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[PMID]:12591110
[Au] Autor:Amobi N; Guillebaud J; Kaisary A; Lloyd-Davies RW; Turner E; Smith IC
[Ad] Endereço:GKT School of Biomedical Sciences, King's College, Guy's Campus, London SE1 1UL, UK.
[Ti] Título:Contractile actions of imidazoline alpha-adrenoceptor agonists and effects of noncompetitive alpha1-adrenoceptor antagonists in human vas deferens.
[So] Source:Eur J Pharmacol;462(1-3):169-77, 2003 Feb 21.
[Is] ISSN:0014-2999
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The contractile actions of imidazoline alpha-adrenoceptor agonists were investigated in human vas deferens longitudinal and circular muscle. The effects of phenoxybenzamine were studied in comparison to dibenamine and SZL-49 (4-amino-6,7-dimethoxy-2-quinazolinyl-4-(2-bicyclo[2,2,2]octa-2,5-dienylcarbonyl-2-piperazine), an alkylating prazosin analogue that discriminates between alpha(1H)- and alpha(1L)-adrenoceptor subtypes. The imidazoline alpha-adrenoceptor agonist, A-61603 (N-[5-(4,5-dihydro-1H-imidazol-2yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide hydrobromide), was a potent agonist (pD(2); longitudinal muscle 6.9, circular muscle 6.4) and cirazoline a partial agonist (pD(2); longitudinal muscle 6.1, circular muscle 5.1). Oxymetazoline was less effective, indanidine and clonidine were ineffective. SZL-49 produced a differential inhibition of contractions evoked by A-61603 in circular (alpha(1H)) compared to longitudinal (alpha(1L)) muscle and phenoxybenzamine had the opposite effect. Dibenamine inhibited the contractions comparably in both muscle types and analyses of its partial alkylation of receptors yielded identical estimates of equilibrium dissociation constant (pK(d)) for A-61603 in longitudinal (5.82) and circular (5.84) muscle. Receptor occupancy-response relationships revealed that whilst the muscle types are not different in receptor reserves for A-61603, contraction to the potent imidazoline is more efficiently coupled in longitudinal than in circular muscle. This underlies the markedly different responsiveness of the muscle types to cirazoline or oxymetazoline (alpha-adrenoceptor agonists with lower efficacies relative to A-61603). The differential inhibitory actions of phenoxybenzamine and SZL-49 are discussed.
[Mh] Termos MeSH primário: Agonistas alfa-Adrenérgicos/farmacologia
Antagonistas Adrenérgicos alfa/farmacologia
Imidazóis/farmacologia
Contração Muscular/efeitos dos fármacos
Prazosina/análogos & derivados
Tetra-Hidronaftalenos/farmacologia
Ducto Deferente/efeitos dos fármacos
[Mh] Termos MeSH secundário: Dibenzilcloretamina/farmacologia
Relação Dose-Resposta a Droga
Seres Humanos
Masculino
Norepinefrina/farmacologia
Oximetazolina/farmacologia
Fenoxibenzamina/farmacologia
Prazosina/farmacologia
Receptores Adrenérgicos alfa 1/efeitos dos fármacos
Ducto Deferente/fisiologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (A 61603); 0 (Adrenergic alpha-Agonists); 0 (Adrenergic alpha-Antagonists); 0 (Imidazoles); 0 (Receptors, Adrenergic, alpha-1); 0 (Tetrahydronaphthalenes); 0TTZ664R7Z (Phenoxybenzamine); 107021-36-3 (SZL 49); 43EXU2S56H (Dibenzylchlorethamine); 8VLN5B44ZY (Oxymetazoline); QK318GVY3Y (cirazoline); X4W3ENH1CV (Norepinephrine); XM03YJ541D (Prazosin)
[Em] Mês de entrada:0307
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:030220
[St] Status:MEDLINE


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[PMID]:11976277
[Au] Autor:Amobi NI; Guillebaud J; Kaisary AV; Turner E; Smith IC
[Ad] Endereço:GKT School of Biomedical Sciences, King's College London, Guy's Campus, London SE1 1UL, UK.
[Ti] Título:Discrimination by SZL49 between contractions evoked by noradrenaline in longitudinal and circular muscle of human vas deferens.
[So] Source:Br J Pharmacol;136(1):127-35, 2002 May.
[Is] ISSN:0007-1188
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The effects of irreversible alpha1-adrenoceptor antagonists, SZL-49 (an alkylating analogue of prazosin), dibenamine and benextramine on contractions to noradrenaline (NA) in longitudinal and circular muscle of human epididymal vas deferens were investigated. Competitive alpha1-adrenoceptor antagonists were also used to further characterize the alpha1-adrenoceptor subtype stimulated by NA in longitudinal and circular muscle. NA evoked concentration-dependent contractions of both muscle types (pD2; 5.4 and 5.2 respectively). The contraction of circular muscle was comparatively more sensitive than that of longitudinal muscle to pretreatment with SZL-49. In contrast, dibenamine or benextramine produced comparable effects in both muscle types. The relationship between receptor occupancy and contraction in either longitudinal or circular muscle was nonlinear, with half-maximal response requiring similar receptor occupancy (longitudinal muscle 14%, circular muscle 16%). Maximal response in both muscle types occurred with little or no receptor reserve (<10%). The competitive alpha1-adrenoceptor antagonists produced dextral shifts of the dose-response curves to NA in longitudinal and circular muscle. The inhibitory potencies, estimated from the apparent pKB values were significantly different in longitudinal and circular muscle respectively for either WB 4101 (pKB, 8.6 and 9.5) or RS-17053 (pKB, 7.1 and 9.0) but not for Rec 15/2739 (pKB, 9.2 and 9.8) or HV 723 (pKB, 8.3 and 8.4). In conclusion, the potency profile of the competitive alpha1-adrenoceptor antagonists and the lack of different receptor reserves for NA in the muscle types suggest that the discriminatory effects of SZL-49 is primarily due to a predominance of the alpha1L-adrenoceptor subtype in longitudinal muscle and alpha1A-subtype in circular muscle.
[Mh] Termos MeSH primário: Cistamina/análogos & derivados
Músculo Liso/efeitos dos fármacos
Norepinefrina/farmacologia
Prazosina/análogos & derivados
Prazosina/farmacologia
Receptores Adrenérgicos alfa 1/efeitos dos fármacos
Ducto Deferente/efeitos dos fármacos
Vasoconstritores/farmacologia
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos alfa/farmacologia
Cistamina/farmacologia
Dibenzilcloretamina/farmacologia
Seres Humanos
Técnicas In Vitro
Masculino
Contração Muscular/efeitos dos fármacos
Músculo Liso/anatomia & histologia
Músculo Liso/fisiologia
Ducto Deferente/fisiologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic alpha-Antagonists); 0 (Receptors, Adrenergic, alpha-1); 0 (Vasoconstrictor Agents); 107021-36-3 (SZL 49); 43EXU2S56H (Dibenzylchlorethamine); 69790-18-7 (benextramine); R110LV8L02 (Cystamine); X4W3ENH1CV (Norepinephrine); XM03YJ541D (Prazosin)
[Em] Mês de entrada:0208
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:020427
[St] Status:MEDLINE


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[PMID]:10420098
[Au] Autor:Arnold OH
[Ad] Endereço:Universitäts-Klinik für Psychiatrie, Wien, Osterreich.
[Ti] Título:Schizophrenia - A disturbance of signal interaction between the entorhinal cortex and the dentate gyrus? The contribution of experimental dibenamine psychosis to the pathogenesis of schizophrenia: A hypothesis.
[So] Source:Neuropsychobiology;40(1):21-32, 1999.
[Is] ISSN:0302-282X
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:In addition to the existence of complex memory (similar to the implicit nondeclarative memory of Squire), the existence of a phylogenetically old apparatus of a memory of situations (SMA) is supposed, which is to some extent comparable with the declarative memory of Squire. During actual sensory information the SMA generates a general frame and forms a general 'mark', indicating whether a given information has its origin inside or outside the body, and whether it is new or known. The procedure of this marking process can be explained as the time-depending arrest of a copy of the actual original information-transporting signal 'shower'; this copy must last until the feedback from thalamocortical centers indicates the termination of the processing of the original signal showers. The arrest of the shower copies is the performance of neuronal networks of the entorhinal cortex (EC) and the gyrus dentatus (GD). The psychopathological and biochemical analyses of experimental dibenamine psychosis show a different effect of dibenamine on the noradrenaline (NA) receptors of the EC and GD, respectively: these effects are responsible for the repeated perception cycles of a single situation. N,N-Dibencylamine blocks the postsynaptic alpha(1)-receptors of the EC without influencing the beta-receptors of the GD. Thus the interaction between EC and GD is changed: instead of new scenes, perceptions that have just been experienced get repeated presence and the quality of familiarity. The prolonged arrest of shower copies simultaneously blocks the entrance of new signal showers from the EC to the GD. No information-transporting signal showers can come in as long as the arrest lasts. In case of a disturbance in NA-dependent actions within the EC and the GD, the duration of arrest of information-transporting signal showers is shortened. Thus the formal frame of experience receives the quality of novelty instead of familiarity, and in addition the qualities of uncertainty, vagueness, and alienity. These very changes in perception and experience represent the basic disturbance of schizophrenia. All the symptoms of schizophrenia may be explained by this basic disturbance. The analysis of biochemical aspects turns attention to the energetic situation of NA and N-methyl-D-aspartate systems. These considerations suggest a genetic background of the basic disturbance of schizophrenia: transmitter effects on membranes of neurons and possibly also on glial cells, and energy supply of these effects may be predetermined genetically. It may be assumed that the compensation of such membrane-dependent disturbances will be possible within wide areas of the neural network, except for the 'bottleneck' of the overlapping region of the iso- and allocortex.
[Mh] Termos MeSH primário: Giro Denteado/fisiopatologia
Córtex Entorrinal/fisiopatologia
Memória/efeitos dos fármacos
Psicoses Induzidas por Substâncias/fisiopatologia
Esquizofrenia/fisiopatologia
[Mh] Termos MeSH secundário: Adulto
Giro Denteado/efeitos dos fármacos
Dibenzilcloretamina
Córtex Entorrinal/efeitos dos fármacos
Predisposição Genética para Doença/patologia
Alucinações/induzido quimicamente
Alucinações/patologia
Alucinações/fisiopatologia
Seres Humanos
Masculino
Rede Nervosa/efeitos dos fármacos
Rede Nervosa/patologia
Rede Nervosa/fisiopatologia
Psicoses Induzidas por Substâncias/etiologia
Psicoses Induzidas por Substâncias/psicologia
Psicologia do Esquizofrênico
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
43EXU2S56H (Dibenzylchlorethamine)
[Em] Mês de entrada:9908
[Cu] Atualização por classe:171101
[Lr] Data última revisão:
171101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:990727
[St] Status:MEDLINE


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[PMID]:9512003
[Au] Autor:Smriga M; Nishiyama N; Saito H
[Ad] Endereço:Laboratory of Chemical Pharmacology, Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan.
[Ti] Título:Mineralocorticoid receptor-mediated enhancement of neuronal excitability and synaptic plasticity in the dentate gyrus in vivo is dependent on the beta-adrenergic activity.
[So] Source:J Neurosci Res;51(5):593-601, 1998 Mar 01.
[Is] ISSN:0360-4012
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The dentate gyrus neurons in the hippocampus contain a high density of both mineralocorticoid and adrenergic receptors. By in vivo extracellular recording from adrenalectomized rats we investigated the possible relationships between the two systems with regard to neuronal excitability and activity-dependent synaptic plasticity. Pretreatment with aldosterone significantly enhanced both basal neuronal excitability and tetanically evoked synaptic plasticity in adrenalectomized, but not sham-operated rats. The enhancement was blocked by spironolactone, indicating a mineralocorticoid receptor-dependent effect. The adrenomedullary hormone epinephrine also significantly enhanced synaptic plasticity via activation of beta-adrenergic receptors. Beta-adrenergic antagonist propranolol, infused directly into the dentate gyrus granule cell layer, significantly reduced the effect of aldosterone on neuronal excitability and partly canceled the aldosterone-enhanced synaptic plasticity. No effect of propranolol was found after its amygdaloid infusion. The mineralocorticoid receptor antagonist spironolactone did not affect the epinephrine-induced effects. These results indicate that the pretreated adrenal steroids interact with the catecholaminergic system in the dentate gyrus of adrenalectomized rats and that the functional beta-adrenergic pathway is involved in the mechanism of mineralocorticoid-induced cellular effects in vivo.
[Mh] Termos MeSH primário: Giro Denteado/química
Plasticidade Neuronal/fisiologia
Neurônios/química
Receptores Adrenérgicos beta/metabolismo
Receptores de Mineralocorticoides/metabolismo
[Mh] Termos MeSH secundário: Adrenalectomia
Antagonistas Adrenérgicos alfa/farmacologia
Agonistas Adrenérgicos beta/farmacologia
Antagonistas Adrenérgicos beta/farmacologia
Aldosterona/farmacologia
Animais
Giro Denteado/fisiologia
Dibenzilcloretamina/farmacologia
Epinefrina/farmacologia
Potenciais Evocados/efeitos dos fármacos
Masculino
Antagonistas de Receptores de Mineralocorticoides/farmacologia
Neurônios/efeitos dos fármacos
Neurônios/fisiologia
Propranolol/farmacologia
Ratos
Ratos Wistar
Espironolactona/farmacologia
Estimulação Química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic alpha-Antagonists); 0 (Adrenergic beta-Agonists); 0 (Adrenergic beta-Antagonists); 0 (Mineralocorticoid Receptor Antagonists); 0 (Receptors, Adrenergic, beta); 0 (Receptors, Mineralocorticoid); 27O7W4T232 (Spironolactone); 43EXU2S56H (Dibenzylchlorethamine); 4964P6T9RB (Aldosterone); 9Y8NXQ24VQ (Propranolol); YKH834O4BH (Epinephrine)
[Em] Mês de entrada:9804
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:980325
[St] Status:MEDLINE


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[PMID]:8902547
[Au] Autor:Sliwinski W; Korolkiewicz R; Rekowski P; Halama A; Korolkiewicz KZ
[Ad] Endereço:Department of Pharmacology, Medical University of Gdansk, Gdansk-Wrzeszcz, Poland.
[Ti] Título:Actions of galanin and some of its analogues on rat isolated gastric fundus.
[So] Source:Fundam Clin Pharmacol;10(5):442-9, 1996.
[Is] ISSN:0767-3981
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The study was undertaken to characterize the effects of porcine galanin (pGal) and some of its analogues on rat gastric fundus muscle strips. pGal, galantide (M15) and pGal(1-14)-[Abu8]SCY-I evoked reproducible concentration-dependent contractions in concentrations of 1-300, 3-1,000 and 100-3,000 nM, respectively, with EC50 values of 13, 70 and 187 nM. Hill's coefficient for pGal is 1.03, indicating an interaction of one pGal molecule with one receptor, fulfilling criteria of classical receptor theory. For M15 and pGal(1-14)-[Abu8]SCY-I, Hill's coefficients are significantly different from 1, namely 0.73 and 1.56, so that one drug molecule may not interact with one receptor. The stimulatory effects of pGal were not modified by dibenamine 10 microM or glybenclamide 1 or 10 microM. Diltiazem 0.1, 1 and 10 microM, papaverine 0.1, 10 microM or dibutyryl cAMP (dib cAMP) 100 and 300 microM, blocked the contraction to pGal in a concentration-dependent manner, indicating an important role for the influx of extracellular calcium ions and regulation by cAMP the pGal-evoked contraction. Diltiazem, dibutyryl cAMP and papaverine were not competitive antagonists of pGal in the stomach smooth muscle.
[Mh] Termos MeSH primário: Galanina/farmacologia
Fundo Gástrico/efeitos dos fármacos
Músculo Liso/efeitos dos fármacos
[Mh] Termos MeSH secundário: Análise de Variância
Animais
Bucladesina/farmacologia
Bloqueadores dos Canais de Cálcio/farmacologia
Dibenzilcloretamina/farmacologia
Diltiazem/farmacologia
Dimetil Sulfóxido/farmacologia
Relação Dose-Resposta a Droga
Feminino
Galanina/análogos & derivados
Fundo Gástrico/metabolismo
Glibureto/farmacologia
Dose Letal Mediana
Masculino
Contração Muscular/efeitos dos fármacos
Papaverina/farmacologia
Parassimpatolíticos/farmacologia
Ratos
Ratos Wistar
Substância P/análogos & derivados
Substância P/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Calcium Channel Blockers); 0 (Parasympatholytics); 0 (galanin(1-14)-(aminobutyrate)SCY-I); 138579-66-5 (galantide); 33507-63-0 (Substance P); 43EXU2S56H (Dibenzylchlorethamine); 63X7MBT2LQ (Bucladesine); 88813-36-9 (Galanin); DAA13NKG2Q (Papaverine); EE92BBP03H (Diltiazem); SX6K58TVWC (Glyburide); YOW8V9698H (Dimethyl Sulfoxide)
[Em] Mês de entrada:9702
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:960101
[St] Status:MEDLINE


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[PMID]:8823669
[Au] Autor:Zernig G; Issaevitch T; Woods JH
[Ad] Endereço:Department of Pharmacology, University of Michigan, Ann Arbor, USA.
[Ti] Título:Calculation of agonist efficacy, apparent affinity, and receptor population changes after administration of insurmountable antagonists: comparison of different analytical approaches.
[So] Source:J Pharmacol Toxicol Methods;35(4):223-37, 1996 Aug.
[Is] ISSN:1056-8719
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The determination of the affinity and efficacy of an agonist in functional (as opposed to radioligand binding) experiments is necessary to explain its potency. Using modeled dose-response data both in their ideal form and with an added average deviation as well as previously published experimental data, a variety of analytical approaches were compared which differed in goodness-of-fit, ease of handling, and range of successful application. A nonlinear curve-fitting algorithm that analyzed several dose-response curves simultaneously and fitted them to an extended version of the operational model of Black and Leff (1983) (Proc R Soc Lond B 220:141-162) was demonstrated to be superior to the other approaches using the above criteria. However, judging from the limitations of the analytical approaches, claims of efficacy or affinity differences between agonists that are based on less than 10-fold numerical differences in the same behavioral paradigm should be viewed with skepticism. It was also found that simple inspection of dose-response curves obtained before and after administration of an insurmountable antagonist give estimates of fair accuracy under most circumstances.
[Mh] Termos MeSH primário: Receptores de Droga/agonistas
Receptores de Droga/antagonistas & inibidores
[Mh] Termos MeSH secundário: Agonistas alfa-Adrenérgicos/farmacologia
Antagonistas Adrenérgicos beta/farmacologia
Algoritmos
Animais
Aorta Torácica/efeitos dos fármacos
Dibenzilcloretamina/farmacologia
Relação Dose-Resposta a Droga
Técnicas In Vitro
Cinética
Modelos Biológicos
Modelos Estatísticos
Contração Muscular/efeitos dos fármacos
Músculo Liso/efeitos dos fármacos
Músculo Liso/metabolismo
Norepinefrina/farmacologia
Coelhos
Receptores Adrenérgicos/metabolismo
Receptores de Droga/metabolismo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Adrenergic alpha-Agonists); 0 (Adrenergic beta-Antagonists); 0 (Receptors, Adrenergic); 0 (Receptors, Drug); 43EXU2S56H (Dibenzylchlorethamine); X4W3ENH1CV (Norepinephrine)
[Em] Mês de entrada:9612
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:960801
[St] Status:MEDLINE


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[PMID]:8050463
[Au] Autor:Jovanovic A; Grbovic L; Tulic I
[Ad] Endereço:Department of Pharmacology, University Medical Center, Medical Faculty, Belgrade, Yugoslavia.
[Ti] Título:Endothelium-dependent relaxation in response to acetylcholine in the human uterine artery.
[So] Source:Eur J Pharmacol;256(2):131-9, 1994 Apr 21.
[Is] ISSN:0014-2999
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The effect of acetylcholine on isolated human uterine artery rings was investigated. Acetylcholine induced concentration and endothelium-dependent relaxation (pD2 = 7.29 +/- 0.03) of the precontracted arterial segments. The dissociation constant (KA) for acetylcholine was 1.35 (0.92-1.77) mumol/l. The occupancy-response relationship was non-linear. Half-maximal response to acetylcholine was obtained with 5.25% receptor occupancy. Muscarinic receptor antagonists: atropine, pirenzepine, methoctramine, p-fluoro-hexahydro-sila-diphenidol (pFHHSiD) and 4-diphenyl-acetoxy-N-methyl-piperidine (4-DAMP) competitively antagonized the response to acetylcholine. The constrained pA2 values were 9.32 +/- 0.03, 7.13 +/- 0.01, 6.26 +/- 0.01, 8.17 +/- 0.01 and 9.13 +/- 0.02, respectively. A selective muscarinic M2 receptor antagonist, gallamine, had no effect on acetylcholine-induced relaxation. It is concluded that in human uterine arteries acetylcholine induces endothelium-dependent relaxation and acts as a full agonist. We suggest that the muscarinic receptors involved in the acetylcholine-induced relaxation of the isolated human uterine artery are predominantly of the M3 subtype.
[Mh] Termos MeSH primário: Acetilcolina/farmacologia
Endotélio Vascular/fisiologia
Músculo Liso Vascular/fisiologia
[Mh] Termos MeSH secundário: Acetilcolina/antagonistas & inibidores
Acetilcolina/metabolismo
Adulto
Artérias/efeitos dos fármacos
Dibenzilcloretamina/farmacologia
Feminino
Seres Humanos
Técnicas In Vitro
Meia-Idade
Antagonistas Muscarínicos
Relaxamento Muscular/efeitos dos fármacos
Músculo Liso Vascular/efeitos dos fármacos
Papaverina/farmacologia
Receptores Muscarínicos/efeitos dos fármacos
Receptores Muscarínicos/metabolismo
Fluxo Sanguíneo Regional/efeitos dos fármacos
Útero/irrigação sanguínea
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Muscarinic Antagonists); 0 (Receptors, Muscarinic); 43EXU2S56H (Dibenzylchlorethamine); DAA13NKG2Q (Papaverine); N9YNS0M02X (Acetylcholine)
[Em] Mês de entrada:9409
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:940421
[St] Status:MEDLINE


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[PMID]:8395286
[Au] Autor:Wiener HL; Thalody GP; Maayani S
[Ad] Endereço:Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, St. John's University, Jamaica, New York 11439.
[Ti] Título:Interactions between responses mediated by activation of adenosine A2 receptors and alpha 1-adrenoceptors in the rabbit isolated aorta.
[So] Source:Br J Pharmacol;109(2):394-404, 1993 Jun.
[Is] ISSN:0007-1188
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:1. This paper describes aspects of the functional antagonism between the responses mediated by activated alpha 1-adrenoceptors and adenosine A2 receptors in the adventitia- and endothelium-denuded aorta of the rabbit. 2. Adenosine A2 receptor agonists relaxed aortic rings pre-contracted with phenylephrine. The relaxation response was agonist concentration-dependent and saturable. The respective contractile and relaxation responses were stable, reproducible, and reversible. 3. Increasing the phenylephrine concentration caused a progressive attenuation of the action of adenosine A2 receptor agonists, consisting of a decreased maximal response and a dextral shift of the adenosine agonist concentration-response curve. This functional antagonism could be completely reversed upon removal of adenosine by either the addition of adenosine deaminase or by wash-out of the adenosine agonist from the tissue. The relaxation response to the adenosine A2 receptor partial agonists, N6-cyclohexyladenosine and R-(-)-N6-(2-phenylisopropyl)adenosine, was abolished at higher phenylephrine concentrations (e.g. 30 EC50). 4. A 1000 fold increase in the adenosine concentration was required to shift the value of the EC50 of phenylephrine six fold, while a similar increase in the value of the EC50 of adenosine could be elicited by only a 32 fold increase in the phenylephrine concentration. A 30 fold increase in the phenylephrine concentration shifted the value of the EC50 of 5'-N-ethylcarboxamidoadenosine four fold. 5. Analysis of the functional antagonism between the responses mediated by these receptors using the Black & Leff (1983) operational model of agonism allowed for the estimation of the agonist dissociation constant, KA, and the apparent efficacy, tau, for both phenylephrine and adenosine A2 receptor agonists. Increasing the concentration of phenylephrine reduced the value of tau for adenosine agonists in a concentration-dependent and saturable manner. Similarly, increasing the concentration of adenosine reduced the value of tau for phenylephrine in a concentration-dependent and saturable manner. The phenylephrine KA value obtained by the method of functional antagonism (1.9 microM) was similar to that obtained by the receptor inactivation method (2.1 microM). 6. Partial occlusion of the alpha 1-adrenoceptor by the alkylating agent, dibenamine, demonstrated that the magnitude of the adenosine A2 receptor-mediated relaxation was inversely proportional to the number of functional alpha 1-adrenoceptors. 7. It is concluded that the magnitude of functional antagonism is proportional to the stimulus elicited through either receptor. We propose that this tissue preparation and pair of receptors is a good model to study quantitative aspects of functional antagonism between activated receptors.
[Mh] Termos MeSH primário: Músculo Liso Vascular/metabolismo
Receptores Adrenérgicos alfa/metabolismo
Receptores Purinérgicos/metabolismo
[Mh] Termos MeSH secundário: Adenosina/análogos & derivados
Adenosina/farmacologia
Adenosina-5'-(N-etilcarboxamida)
Animais
Aorta Torácica/efeitos dos fármacos
Dibenzilcloretamina/farmacologia
Endotélio Vascular/fisiologia
Técnicas In Vitro
Indicadores e Reagentes
Masculino
Contração Muscular/efeitos dos fármacos
Músculo Liso Vascular/efeitos dos fármacos
Fenilefrina/farmacologia
Capuzes de RNA/farmacologia
Coelhos
Receptores Adrenérgicos alfa/efeitos dos fármacos
Receptores Purinérgicos/efeitos dos fármacos
Vasodilatadores/farmacologia
[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 (Indicators and Reagents); 0 (RNA Caps); 0 (Receptors, Adrenergic, alpha); 0 (Receptors, Purinergic); 0 (Vasodilator Agents); 1867-73-8 (N(6)-methyladenosine); 1WS297W6MV (Phenylephrine); 35920-39-9 (Adenosine-5'-(N-ethylcarboxamide)); 36396-99-3 (N(6)-cyclohexyladenosine); 43EXU2S56H (Dibenzylchlorethamine); K72T3FS567 (Adenosine)
[Em] Mês de entrada:9309
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:930601
[St] Status:MEDLINE


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[PMID]:1409536
[Au] Autor:Lee HH; Terada M
[Ad] Endereço:Department of Parasitology, Hamamatsu University School of Medicine, Japan.
[Ti] Título:In vitro effects of milbemycin oxime: mechanism of action against Angiostrongylus cantonensis and Dirofilaria immitis.
[So] Source:Parasitol Res;78(4):349-53, 1992.
[Is] ISSN:0932-0113
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The neuropharmacological mechanisms underlying the action of milbemycin oxime on the motility of Angiostrongylus cantonensis and Dirofilaria immitis were examined in vitro. In A. cantonensis, milbemycin oxime caused inhibitory effects at low concentrations of > or = 10(-9) g/ml, and paralysis was elicited at 10(-8) - 10(-6) g/ml. The paralysis was antagonized by picrotoxin and bicuculline but not by dibenamine. In addition, stimulatory effects were observed when the antibiotic was used at higher concentrations of 3-5 x 10(-6) g/ml, and the action was antagonized by strychnine. Both effects were also observed in the preparation contracted by eserine or pyrantel. When D. immitis was treated with milbemycin oxime at concentrations of 10(-7) and 3-5 x 10(-6) g/ml, only slight inhibitory and stimulatory effects, respectively, were observed. These effects were partially antagonized by picrotoxin and strychnine, respectively. These results suggest that the inhibitory and stimulatory actions of milbemycin oxime are caused through gabergic and cholinergic mechanisms in A. cantonensis and D. immitis.
[Mh] Termos MeSH primário: Angiostrongylus/efeitos dos fármacos
Anti-Helmínticos/farmacologia
Antibacterianos/farmacologia
Dirofilaria immitis/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Anti-Helmínticos/antagonistas & inibidores
Antibacterianos/antagonistas & inibidores
Bicuculina/farmacologia
Dibenzilcloretamina/farmacologia
Cães
Feminino
Macrolídeos
Movimento/efeitos dos fármacos
Picrotoxina/farmacologia
Ratos
Estricnina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anthelmintics); 0 (Anti-Bacterial Agents); 0 (Macrolides); 124-87-8 (Picrotoxin); 43EXU2S56H (Dibenzylchlorethamine); 51570-36-6 (milbemycin); H9Y79VD43J (Strychnine); Y37615DVKC (Bicuculline)
[Em] Mês de entrada:9211
[Cu] Atualização por classe:170805
[Lr] Data última revisão:
170805
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:920101
[St] Status:MEDLINE


  10 / 421 MEDLINE  
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[PMID]:1847200
[Au] Autor:Christ GJ; Jean-Jacques M
[Ad] Endereço:Department of Urology, Albert Einstein College of Medicine, Bronx, New York.
[Ti] Título:Mutual-effect amplification of contractile responses elicited by simultaneous activation of alpha-1 adrenergic and 5-hydroxytryptamine2 receptors in isolated rat aorta.
[So] Source:J Pharmacol Exp Ther;256(2):553-61, 1991 Feb.
[Is] ISSN:0022-3565
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:5-Hydroxytryptamine (5-HT), and the selective alpha-1 agonists phenylephrine (PE) and oxymetazoline (OXY), were used to study the effects of simultaneous coactivation of the 5-HT2 and alpha-1 adrenergic receptors, respectively, on the contractile responses of isolated rat aortic rings. Dissociation constants (KA) were determined for each of the agonists at their respective receptor subtypes. The KA values for PE and OXY at the alpha-1 receptor were 316 nM and 1.82 microM, respectively, while the KA for 5-HT at the 5-HT2 receptor was 478 nM. Concentration-response curves for each agonist were analyzed by the Black and Leff operational model of pharmacological agonism to determine efficacy (tau) and slope factor values. The estimated tau for PE (16.02) was much greater than the tau for either OXY (4.15) or 5-HT (2.95), which had similar efficacies. Using a previously described drug concentration paradigm, a mutual-effect amplification of the 5-HT-induced contractile response was observed with mixtures of 5-HT and PE, whereas mixtures of OXY and 5-HT elicited a mutual-effect amplification of the observed response to OXY alone. In both cases, the theoretical concentration-response curve constructed using the Poch and Holzmann method of equiactive substitution demonstrated that mutual-effect amplification was largely the result of simple additivity of agonist effects. In addition, estimates of tau and slope factor determined from the Black and Leff equation were substituted into the Leff model of mutual-effect amplification and used to accurately predict the location of the concentration-response curves elicited by mixtures of 5-HT and PE, as well as mixtures of OXY and 5-HT. This represents the first time a mathematical model has been used to accurately predict the outcome of coactivation of the alpha-1 and 5-HT2 receptors.(ABSTRACT TRUNCATED AT 250 WORDS)
[Mh] Termos MeSH primário: Receptores Adrenérgicos alfa/efeitos dos fármacos
Receptores de Serotonina/efeitos dos fármacos
Vasoconstrição/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Aorta/efeitos dos fármacos
Dibenzilcloretamina/farmacologia
Relação Dose-Resposta a Droga
Técnicas In Vitro
Masculino
Oximetazolina/metabolismo
Oximetazolina/farmacologia
Fenilefrina/metabolismo
Fenilefrina/farmacologia
Ratos
Ratos Endogâmicos F344
Serotonina/farmacologia
Especificidade da Espécie
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Receptors, Adrenergic, alpha); 0 (Receptors, Serotonin); 1WS297W6MV (Phenylephrine); 333DO1RDJY (Serotonin); 43EXU2S56H (Dibenzylchlorethamine); 8VLN5B44ZY (Oxymetazoline)
[Em] Mês de entrada:9103
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:910201
[St] Status:MEDLINE



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