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Pesquisa : D02.886.904.200 [Categoria DeCS]
Referências encontradas : 169 [refinar]
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[PMID]:11714875
[Au] Autor:Wieland K; Bongers G; Yamamoto Y; Hashimoto T; Yamatodani A; Menge WM; Timmerman H; Lovenberg TW; Leurs R
[Ad] Endereço:Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Vrije Universiteit, Division of Chemistry, Amsterdam, The Netherlands.
[Ti] Título:Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
[So] Source:J Pharmacol Exp Ther;299(3):908-14, 2001 Dec.
[Is] ISSN:0022-3565
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Agonist-independent activity of G-protein-coupled receptor, also referred to as constitutive activity, is a well-documented phenomenon and has been reported recently for both the histamine H(1) and H(2) receptors. Using SK-N-MC cell lines stably expressing the human and rat H(3) receptors at physiological receptor densities (500-600 fmol/mg of protein), we show that both the rat and human H(3) receptors show a high degree of constitutive activity. The forskolin-mediated cAMP production in SK-N-MC cells is inhibited strongly upon expression of the G(i)-coupled H(3) receptor. The cAMP production can be further inhibited upon agonist stimulation of the H(3) receptor and can be enhanced by a variety of H(3) antagonists acting as inverse agonists at the H(3) receptor. Thioperamide, clobenpropit, and iodophenpropit raise the cAMP levels in SK-N-MC cells with potencies that match their receptor binding affinities. Surprisingly, impentamine and burimamide act as effective H(3) agonists. Modification of the amine group of impentamine dramatically affected the pharmacological activity of the ligand. Receptor affinity was reduced slightly for most impentamine analogs, but the functional activity of the ligands varied from agonist to neutral antagonist and inverse agonist, indicating that subtle changes in the chemical structures of impentamine analogs have major impact on the (de)activation steps of the H(3) receptor. In conclusion, upon stable expression of the rat and human H(3) receptor in SK-N-MC cells constitutive receptor activity is detected. In this experimental system, H(3) receptors ligands, previously identified as H(3) antagonists, cover the whole spectrum of pharmacological activities, ranging from full inverse agonists to agonists.
[Mh] Termos MeSH primário: Antagonistas dos Receptores Histamínicos/farmacologia
Receptores Histamínicos H3/biossíntese
Tioureia/análogos & derivados
[Mh] Termos MeSH secundário: Animais
Burimamida/farmacologia
AMP Cíclico/metabolismo
Seres Humanos
Imidazóis/farmacologia
Masculino
Ratos
Ratos Wistar
Receptores Histamínicos H3/efeitos dos fármacos
Receptores Histamínicos H3/metabolismo
Proteínas Recombinantes/efeitos dos fármacos
Proteínas Recombinantes/metabolismo
Tioureia/farmacologia
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine Antagonists); 0 (Imidazoles); 0 (Receptors, Histamine H3); 0 (Recombinant Proteins); 0 (impentamine); 677MJ4VPZC (imetit); E0399OZS9N (Cyclic AMP); GYV9AM2QAG (Thiourea); TN5A4OD2TV (Burimamide)
[Em] Mês de entrada:0112
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:011121
[St] Status:MEDLINE


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[PMID]:10911922
[Au] Autor:Hough LB; Nalwalk JW; Barnes WG; Leurs R; Menge WM; Timmerman H; Wentland M
[Ad] Endereço:Department of Pharmacology and Neuroscience, Albany Medical College, New York 12208, USA. houghl@mail.amc.edu
[Ti] Título:A third life for burimamide. Discovery and characterization of a novel class of non-opioid analgesics derived from histamine antagonists.
[So] Source:Ann N Y Acad Sci;909:25-40, 2000.
[Is] ISSN:0077-8923
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Burimamide, a histamine (HA) derivative with both H2- and H3-blocking properties, induces antinociception when injected into the rodent CNS. Several related compounds share this property, and structure-activity studies have shown that this new class of analgesics is distinct from known HA antagonists. The prototype, named improgan, shows a preclinical profile of a highly effective analgesic, with activity against thermal, mechanical and inflammatory nociception after doses that do not alter motor balance or locomotor activity. Improgen analgesia is not blocked by opioid antagonists and is observed in opioid receptor knock-out mice. Unlike morphine, improgan does not induce tolerance after daily dosing. Extensive in vitro pharmacology studies have excluded known histaminergic, opioid, serotonergic, GABAergic and adrenergic receptor mechanisms, as well as 50 other sites of action. The improgan-like analgesic activity of some HA congeners suggests an analgesic action on a novel HA receptor, but further studies are required to substantiate this. Studies in progress are characterizing the sites and mechanisms of action of improgan, and developing brain-penetrating derivatives that could be useful for clinical pain.
[Mh] Termos MeSH primário: Analgésicos não Entorpecentes/farmacologia
Burimamida/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
[Mh] Termos MeSH secundário: Animais
Seres Humanos
Camundongos
Receptores Histamínicos/efeitos dos fármacos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.; REVIEW
[Nm] Nome de substância:
0 (Analgesics, Non-Narcotic); 0 (Histamine H2 Antagonists); 0 (Receptors, Histamine); TN5A4OD2TV (Burimamide)
[Em] Mês de entrada:0008
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:000727
[St] Status:MEDLINE


  3 / 169 MEDLINE  
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[PMID]:10638637
[Au] Autor:Hough LB; Nalwalk JW; Leurs R; Menge WM; Timmerman H
[Ad] Endereço:Department of Pharmacology and Neuroscience, Albany Medical College, NY 12208, USA. houghl@mail.amc.edu
[Ti] Título:Antinociceptive activity of derivatives of improgran and burimamide.
[So] Source:Pharmacol Biochem Behav;65(1):61-6, 2000 Jan 01.
[Is] ISSN:0091-3057
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Improgan, a compound related to H2 and H3 antagonists, induces antinociception in rodents after intraventricular administration. Characteristics of improgan and its congeners include: (a) morphine-like antinociception on thermal and mechanical tests in two species; (b) no impairment of motor coordination or locomotor activity; (c) evidence for a novel, nonopioid mechanism that is independent of known histamine receptors; (d) lack of tolerance with daily dosing; and (e) unique structure-activity relationships (SARs). Presently, the antinociceptive activity of several new derivatives of improgan was investigated in rats. Among compounds similar to burimamide, VUF4577 (possessing a two-carbon side chain) and VUF4582 (an N-phenyl derivative of VUF4577) induced complete, dose- and time-dependent antinociception on the hot-plate and tail-flick tests with no behavioral side effects. These compounds (with ED50 values of 71-117 nmol) were approximately twice as potent as burimamide itself (a four-carbon derivative). Two other derivatives in which the thiourea group (C=S, known to cause human toxicity) was replaced by either nitroethene (C=CH-NO2, VUF5405) or urea (C=O, VUF5407) also showed effective, potent antinociception on both assays. The latter compound is the most potent improgan-like drug discovered to date (ED50 = 71 nmol). Furthermore, positional isomers of antinociceptive compounds either lacked activity (VUF5394) or induced toxicity (VUF5393), revealing a high degree of pharmacological specificity. Although the mechanism of improgan antinociception remains unknown, the present results show promise for the further development of safe, effective, and potent pain-relieving compounds.
[Mh] Termos MeSH primário: Analgésicos não Entorpecentes/farmacologia
Burimamida/farmacologia
Cimetidina/análogos & derivados
Antagonistas dos Receptores Histamínicos H2/farmacologia
Receptores Histamínicos H3/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Cimetidina/farmacologia
Relação Dose-Resposta a Droga
Masculino
Ratos
Ratos Sprague-Dawley
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Analgesics, Non-Narcotic); 0 (Histamine H2 Antagonists); 0 (Receptors, Histamine H3); 0 (SKF 92374); 80061L1WGD (Cimetidine); TN5A4OD2TV (Burimamide)
[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:000119
[St] Status:MEDLINE


  4 / 169 MEDLINE  
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[PMID]:10456436
[Au] Autor:West RE; Wu RL; Billah MM; Egan RW; Anthes JC
[Ad] Endereço:Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. robert.west@spcorp.com
[Ti] Título:The profiles of human and primate [3H]Nalpha-methylhistamine binding differ from that of rodents.
[So] Source:Eur J Pharmacol;377(2-3):233-9, 1999 Jul 21.
[Is] ISSN:0014-2999
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Characterization of the histamine H3 receptor in rodent species has been extensive but limited characterization has been done with primate or human tissue. We have characterized the binding of [3H]Nalpha-methylhistamine to cynomolgus monkey and human brain membranes to determine whether there are any significant differences among species' pharmacology. In monkey, [3H]Nalpha-methylhistamine bound, in a guanine nucleotide-sensitive fashion, to an apparently homogeneous class of sites at equilibrium (K(D) = 1.4 nM, Bmax = 34 fmol/mg protein). The profile of binding was broadly similar to that of rodents, with a couple of significant differences. Most notably, the potency of the histamine H3-receptor-specific antagonist thioperamide (Ki = 240 nM) was substantially less than reported for rodents and under assay conditions that yield a two-site curve fit in rodents only a single class of thioperamide binding sites was detected in monkey. Burimamide, however, yielded a two-site curve fit (KiH = 6.7 nM, KiL = 1100 nM) independent of the presence of sodium in the assay, as it does in rodents. Characterization of the human brain histamine H3 receptor showed that it was similar to the monkey and not rodent receptor. Our findings indicate that differences between primate and rodent histamine H3 receptors of potentially serious importance for the discovery of antagonists active in humans do exist.
[Mh] Termos MeSH primário: Encéfalo/metabolismo
Membrana Celular/metabolismo
Metilistaminas/metabolismo
Piperidinas/metabolismo
[Mh] Termos MeSH secundário: Animais
Burimamida/metabolismo
Nucleotídeos de Guanina/farmacologia
Seres Humanos
Técnicas In Vitro
Macaca fascicularis
Receptores Histamínicos/metabolismo
Especificidade da Espécie
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Guanine Nucleotides); 0 (Methylhistamines); 0 (Piperidines); 0 (Receptors, Histamine); II4319BWUI (thioperamide); TN5A4OD2TV (Burimamide)
[Em] Mês de entrada:9910
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:990824
[St] Status:MEDLINE


  5 / 169 MEDLINE  
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[PMID]:9681472
[Au] Autor:Alewijnse AE; Smit MJ; Hoffmann M; Verzijl D; Timmerman H; Leurs R
[Ad] Endereço:Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, The Netherlands.
[Ti] Título:Constitutive activity and structural instability of the wild-type human H2 receptor.
[So] Source:J Neurochem;71(2):799-807, 1998 Aug.
[Is] ISSN:0022-3042
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Stable expression of the human H2 receptor in Chinese hamster ovary cells resulted in an increase in basal cyclic AMP (cAMP) production, which was inhibited by the inverse agonists cimetidine, famotidine, and ranitidine with potencies similar to those found for the rat H2 receptor. Burimamide, a neutral antagonist at the rat H2 receptor, behaved as a weak partial agonist at the human H2 receptor. Burimamide competitively antagonized both the histamine-induced increase in cAMP and the cimetidine-induced reduction of the basal cAMP level with apparent K(B) values that were similar to its H2 receptor affinity. Investigation of the modulation of receptor expression after long-term drug treatment revealed that at low concentrations histamine induced a significant reduction in H2 receptor expression, whereas at high concentrations receptor expression was slightly increased. The partial agonist burimamide induced, like inverse agonists, an up-regulation of the human H2 receptor after prolonged treatment. These findings suggest a structural instability of the constitutively active human H2 receptor in transfected Chinese hamster ovary cells. Occupation of the H2 receptor by any ligand reduces the instability, thus resulting in higher cellular expression levels.
[Mh] Termos MeSH primário: Antagonistas dos Receptores Histamínicos H2/farmacologia
Receptores Histamínicos H2/genética
Regulação para Cima/genética
[Mh] Termos MeSH secundário: Animais
Ligação Competitiva/fisiologia
Burimamida/farmacologia
Células CHO/fisiologia
Cimetidina/farmacologia
Cricetinae
AMP Cíclico/metabolismo
Relação Dose-Resposta a Droga
Regulação para Baixo/genética
Famotidina/farmacologia
Expressão Gênica/efeitos dos fármacos
Seres Humanos
Ranitidina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine H2 Antagonists); 0 (Receptors, Histamine H2); 5QZO15J2Z8 (Famotidine); 80061L1WGD (Cimetidine); 884KT10YB7 (Ranitidine); E0399OZS9N (Cyclic AMP); TN5A4OD2TV (Burimamide)
[Em] Mês de entrada:9808
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:980729
[St] Status:MEDLINE


  6 / 169 MEDLINE  
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[PMID]:9400031
[Au] Autor:Hough LB; Nalwalk JW; Li BY; Leurs R; Menge WM; Timmerman H; Carlile ME; Cioffi C; Wentland M
[Ad] Endereço:Department of Pharmacology and Neuroscience, Albany Medical College, Albany, New York 12208, USA.
[Ti] Título:Novel qualitative structure-activity relationships for the antinociceptive actions of H2 antagonists, H3 antagonists and derivatives.
[So] Source:J Pharmacol Exp Ther;283(3):1534-43, 1997 Dec.
[Is] ISSN:0022-3565
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Recent studies have shown that cimetidine, burimamide and improgan (also known as SKF92374, a cimetidine congener lacking H2 antagonist activity) induce antinociception after intracerebroventricular administration in rodents. Because these substances closely resemble the structure of histamine (a known mediator of some endogenous analgesic responses), yet no role for known histamine receptors has been found in the analgesic actions of these agents, the structure-activity relationships for the antinociceptive effects of 21 compounds chemically related to H2 and H3 antagonists were investigated in this study. Antinociceptive activity was assessed on the hot-plate and tail-flick tests after intracerebroventricular administration in rats. Eleven compounds induced time-dependent (10-min peak) and dose-dependent antinociceptive activity with no observable behavioral impairment. ED50 values, estimated by nonlinear regression, were highly correlated across nociceptive assays (r2 = 0.98, n = 11). Antinociceptive potencies varied more than 6-fold (80-464 nmol), but were not correlated with activity on H1, H2 or H3 receptors. Although highly potent H3 antagonists such as thioperamide lacked antinociceptive activity, homologs of burimamide and thioperamide containing N-aromatic substituents retained H3 antagonist activity and also showed potent, effective analgesia. A literature review of the pharmacology of these agents did not find a basis for their antinociceptive effects. Taken with previous findings, the present results suggest: 1) these compounds act on the brain to activate powerful analgesic responses that are independent of known histamine receptors, 2) the structure-activity profile of these agents is novel and 3) brain-penetrating derivatives of these compounds could be clinically useful analgesics.
[Mh] Termos MeSH primário: Analgésicos não Entorpecentes/farmacologia
Antagonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Receptores Histamínicos H3/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Burimamida/farmacologia
Relação Dose-Resposta a Droga
Imidazóis/farmacologia
Masculino
Piperidinas/farmacologia
Ratos
Ratos Sprague-Dawley
Relação Estrutura-Atividade
Tioureia/análogos & derivados
Tioureia/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Analgesics, Non-Narcotic); 0 (Histamine Antagonists); 0 (Histamine H2 Antagonists); 0 (Imidazoles); 0 (Piperidines); 0 (Receptors, Histamine H3); GYV9AM2QAG (Thiourea); II4319BWUI (thioperamide); RKU631JF4H (clobenpropit); TN5A4OD2TV (Burimamide)
[Em] Mês de entrada:9801
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:980212
[St] Status:MEDLINE


  7 / 169 MEDLINE  
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[PMID]:8866956
[Au] Autor:Lamberti C; Bartolini A; Ghelardini C; Malmberg-Aiello P
[Ad] Endereço:Department of Preclinical and Clinical Pharmacology, University of Florence, Firenze, Italy.
[Ti] Título:Investigation into the role of histamine receptors in rodent antinociception.
[So] Source:Pharmacol Biochem Behav;53(3):567-74, 1996 Mar.
[Is] ISSN:0091-3057
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The aim of the present study is to the elucidate the confusion that exists in the literature concerning which receptor subtype is involved in mediating histamine antinociception. To this purpose impromidine 3HCl and burimamide were used. Because both substances have been described to block histamine H3-receptor, and, at higher doses, also to act on the postsynaptic site as agonist and antagonist, respectively, they were administered in a wide range of ICV doses, to distinguish the effects due to action on different receptors. Experiments were performed in mice and rats by means of tests inducing three different kinds of noxious stimuli: mechanical (paw pressure), chemical (abdominal constriction), and thermal (hot plate). Both substances showed, at the lowest doses tested, antinociception, which was antagonized by the selective H3-receptor agonist, (R)-alpha-methylhistamine 2HCl (RAMH) (10 mg/kg SC in mice or 0.5 microgram per rat ICV). At higher doses impromidine was antinociceptive while burimamide was hypernociceptive, in accordance with their opposite action on the H2-receptor. It is suggested that the histaminergic system modulates nociception via activation of the H2-receptor.
[Mh] Termos MeSH primário: Dor/metabolismo
Receptores Histamínicos/efeitos dos fármacos
Receptores Histamínicos/metabolismo
[Mh] Termos MeSH secundário: Animais
Burimamida/farmacologia
Relação Dose-Resposta a Droga
Histamina/metabolismo
Impromidina/farmacologia
Masculino
Camundongos
Camundongos Endogâmicos
Medição da Dor
Ratos
Ratos Wistar
Tempo de Reação/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Receptors, Histamine); 820484N8I3 (Histamine); 931L4X5WMM (Impromidine); TN5A4OD2TV (Burimamide)
[Em] Mês de entrada:9701
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:960301
[St] Status:MEDLINE


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PubMed Central Texto completo
[PMID]:8692899
[Au] Autor:Smit MJ; Leurs R; Alewijnse AE; Blauw J; Van Nieuw Amerongen GP; Van De Vrede Y; Roovers E; Timmerman H
[Ad] Endereço:Leiden/Amsterdam Center for Drug Research, Department of Pharmacochemistry, Vrije Universiteit, Amsterdam, The Netherlands.
[Ti] Título:Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors.
[So] Source:Proc Natl Acad Sci U S A;93(13):6802-7, 1996 Jun 25.
[Is] ISSN:0027-8424
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Histamine H2 receptors transfected in Chinese hamster ovary (CHO) cells are time- and dose-dependently upregulated upon exposure to the H2 antagonists cimetidine and ranitidine. This effect appears to be H2 receptor-mediated as no change in receptor density was observed after H1 or H3 antagonist treatment or after incubation with the structural analogue of cimetidine, VUF 8299, which has no H2 antagonistic effects. By using transfected CHO cells expressing different densities of wild-type H2 receptors or an uncoupled H2Leu124Ala receptor, the histamine H2 receptor was found to display considerable agonist-independent H2 receptor activity. Cimetidine and ranitidine, which both induce H2 receptor upregulation, actually functioned as inverse agonists in those cell lines displaying spontaneous agonist-independent H2 receptor activity. Burimamide, on the other hand, was shown to act as a neutral antagonist and did as expected not induce H2 receptor upregulation after long-term exposure. The displayed inverse agonism of H2 antagonists appears to be a mechanistic basis for the observed H2 antagonist-induced H2 receptor upregulation in transfected CHO cells. These observations shed new light on the pharmacological classification of the H2 antagonists and may offer a plausible explanation for the observed development of tolerance after prolonged clinical use.
[Mh] Termos MeSH primário: Agonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos H2/farmacologia
Receptores Histamínicos H2/fisiologia
Regulação para Cima
[Mh] Termos MeSH secundário: Animais
Burimamida/farmacologia
Células CHO
Cimetidina/farmacologia
Colforsina/farmacologia
Cricetinae
AMP Cíclico/metabolismo
Ranitidina/farmacologia
Receptores Histamínicos H2/genética
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 (Receptors, Histamine H2); 1F7A44V6OU (Colforsin); 80061L1WGD (Cimetidine); 884KT10YB7 (Ranitidine); E0399OZS9N (Cyclic AMP); TN5A4OD2TV (Burimamide)
[Em] Mês de entrada:9608
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:960625
[St] Status:MEDLINE


  9 / 169 MEDLINE  
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[PMID]:7783156
[Au] Autor:Vollinga RC; Menge WM; Leurs R; Timmerman H
[Ad] Endereço:Leiden/Amsterdam Center for Drug Research, Department of Pharmacochemistry, Vrije Universiteit Amsterdam, The Netherlands.
[Ti] Título:New analogs of burimamide as potent and selective histamine H3 receptor antagonists: the effect of chain length variation of the alkyl spacer and modifications of the N-thiourea substituent.
[So] Source:J Med Chem;38(12):2244-50, 1995 Jun 09.
[Is] ISSN:0022-2623
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Burimamide was one of the first compounds reported to antagonize the activation of the histamine H3 receptor by histamine. We have prepared a large series of burimamide analogs by variation of the alkyl spacer length of burimamide from two methylene groups to six methylene groups and also by replacement of the N-methyl group with other alkyl and aryl groups. All analogs are reversible, competitive H3 antagonists as determined on the guinea pig intestine. Elongation of the alkyl chain from an ethylene chain to a hexylene chain results in an increase of the H3 antagonistic activity. The H3 selective pentylene and hexylene analogs of burimamide are about 10 times more potent than burimamide. The N-thiourea substituents, however, have no beneficial influence on the affinity.
[Mh] Termos MeSH primário: Burimamida/análogos & derivados
Antagonistas dos Receptores Histamínicos
Tioureia/química
[Mh] Termos MeSH secundário: Animais
Burimamida/química
Burimamida/farmacologia
Células CHO
Cricetinae
Cobaias
Técnicas In Vitro
Jejuno/efeitos dos fármacos
Jejuno/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine Antagonists); GYV9AM2QAG (Thiourea); TN5A4OD2TV (Burimamide)
[Em] Mês de entrada:9507
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:950609
[St] Status:MEDLINE


  10 / 169 MEDLINE  
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Fotocópia
[PMID]:8012822
[Au] Autor:Cumming P; Gjedde A
[Ad] Endereço:Montreal Neurological Institute, Qué, Canada.
[Ti] Título:Subclasses of histamine H3 antagonist binding sites in rat brain.
[So] Source:Brain Res;641(2):203-7, 1994 Apr 04.
[Is] ISSN:0006-8993
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Histamine H3 antagonists have been reported to discriminate subclasses of histamine H3 agonist binding in rat cortical membranes. This phenomenon was investigated by autoradiography of cryostat sections of rat forebrain labelled with [3H]N alpha-methylhistamine ([3H]NAMH, 4 nM). Displacement curves with thioperamide detected a single site in cortex and striatum (pIC50 = 8.18 +/- 0.03). However, Hill coefficients (nH = 0.51 +/- 0.12) suggested the possible presence of multiple binding sites. Displacement with burimamide was consistent with two site models in all brain regions examined (pIC50(A) = 7.9 +/- 1.5; pIC50(B) = 5.6 +/- 0.7), except for the medial septum where a single site was detected. Elsewhere, the relative abundance of the two sites displaced by burimamide (H3A:H3B) appeared to be 1:2. Thioperamide may have failed to discriminate two sites because the IC50s were too similar to be distinguished in the present autoradiographic study.
[Mh] Termos MeSH primário: Encéfalo/metabolismo
Metilistaminas/metabolismo
Receptores Histamínicos H3/metabolismo
[Mh] Termos MeSH secundário: Animais
Autorradiografia
Sítios de Ligação
Ligação Competitiva
Encéfalo/citologia
Burimamida/farmacologia
Córtex Cerebral/metabolismo
Corpo Estriado/metabolismo
Antagonistas dos Receptores Histamínicos
Masculino
Especificidade de Órgãos
Piperidinas/farmacologia
Prosencéfalo/metabolismo
Ratos
Ratos Wistar
Trítio
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine Antagonists); 0 (Methylhistamines); 0 (Piperidines); 0 (Receptors, Histamine H3); 10028-17-8 (Tritium); 6986-90-9 (alpha-methylhistamine); II4319BWUI (thioperamide); TN5A4OD2TV (Burimamide)
[Em] Mês de entrada:9407
[Cu] Atualização por classe:161123
[Lr] Data última revisão:
161123
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:940404
[St] Status:MEDLINE



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