enhanced by a factor of 4-5. The increase in sensitivity was dependent on the type of ion source which interfaced the mass spectrometer. The benefit of the switching valve was greater with a line of sight type source than with an orthogonal one. The detection limit for a trace compound in a matrix compound was improved by up to a factor of 10 with the line of sight type source but only by a factor of 5 with the orthogonal source.
[Mh] Termos MeSH primário: Cimetidina/normas
Contaminação de Medicamentos
Espectrometria de Massas/métodos
[Mh] Termos MeSH secundário: Cimetidina/química
Metiamida/química
Metiamida/isolamento & purificação
Estrutura Molecular
Sensibilidade e Especificidade
Espectrofotometria Ultravioleta/métodos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
3K7670861M (Metiamide); 80061L1WGD (Cimetidine)
[Em] Mês de entrada:0001
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:991124
[St] Status:MEDLINE


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[PMID]:9972321
[Au] Autor:Ali SA; Peter J; Ali AS
[Ad] Endereço:Post Graduate Zoology Department, Saifia College of Science and Education, Bhopal, India.
[Ti] Título:Histamine receptors in the skin melanophores of Indian bullfrog Rana tigerina.
[So] Source:Comp Biochem Physiol A Mol Integr Physiol;121(3):229-34, 1998 Nov.
[Is] ISSN:1095-6433
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Histamine and 2-methyl histamine caused dose-dependent aggregation of the integumental melanophores of Rana tigerina both in vitro and in vivo. The aggregating effects were antagonised by mepyramine and metiamide, specific H1 and H2 receptor blockers, respectively. Compound 48/80 and EDTA augmented the melanin-aggregating effects of exogenously applied histamine and 2-methyl histamine in in vivo experiments. 4-Methyl histamine, a specific H2 receptor agonist, dispersed the frog melanophores in in vitro studies, the dispersing effects were blocked by metiamide.
[Mh] Termos MeSH primário: Melanóforos/metabolismo
Ranidae/metabolismo
Receptores Histamínicos/metabolismo
Pele/metabolismo
[Mh] Termos MeSH secundário: Animais
Ácido Edético/farmacologia
Histamina/farmacologia
Antagonistas dos Receptores Histamínicos H1/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Técnicas In Vitro
Melaninas/metabolismo
Melanóforos/efeitos dos fármacos
Metilistaminas/farmacologia
Metiamida/farmacologia
Pirilamina/farmacologia
Ranidae/anatomia & histologia
Receptores Histamínicos/efeitos dos fármacos
Pele/efeitos dos fármacos
Pigmentação da Pele/efeitos dos fármacos
Pigmentação da Pele/fisiologia
p-Metoxi-N-metilfenetilamina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine H1 Antagonists); 0 (Histamine H2 Antagonists); 0 (Melanins); 0 (Methylhistamines); 0 (Receptors, Histamine); 3K7670861M (Metiamide); 4091-50-3 (p-Methoxy-N-methylphenethylamine); 54ST71P9EE (4-methylhistamine); 820484N8I3 (Histamine); 9G34HU7RV0 (Edetic Acid); H5DHG2WBHM (2-methylhistamine); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:9903
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:990211
[St] Status:MEDLINE


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[PMID]:9092167
[Au] Autor:Aslanian GG
[Ad] Endereço:NII of Pediatrics and Pediatric Surgery MZ RF, Moscow.
[Ti] Título:[Age differences in topic concentrations and activity of H2- and B2-receptors in the larynx and trachea].
[Ti] Título:Vozrastnye razlichiia topicheskoi kontsentratsii i aktivnosti H2- i B2-retseptorov v gortani i trakhee..
[So] Source:Vestn Otorinolaringol;(1):36-9, 1997.
[Is] ISSN:0042-4668
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:H2- and B2-receptors concentrations and activity were measured in 12 adult (6-7-month-old) and 12 young (1.5-2-month-old) rabbits by vascular reactions to histamine and bradykinin with and without prior usage of relevant specific receptor blocker. The findings suggest that concentration and activity of H2- and B2-receptors in young animals are the highest in the larynx. In mature animals-partially in trachea. With aging these concentrations and activity diminish in the larynx and rise in the trachea, the changes of B2-receptors are more significant.
[Mh] Termos MeSH primário: Envelhecimento/metabolismo
Laringe/metabolismo
Receptores da Bradicinina/metabolismo
Receptores Histamínicos H2/metabolismo
Traqueia/metabolismo
[Mh] Termos MeSH secundário: Fatores Etários
Animais
Antagonistas dos Receptores da Bradicinina
Antagonistas dos Receptores Histamínicos H2/farmacologia
Hipolipemiantes/farmacologia
Laringe/irrigação sanguínea
Laringe/efeitos dos fármacos
Metiamida/farmacologia
Microcirculação/efeitos dos fármacos
Microcirculação/fisiologia
Piridinolcarbamato/farmacologia
Coelhos
Receptores Histamínicos H2/efeitos dos fármacos
Traqueia/irrigação sanguínea
Traqueia/efeitos dos fármacos
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bradykinin Receptor Antagonists); 0 (Histamine H2 Antagonists); 0 (Hypolipidemic Agents); 0 (Receptors, Bradykinin); 0 (Receptors, Histamine H2); 3K7670861M (Metiamide); 81R511UV73 (Pyridinolcarbamate)
[Em] Mês de entrada:9704
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:970101
[St] Status:MEDLINE


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[PMID]:9063075
[Au] Autor:Peter J; Ali AS; Ali SA
[Ad] Endereço:PG Zoology Department, Saifia Postgraduate College of Science and Education, Bhopal, India.
[Ti] Título:Effect of histaminergic drugs on integumental melanophores of adult Bufo melanostictus.
[So] Source:Indian J Exp Biol;34(5):427-30, 1996 May.
[Is] ISSN:0019-5189
[Cp] País de publicação:India
[La] Idioma:eng
[Ab] Resumo:Histamine and 2-methyl histamine caused dose-dependent aggregation of melanophores in toad B. melanostictus. The effects were effectively antagonised by mepyramine, a specific H1 histamine receptor antagonist, and metiamide a specific H2 receptor antagonist. On the other, hand 4-methyl histamine, a specific H2 receptor agonist dispersed the melanophores. The results suggest that adult Bufo melanophores have H1 histamine receptors which mediate melanophore aggregation, however, dispersion of melanophores may be controlled by undifferentiated histamine receptors of H2 type.
[Mh] Termos MeSH primário: Histamínicos/farmacologia
Melanóforos/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Bufonidae
Agregação Celular/efeitos dos fármacos
Histamina/farmacologia
Técnicas In Vitro
Melanóforos/metabolismo
Metilistaminas/farmacologia
Metiamida/farmacologia
Pirilamina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine Agents); 0 (Methylhistamines); 3K7670861M (Metiamide); 54ST71P9EE (4-methylhistamine); 820484N8I3 (Histamine); H5DHG2WBHM (2-methylhistamine); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:9704
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:960501
[St] Status:MEDLINE


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[PMID]:8723539
[Au] Autor:Krstic MK; Stepanovic R; Ilic K; Krstic SK
[Ad] Endereço:Faculty of Medicine, Department of Pharmacology, Belgrade, Yugoslavia.
[Ti] Título:Endothelium-independent contractile and relaxant responses to histamine in the rabbit aorta and common carotid, mesenteric, renal, and femoral arteries.
[So] Source:Gen Pharmacol;27(3):529-33, 1996 Apr.
[Is] ISSN:0306-3623
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:1. The role of the vascular endothelium in the relaxant and contractile responses to histamine of the isolated rabbit aorta; common carotid, mesenteric, renal, and femoral arteries; as well as receptor types mediating these responses were analyzed. 2. Histamine (10(-8) to 10(-4) mol/l) contracted resting rings and caused a further concentration-dependent contraction of rings of the arteries precontracted by phenylephrine. 3. Pyrilamine abolished the contractile response to histamine in resting rings of the arteries, whereas it reversed that response into a concentration-dependent relaxant response in precontracted rings of the arteries. The relaxant effect of histamine was abolished by metiamide, but it was not affected by sotalol and atropine. Moreover, in control experiments, the phenylephrine-induced contractions and acetylcholine-induced relaxations were not changed by pyrilamine and metiamide, respectively. 4. Endothelial removal did not influence the contractile and relaxant responses of the arteries to histamine. 5. These findings indicate that, in the isolated rabbit aorta and common carotid, mesenteric, renal, and femoral arteries, the contractile effect of histamine resulting from the activation of H1 receptors overcomes its relaxant effect resulting from the activation of H2 receptors. The effects of histamine are neither mediated nor modulated by the endothelial cells.
[Mh] Termos MeSH primário: Artérias/efeitos dos fármacos
Endotélio Vascular/fisiologia
Histamina/farmacologia
Músculo Liso Vascular/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Feminino
Antagonistas dos Receptores Histamínicos H1/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Técnicas In Vitro
Masculino
Metiamida/farmacologia
Contração Muscular/efeitos dos fármacos
Relaxamento Muscular/efeitos dos fármacos
Pirilamina/farmacologia
Coelhos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine H1 Antagonists); 0 (Histamine H2 Antagonists); 3K7670861M (Metiamide); 820484N8I3 (Histamine); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:9702
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:960401
[St] Status:MEDLINE


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Fotocópia
[PMID]:7732870
[Au] Autor:Jonsson EW; Dahlén SE
[Ad] Endereço:Department of Physiology & Pharmacology, Karolinska Institutet, Stockholm, Sweden.
[Ti] Título:Leukotrienes and other mediators of the Schultz-Dale reaction in guinea-pig lung parenchyma.
[So] Source:Adv Prostaglandin Thromboxane Leukot Res;23:353-5, 1995.
[Is] ISSN:0732-8141
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Inflamação/fisiopatologia
Leucotrienos/metabolismo
Pulmão/fisiopatologia
[Mh] Termos MeSH secundário: Animais
Cobaias
Leucotrieno B4/antagonistas & inibidores
Pulmão/efeitos dos fármacos
Pulmão/imunologia
Masculino
Metiamida/farmacologia
Ovalbumina/imunologia
Pirilamina/farmacologia
Quinolinas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Leukotrienes); 0 (Quinolines); 128253-31-6 (2-(4-(quinolin-2-yl-methoxy)phenyl)-2-cyclopentylacetic acid); 1HGW4DR56D (Leukotriene B4); 3K7670861M (Metiamide); 9006-59-1 (Ovalbumin); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:9505
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:950101
[St] Status:MEDLINE



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