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  • 1
    Keywords: Medicine ; Pharmacology ; Biomedicine ; Pharmacology/Toxicology ; Springer eBooks
    Description / Table of Contents: Methodologies to Identify and Analyze Genetic Polymorphisms for Human Histamine Receptors -- Development, Characterization, and Validation of Anti-Human H3 Receptor Isoform-Specific Antibodies -- Approaches to Recombinant Histamine H3/H4 Receptor Expression in Mammalian Cells -- Histamine H2 Receptor Biased Signaling Methods -- Ligand-Binding Kinetics on Histamine Receptors -- Methods to Study the Molecular Pharmacology of the Histamine H4 Receptor -- Chemiluminescence: A Sensitive Method for Detecting the Effects of Histamine Receptor Agonists/Antagonists on Neutrophil Oxidative Burst -- Techniques Used in Pharmacological Evaluation of Histamine H4 Receptor Function on Native Human Eosinophils -- Assessment of the Efficacy of Histamine Receptor Antagonists in Murine Models of Atopic Dermatitis -- Methodological Approaches to Study Histamine Pharmacology in the Kidney: From Cell Culture and Cell Imaging to Functional Assays and Electron Microscopy -- Histamine and the Kidney: In Vivo Animal Models -- Methodological Approaches to Investigate the Effects of Histamine Receptor Targeting Compounds in Preclinical Models of Breast Cancer -- Evaluation of Histidine Decarboxylase (HDC) Activity and Human Histamine Receptor 3 (H3R) and HDC mRNA Levels -- Cerebrospinal Fluid Markers in Neuroinflammation: The Paradigm of Optic Neuritis -- In Vivo Diagnostic Procedures for IgE-Mediated Allergic Disorders -- Dermatological Indications of Antihistamines -- Histamine Quantification in Human Blood Samples
    Abstract: This book illustrates the current state-of-the-art in histamine research, with a focus on the appropriate methodologies to investigate the pharmacological properties and the therapeutic exploitation of HRs and their ligands. In addition, the range of techniques described provides an introduction to complementary cross-methodological disciplines beyond these fields. This multi-disciplinary approach is required to define the ‘decision gates’ that determine the development of more effective and safer therapeutic options for many forms of highly prevalent and debilitating diseases, such as asthma, dementias, dermatitis, and arthritis. Written for the Methods in Pharmacology and Toxicology series, chapters concentrate on practical, hands-on protocols from experts in the techniques. Authoritative and thorough, Histamine Receptors as Drug Targets seeks to aid pharmacologists, biochemists, drug discovery researchers, molecular biologists, chemists, toxicologists, lab scientists, medical doctors, principle investigators, research scientists, lab directors and technicians, as well as graduate students around the world in pursuing the study of this vital scientific area
    Pages: XVI, 517 p. 138 illus., 93 illus. in color. : online resource.
    ISBN: 9781493968435
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  • 2
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Histamine may be released from rat peritoneal mast cells by compound 48/80 and peptide 401 in the presence and absence of extracellular calcium. The process is non-cytolytic and requires an intact cell metabolism. The release produced under both conditions is inhibited by disodium cromoglycate, theophylline, dibutyryl cyclic AMP and (at high concentrations) quercetin. The efficacy of the drugs in the absence of extracellular calcium cannot be explained in terms of their postulated effect on the calciumgating mechanism operative in anaphylactic secretion. Alternative modes of action of the compounds are thus considered.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Inflammation research 12 (1982), S. 60-63 
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The enzyme collagenase was used to disperse human lung into its component cells. The resulting cell suspensions containedcirca 8% mast cells and were used for studies of mediator release without further purification. They exhibited a low (circa 7%) spontaneous release of histamine. They could be sensitized passively and released histamine upon challenge with anti-human IgE. They responded to concanavalin A but not to dextran. Phosphatidyl serine did not potentiate the release induced by these agents. The calcium ionophores, A23187 and ionomycin, both elicited histamine release. The cells were refractory to the action of the basic releasers 48/80 and peptide 401 (MCD-peptide). These results indicate marked differences between human pulmonary mast cells and the more widely used rat peritoneal mast cells.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The calcium antagonists verapamil and nifedipine inhibited histamine release induced from rat peritoneal mast cells by a number of secretory stimuli. However, the concentrations required were much higher than those active in smooth muscle preparations. The inhibition was unaffected by elevated levels of external calcium and the drugs prevented release in the absence of added calcium. The novel calcium antagonist, PY 108-068, had no effect on histamine secretion from mast cells. These results suggest that calcium channels in the mastocyte may differ from those in smooth muscle and that at concentrations required to inhibit secretion, verapamil and nifedipine may have non-specific stabilizing effects on the mast cell membrane.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Histamine release caused by drugs and/or their solvents in clinical conditions is a well documented observation but the mechanism of this reaction is poorly understood. hence in this study, the histamine releasing ability of cremophor El® and six derivatives of 12-hydroxystearic acid (12-HSA) were compared in two models: thein vivo anaesthetized dog and thein vitro isolated rat peritoneal mast cells. The results obtained in both systems differed markedly. Only one compound DH (the diester of 12-HSA with polyethylene glycol) released histamine in both systems. The two substances, which exhibited the weakest histamine releasing ability in the dog model (almost inactive at the doses given) were powerful releasers of histamine from rat peritoneal mast cells (TN, 12-HSA polymerized with ethylene oxide; and ME, the monoester of 12-HSA esterified with polyethylene glycol). The release of histamine from rat peritoneal mast cells was potentiated as the temperature was elevated above 37°C. Due to the heterogenelty of mast cells from both different species and different tissues in the same animal, it is important to choose the appropriate predictive model for clinically important adverse reactions to drugs and/or their solvents. Agents which release histamine by non-specific mechanisms are not uninteresting for the clinical situation.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Inflammation research 41 (1994), S. C3 
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 7
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary The effects in vivo and in vitro of the antiserum to mouse nerve growth factor (NGF) are independent of the presence of complement. These results are consistent with the view that the antiserum acts by neutralizing endogenous NGF.
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Clinically relevant histamine release caused by drugs and/or their solvents is a well known phenomenon. The mechanisms whereby these reactions occur are largely unknown. It was thought that the solubilizing agents potentiate the histamine release elicited by the drugs. Therefore the ability of the two detergents, Cremophor El® and Triton X100, to modulate histamine release from rat peritoneal mast cells was examined. Both detergents were used in concentrations that did not themselves induce histamine release. The addition of the detergents to incubation media containing compound 48/80 (0.1 μg/ml) elevated the release considerably (48/80 alone=16.2±2.1% (n=3); plus Cremophor El® (5%)=41.1±3.3% (n=4); plus Triton X100 (0.02 μl/ml)=39.7±3.9% (n=3); plus Triton X100 (0.01 μl/ml)=33.4±5.0% (n=3)). In contrast, histamine release induced by Concanavalin A or the calcium ionophore A 23187 was inhibited by both detergents. Thus low concentrations of detergents appear to have a dual role, with both potentiation and inhibition of histamine release being observed. Surgical patients receive many drugs, some soluble in aqueous solutions, others only with the aid of solubilizing agents. ‘Hangover effects’ due to different plasma half lives, may therefore cause a seemingly harmless drug to act as a histamine liberator. It is therefore important to examine the action of clinically used solvents on histamine liberation caused by therapeutic agents, in order to gain a further understanding of the reaction mechanisms of adverse reactions to drugs.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Inflammation research 38 (1993), S. C153 
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 10
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract A number of enzymes were screened for their ability to dissociate mesenteric tissues from the rat and guinea pig into their component cells. The bacterial enzyme collagenase was found to be the most satisfactory agent and a procedure based on the use of this protease was developed. The resulting suspensions contained 1–2% free mast cells and exhibited a low (ca. 5%) spontaneous release of histamine. The tissue cells contained less histamine than rat peritoneal mast cells and the guinea pig cells were smaller in size. Cells obtained from actively sensitized animals responded to antigenic challenge more strongly than the chopped tissue indicating that they were functionally intact. Rat mesenteric cells could be passively sensitized with homologous reaginic antibody and also responded to anti-rat IgE. The immunologically induced releases from rat mesenteric and peritoneal cells showed differing sensitivities to potentiation by phosphatidyl serine but the responses were directly comparable in the absence of this effect. Rat mesenteric cells also responded, but less effectively than the peritoneal cells, to the ionophore A23187, concanavalin A, ATP and basic secretagogues. They were, however, essentially refractory to the action of dextran. In contrast, guinea pig mast cells responded strongly only to the ionophore and weakly or not at all to the other agents. These results indicate marked inter-and intra-species differences in the reactivity of mast cells and suggest that rat peritoneal cells should not be used as the sole model for studying histamine secretion.
    Type of Medium: Electronic Resource
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