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  1 / 2552 MEDLINE  
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[PMID]:28964277
[Au] Autor:Yu C; Li L; Xia Q; Tang Y
[Ad] Endereço:Department of Otorhinolaryngology Head and Neck, West China Hospital of Sichuan University, Chengdu, Sichuan, China.
[Ti] Título:Expression and localization of histamine H , H , and H receptors in rat olfactory epithelium.
[So] Source:Int J Pediatr Otorhinolaryngol;101:102-106, 2017 Oct.
[Is] ISSN:1872-8464
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: Histamine is an important chemical mediator in the development of allergic rhinitis and plays a key role in eliciting the nasal symptoms of the disorder. Histamine may also affect smell as a neurotransmitter. However, whether histamine receptors are present in the mammalian olfactory epithelium has not yet been examined. The aim of this study was to investigate the expression and distribution of histamine H , H , and H receptors in rat olfactory epithelium. METHODS: Real-time quantitative PCR and immunohistochemical staining were performed to examine the mRNA level and protein expression and localization of histamine receptors (H , H , and H ) in rat olfactory epithelium. RESULTS: We demonstrated that mRNAs encoding histamine H , H , and H receptors were detected in rat olfactory epithelium. Immunohistochemistry also showed strong positive staining for these receptors. Co-localization of histamine H , H , and H receptors with olfactory mature protein revealed that these three histamine receptors were mainly localized in olfactory receptor neurons. CONCLUSIONS: These findings indicate that histamine H , H , and H receptors are present in rat olfactory epithelium and may play a physiological role in olfactory transmission.
[Mh] Termos MeSH primário: Mucosa Olfatória/metabolismo
Receptores Histamínicos/metabolismo
[Mh] Termos MeSH secundário: Animais
Histamina
Imuno-Histoquímica
Masculino
Ratos
Reação em Cadeia da Polimerase em Tempo Real
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Receptors, Histamine); 820484N8I3 (Histamine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171023
[Lr] Data última revisão:
171023
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171002
[St] Status:MEDLINE


  2 / 2552 MEDLINE  
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[PMID]:28688766
[Au] Autor:Shteinikov VY; Korosteleva AS; Tikhonova TB; Potapieva NN; Tikhonov DB
[Ad] Endereço:I.M.Sechenov Institute of Evolutionary Physiology and Biochemistry RAS, St. Petersburg, Russia.
[Ti] Título:Ligands of histamine receptors modulate acid-sensing ion channels.
[So] Source:Biochem Biophys Res Commun;490(4):1314-1318, 2017 Sep 02.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Recently we found that synthetic compounds containing amino group linked to hydrophobic or aromatic moiety are potent modulators of the proton-gated channels (ASICs). These structures have clear similarity with ligands of histamine receptors. We have also demonstrated that histamine potentiates homomeric ASIC1a by shifting its activation dependence to less acidic conditions. In the present work the action of a series of histamine receptors ligands on recombinant ASIC1a and ASIC2a was characterized. Two types of action were found for ASIC1a. 1-methylhistamine, N-alpha-methylhistamine, dimaprit and thioperamide caused significant potentiation, which was pH-dependent and voltage-independent. The H4R antagonist A943931 caused inhibition, which is likely due to voltage-dependent pore block. ASIC2a were virtually insensitive to the drugs tested. We conclude that ligands of histamine receptors should also be considered as ASIC modulators.
[Mh] Termos MeSH primário: Canais Iônicos Sensíveis a Ácido/genética
Agonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos/farmacologia
Histamina/farmacologia
Receptores Histamínicos/genética
[Mh] Termos MeSH secundário: Canais Iônicos Sensíveis a Ácido/metabolismo
Animais
Células CHO
Cricetulus
Dimaprit/farmacologia
Regulação da Expressão Gênica
Seres Humanos
Concentração de Íons de Hidrogênio
Ligantes
Metilistaminas/farmacologia
Técnicas de Patch-Clamp
Piperidinas/farmacologia
Receptores Histamínicos/metabolismo
Proteínas Recombinantes/genética
Proteínas Recombinantes/metabolismo
Transdução de Sinais
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ASIC1 protein, human); 0 (ASIC2 protein, human); 0 (Acid Sensing Ion Channels); 0 (Histamine Agonists); 0 (Histamine Antagonists); 0 (Ligands); 0 (Methylhistamines); 0 (Piperidines); 0 (Receptors, Histamine); 0 (Recombinant Proteins); 6986-90-9 (alpha-methylhistamine); 820484N8I3 (Histamine); II4319BWUI (thioperamide); KCB81T4EOF (tele-methylhistamine); ZZQ699148P (Dimaprit)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170808
[Lr] Data última revisão:
170808
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170710
[St] Status:MEDLINE


  3 / 2552 MEDLINE  
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[PMID]:28546154
[Au] Autor:Kang JW; Lee YH; Kang MJ; Lee HJ; Oh R; Min HJ; Namkung W; Choi JY; Lee SN; Kim CH; Yoon JH; Cho HJ
[Ad] Endereço:Department of Otorhinolaryngology, Jeju National University College of Medicine, Jeju, Korea; and.
[Ti] Título:Synergistic mucus secretion by histamine and IL-4 through TMEM16A in airway epithelium.
[So] Source:Am J Physiol Lung Cell Mol Physiol;313(3):L466-L476, 2017 Sep 01.
[Is] ISSN:1522-1504
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Histamine is an important mediator of allergic reactions, and mucus hypersecretion is a major allergic symptom. However, the direct effect of histamine on mucus secretion from airway mucosal epithelia has not been clearly demonstrated. TMEM16A is a Ca -activated chloride channel, and it is closely related to fluid secretion in airway mucosal epithelia. We investigated whether histamine directly induces fluid secretion from epithelial cells or submucosal glands (SMG) and mechanisms related, therewith, in allergic airway diseases. In pig airway tissues from the nose or trachea, histamine was a potent secretagogue that directly induced strong responses. However, gland secretion from human nasal tissue was not induced by histamine, even in allergic rhinitis patients. Histamine type 1 receptor (H1R) and histamine type 2 receptor (H2R) were not noted in SMG by in situ hybridization. Cultured primary human nasal epithelial (NHE) cells were used for the measurement of short-circuit current changes with the Ussing chamber. Histamine-induced slight responses of anion secretions under normal conditions. The response was enhanced by IL-4 stimulation through TMEM16A, which might be related to fluid hypersecretion in allergic rhinitis. Pretreatment with IL-4 augmented the histamine response that was suppressed by a TMEM16A inhibitor. TMEM16A expression was enhanced by 24-h treatment of IL-4 in human nasal epithelial cells. The expression of TMEM16A was significantly elevated in an allergic rhinitis group, compared with a control group. We elucidated histamine-induced fluid secretions in synergy with IL-4 through TMEM16A in the human airway epithelium. In addition, we observed species differences between pigs and humans in terms of gland secretion of histamine.
[Mh] Termos MeSH primário: Canais de Cloreto/metabolismo
Histamina/farmacologia
Interleucina-4/farmacologia
Muco/secreção
Proteínas de Neoplasias/metabolismo
Mucosa Respiratória/secreção
[Mh] Termos MeSH secundário: Adulto
Animais
Anoctamina-1
Células Cultivadas
Células Epiteliais/efeitos dos fármacos
Células Epiteliais/metabolismo
Regulação da Expressão Gênica/efeitos dos fármacos
Seres Humanos
Ativação do Canal Iônico/efeitos dos fármacos
Modelos Biológicos
Nariz/metabolismo
RNA Mensageiro/genética
RNA Mensageiro/metabolismo
Receptores Histamínicos/genética
Receptores Histamínicos/metabolismo
Mucosa Respiratória/efeitos dos fármacos
Rinite Alérgica/metabolismo
Rinite Alérgica/patologia
Sus scrofa
Traqueia/patologia
Conchas Nasais/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ANO1 protein, human); 0 (Anoctamin-1); 0 (Chloride Channels); 0 (Neoplasm Proteins); 0 (RNA, Messenger); 0 (Receptors, Histamine); 207137-56-2 (Interleukin-4); 820484N8I3 (Histamine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170527
[St] Status:MEDLINE
[do] DOI:10.1152/ajplung.00103.2017


  4 / 2552 MEDLINE  
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[PMID]:28321587
[Au] Autor:Bähre H; Kaever V
[Ad] Endereço:Institute of Pharmacology, Hannover Medical School, Carl-Neuberg-Str. 1, Hannover, D-30625, Germany.
[Ti] Título:Analytical Methods for the Quantification of Histamine and Histamine Metabolites.
[So] Source:Handb Exp Pharmacol;241:3-19, 2017.
[Is] ISSN:0171-2004
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The endogenous metabolite histamine (HA) is synthesized in various mammalian cells but can also be ingested from exogenous sources. It is involved in a plethora of physiological and pathophysiological processes. So far, four different HA receptors (H R-H R) have been described and numerous HAR antagonists have been developed. Contemporary investigations regarding the various roles of HA and its main metabolites have been hampered by the lack of highly specific and sensitive analytic methods for all of these analytes. Liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) is the method of choice for identification and sensitive quantification of many low-molecular weight endogenous metabolites. In this chapter, different methodological aspects of HA quantification as well as recommendations for LC-MS/MS methods suitable for analysis of HA and its main metabolites are summarized.
[Mh] Termos MeSH primário: Histamina/metabolismo
[Mh] Termos MeSH secundário: Animais
Cromatografia Líquida/métodos
Antagonistas dos Receptores Histamínicos/farmacologia
Seres Humanos
Receptores Histamínicos/metabolismo
Espectrometria de Massas em Tandem/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Histamine Antagonists); 0 (Receptors, Histamine); 820484N8I3 (Histamine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170322
[St] Status:MEDLINE
[do] DOI:10.1007/164_2017_22


  5 / 2552 MEDLINE  
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[PMID]:28274820
[Au] Autor:Andersson R; Galter D; Papadia D; Fisahn A
[Ad] Endereço:Neuronal Oscillations Laboratory, Neurogeriatrics Division, Center for Alzheimer Research, Dept. of Neurobiology, Care Sciences and Society, Karolinska Institutet, 14186 Stockholm, Sweden.
[Ti] Título:Histamine induces KCNQ channel-dependent gamma oscillations in rat hippocampus via activation of the H1 receptor.
[So] Source:Neuropharmacology;118:13-25, 2017 May 15.
[Is] ISSN:1873-7064
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Histamine is an aminergic neurotransmitter, which regulates wakefulness, arousal and attention in the central nervous system. Histamine receptors have been the target of efforts to develop pro-cognitive drugs to treat disorders such as Alzheimer's disease and schizophrenia. Cognitive functions including attention are closely associated with gamma oscillations, a rhythmical electrical activity pattern in the 30-80 Hz range, which depends on the synchronized activity of excitatory pyramidal cells and inhibitory fast-spiking interneurons. We set out to explore whether histamine has a role in promoting gamma oscillations in the hippocampus. Using in-situ hybridization we demonstrate that histamine receptor subtypes 1, 2 and 3 are expressed in stratum pyramidale of area CA3 in rats. We show that both pyramidal cells and fast-spiking interneurons depolarize and increase action potential firing in response to histamine in vitro. The activation of histamine receptors generates dose-dependent, transient gamma oscillations in area CA3 of the hippocampus - the locus of the gamma rhythm generator. We also demonstrate that this histamine effect is independent of muscarinic receptors. Using specific antagonists we provide evidence that histamine gamma rhythmogenesis specifically depends on the H1 receptor. Histamine also depolarized both pyramidal cells and fast-spiking interneurons and increased membrane resistance in pyramidal cells. The increased membrane resistance is potentially mediated by the inhibition of potassium channels because application of the KCNQ channel opener ICA110381 abolished the oscillations. Taken together our data demonstrate a novel and physiological mechanism for generating gamma oscillations in hippocampus and suggest a role for KCNQ channels in this cognition-relevant brain activity.
[Mh] Termos MeSH primário: Ritmo Gama/efeitos dos fármacos
Hipocampo
Histamínicos/farmacologia
Histamina/farmacologia
Canais de Potássio KCNQ/metabolismo
Receptores Histamínicos/metabolismo
[Mh] Termos MeSH secundário: Potenciais de Ação/efeitos dos fármacos
Animais
Animais Recém-Nascidos
Benzamidas/farmacologia
Glutamato Descarboxilase/metabolismo
Hipocampo/citologia
Hipocampo/efeitos dos fármacos
Hipocampo/fisiologia
Técnicas In Vitro
Masculino
Moduladores de Transporte de Membrana/farmacologia
Rede Nervosa/efeitos dos fármacos
Rede Nervosa/fisiologia
Neurônios/efeitos dos fármacos
Neurotransmissores/farmacologia
Piridinas/farmacologia
Ratos
Ratos Sprague-Dawley
Ubiquitina Tiolesterase/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4-chloro-N-(6-chloropyridin-3-yl)benzamide); 0 (Benzamides); 0 (Histamine Agents); 0 (KCNQ Potassium Channels); 0 (Membrane Transport Modulators); 0 (Neurotransmitter Agents); 0 (Pyridines); 0 (Receptors, Histamine); 820484N8I3 (Histamine); EC 3.4.19.12 (Ubiquitin Thiolesterase); EC 4.1.1.15 (Glutamate Decarboxylase); EC 4.1.1.15 (glutamate decarboxylase 1)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170906
[Lr] Data última revisão:
170906
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170310
[St] Status:MEDLINE


  6 / 2552 MEDLINE  
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[PMID]:28233185
[Au] Autor:Thurmond RL; Venable J; Savall B; La D; Snook S; Dunford PJ; Edwards JP
[Ad] Endereço:Janssen Research & Development, LLC, San Diego, CA, 92121, USA. RTHURMON@its.jnj.com.
[Ti] Título:Clinical Development of Histamine H Receptor Antagonists.
[So] Source:Handb Exp Pharmacol;241:301-320, 2017.
[Is] ISSN:0171-2004
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The discovery of the histamine H receptor (H R) provided a new avenue for the exploration of the physiological role of histamine, as well as providing a new drug target for the development of novel antihistamines. The first step in this process was the identification of selective antagonists to help unravel the pharmacology of the H R relative to other histamine receptors. The discovery of the selective H R antagonist JNJ 7777120 was vital for showing a role for the H R in inflammation and pruritus. While this compound has been very successful as a tool for understanding the function of the receptor, it has drawbacks, including a short in vivo half-life and hypoadrenocorticism toxicity in rats and dogs, that prevented advancing it into clinical studies. Further research let to the discovery of JNJ 39758979, which, similar to JNJ 7777120, was a potent and selective H R antagonist and showed anti-inflammatory and anti-pruritic activity preclinically. JNJ 39758979 advanced into human clinical studies and showed efficacy in reducing experimental pruritus and in patients with atopic dermatitis. However, development of this compound was terminated due to the occurrence of drug-induced agranulocytosis. This was overcome by developing another H R antagonist with a different chemical structure, toreforant, that does not appear to have this side effect. Toreforant has been tested in clinical studies in patients with rheumatoid arthritis, asthma, or psoriasis. In conclusions there have been many H R antagonists reported in the literature, but only a few have been studied in humans underscoring the difficulty in finding ligands with all of the properties necessary for testing in the clinic. Nevertheless, the clinical data to date suggests that H R antagonists can be beneficial in treating atopic dermatitis and pruritus.
[Mh] Termos MeSH primário: Antagonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos/uso terapêutico
Histamina/metabolismo
Receptores Histamínicos/metabolismo
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios/farmacologia
Anti-Inflamatórios/uso terapêutico
Dermatite Atópica/tratamento farmacológico
Dermatite Atópica/metabolismo
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Histamine Antagonists); 0 (Receptors, Histamine); 820484N8I3 (Histamine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170225
[St] Status:MEDLINE
[do] DOI:10.1007/164_2016_130


  7 / 2552 MEDLINE  
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[PMID]:28233178
[Au] Autor:Shan L; Bao AM; Swaab DF
[Ad] Endereço:Department of Neurobiology, Key Laboratory of Medical Neurobiology of Ministry of Health of China, Zhejiang Province Key Laboratory of Neurobiology, Zhejiang University School of Medicine, Hangzhou, China.
[Ti] Título:Changes in Histidine Decarboxylase, Histamine N-Methyltransferase and Histamine Receptors in Neuropsychiatric Disorders.
[So] Source:Handb Exp Pharmacol;241:259-276, 2017.
[Is] ISSN:0171-2004
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Compared to other monoamine neurotransmitters, information on the association between the histaminergic system and neuropsychiatric disorders is scarce, resulting in a lack of histamine-related treatment for these disorders. The current chapter tries to combine information obtained from genetic studies, neuroimaging, post-mortem human brain studies and cerebrospinal fluid measurements with data from recent clinical trials on histamine receptor agonists and antagonists, with a view to determining the possible role of the histaminergic system in neuropsychiatric disorders and to pave the way for novel histamine-related therapeutic strategies.
[Mh] Termos MeSH primário: Histamina N-Metiltransferase/metabolismo
Histidina Descarboxilase/metabolismo
Transtornos Mentais/metabolismo
Receptores Histamínicos/metabolismo
[Mh] Termos MeSH secundário: Animais
Encéfalo/metabolismo
Histamina/metabolismo
Seres Humanos
Neuropsiquiatria/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Receptors, Histamine); 820484N8I3 (Histamine); EC 2.1.1.8 (Histamine N-Methyltransferase); EC 4.1.1.22 (Histidine Decarboxylase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170225
[St] Status:MEDLINE
[do] DOI:10.1007/164_2016_125


  8 / 2552 MEDLINE  
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[PMID]:28233175
[Au] Autor:Schneider EH; Seifert R
[Ad] Endereço:Institute of Pharmacology, Medical School of Hannover, Carl-Neuberg-Str. 1, 30625, Hannover, Germany. schneider.erich@mh-hannover.de.
[Ti] Título:Pharmacological Characterization of Human Histamine Receptors and Histamine Receptor Mutants in the Sf9 Cell Expression System.
[So] Source:Handb Exp Pharmacol;241:63-118, 2017.
[Is] ISSN:0171-2004
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:A large problem of histamine receptor research is data heterogeneity. Various experimental approaches, the complex signaling pathways of mammalian cells, and the use of different species orthologues render it difficult to compare and interpret the published results. Thus, the four human histamine receptor subtypes were analyzed side-by-side in the Sf9 insect cell expression system, using radioligand binding assays as well as functional readouts proximal to the receptor activation event (steady-state GTPase assays and [ S]GTPγS assays). The human H R was co-expressed with the regulators of G protein signaling RGS4 or GAIP, which unmasked a productive interaction between hH R and insect cell Gα . By contrast, functional expression of the hH R required the generation of an hH R-Gsα fusion protein to ensure close proximity of G protein and receptor. Fusion of hH R to the long (Gsα ) or short (Gsα ) splice variant of Gα resulted in comparable constitutive hH R activity, although both G protein variants show different GDP affinities. Medicinal chemistry studies revealed profound species differences between hH R/hH R and their guinea pig orthologues gpH R/gpH R. The causes for these differences were analyzed by molecular modeling in combination with mutational studies. Co-expression of the hH R with Gα , Gα , Gα , and Gα in Sf9 cells revealed high constitutive activity and comparable interaction efficiency with all G protein isoforms. A comparison of various cations (Li , Na , K ) and anions (Cl , Br , I ) revealed that anions with large radii most efficiently stabilize the inactive hH R state. Potential sodium binding sites in the hH R protein were analyzed by expressing specific hH R mutants in Sf9 cells. In contrast to the hH R, the hH R preferentially couples to co-expressed Gα in Sf9 cells. Its high constitutive activity is resistant to NaCl or GTPγS. The hH R shows structural instability and adopts a G protein-independent high-affinity state. A detailed characterization of affinity and activity of a series of hH R antagonists/inverse agonists allowed first conclusions about structure/activity relationships for inverse agonists at hH R. In summary, the Sf9 cell system permitted a successful side-by-side comparison of all four human histamine receptor subtypes. This chapter summarizes the results of pharmacological as well as medicinal chemistry/molecular modeling approaches and demonstrates that these data are not only important for a deeper understanding of H R pharmacology, but also have significant implications for the molecular pharmacology of GPCRs in general.
[Mh] Termos MeSH primário: Expressão Gênica/genética
Mutação/genética
Receptores Histamínicos/genética
Receptores Histamínicos/metabolismo
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação/genética
Proteínas de Ligação ao GTP/genética
Proteínas de Ligação ao GTP/metabolismo
Seres Humanos
Células Sf9
Transdução de Sinais/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Receptors, Histamine); EC 3.6.1.- (GTP-Binding Proteins)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170225
[St] Status:MEDLINE
[do] DOI:10.1007/164_2016_124


  9 / 2552 MEDLINE  
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[PMID]:28110354
[Au] Autor:Strasser A; Wittmann HJ
[Ad] Endereço:Department of Pharmaceutical/Medicinal Chemistry II, Institute of Pharmacy, University of Regensburg, Universitäts-Str. 31, Regensburg, 93040, Germany. andrea.strasser@chemie.uni-regensburg.de.
[Ti] Título:Molecular Modelling Approaches for the Analysis of Histamine Receptors and Their Interaction with Ligands.
[So] Source:Handb Exp Pharmacol;241:31-61, 2017.
[Is] ISSN:0171-2004
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Several experimental techniques to analyse histamine receptors are available, e.g. pharmacological characterisation of known or new compounds by different types of assays or mutagenesis studies. To obtain insights into the histamine receptors on a molecular and structural level, crystal structures have to be determined and molecular modelling studies have to be performed. It is widely accepted to generate homology models of the receptor of interest based on an appropriate crystal structure as a template and to refine the resulting models by molecular dynamic simulations. A lot of modelling techniques, e.g. docking, QSAR or interaction fingerprint methods, are used to predict binding modes of ligands and pharmacological data, e.g. affinity or even efficacy. However, within the last years, molecular dynamic simulations got more and more important: First of all, molecular dynamic simulations are very helpful to refine the binding mode of a ligand to a histamine receptor, obtained by docking studies. Furthermore, with increasing computational performance it got possible to simulate complete binding pathways of ions or ligands from the aqueous extracellular phase into the allosteric or orthosteric binding pocket of histamine receptors.
[Mh] Termos MeSH primário: Receptores Histamínicos/química
Receptores Histamínicos/metabolismo
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Sítios de Ligação/fisiologia
Seres Humanos
Ligantes
Modelos Moleculares
Simulação de Dinâmica Molecular
Conformação Proteica
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Ligands); 0 (Receptors, Histamine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170123
[St] Status:MEDLINE
[do] DOI:10.1007/164_2016_113


  10 / 2552 MEDLINE  
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[PMID]:28109127
[Au] Autor:Corrêa MF; Varela MT; Balbino AM; Torrecilhas AC; Landgraf RG; Troncone LRP; Fernandes JPDS
[Ad] Endereço:Departamento de Ciências Farmacêuticas, Universidade Federal de São Paulo, Diadema, SP, Brazil.
[Ti] Título:1-[(2,3-Dihydro-1-benzofuran-2-yl) methyl]piperazines as novel anti-inflammatory compounds: Synthesis and evaluation on H R/H R.
[So] Source:Chem Biol Drug Des;90(2):317-322, 2017 Aug.
[Is] ISSN:1747-0285
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The histamine receptors (HRs) are members of G-protein-coupled receptor superfamily and traditional targets of huge therapeutic interests. Recently, H R and H R have been explored as targets for drug discovery, including in the search for dual-acting H R/H R ligands. The H R, the most recent histamine receptor, is a promising target for novel anti-inflammatory agents in several conditions such as asthma and other chronic inflammatory diseases. Due to similarity with previously reported ligands of HRs, a set of 1-[(2,3-dihydro-1-benzofuran-2-yl)methyl]piperazines were synthesized and evaluated in competitive binding assays as H R/H R ligands herein. The results showed the compounds presented affinity (K ) for H R/H R in micromolar range, and they are more selective to H R. All the compounds showed no important cytotoxicity to mammalian cells. The phenyl-substituted compound LINS01005 has shown the higher affinity of the set for H R, but no considerable selectivity toward this receptor over H R. LINS01005 showed interesting anti-inflammatory activity in murine asthma model, reducing the eosinophil counts in bronchoalveolar lavage fluid, as well as the COX-2 expression. The presented compounds are valuable prototypes for further improvements to achieve better anti-inflammatory agents.
[Mh] Termos MeSH primário: Anti-Inflamatórios/química
Anti-Inflamatórios/farmacologia
Piperazinas/química
Piperazinas/farmacologia
Receptores Acoplados a Proteínas-G/imunologia
Receptores Histamínicos H3/imunologia
Receptores Histamínicos/imunologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios/síntese química
Anti-Inflamatórios/uso terapêutico
Asma/tratamento farmacológico
Asma/imunologia
Benzofuranos/síntese química
Benzofuranos/química
Benzofuranos/farmacologia
Benzofuranos/uso terapêutico
Seres Humanos
Piperazinas/síntese química
Piperazinas/uso terapêutico
Ratos
Receptores Histamínicos H4
[Pt] Tipo de publicação:LETTER
[Nm] Nome de substância:
0 (1-benzofuran); 0 (Anti-Inflammatory Agents); 0 (Benzofurans); 0 (HRH4 protein, human); 0 (Piperazines); 0 (Receptors, G-Protein-Coupled); 0 (Receptors, Histamine); 0 (Receptors, Histamine H3); 0 (Receptors, Histamine H4)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170122
[St] Status:MEDLINE
[do] DOI:10.1111/cbdd.12947



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