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  • 1
    ISSN: 1420-908X
    Keywords: Rat mast cell proteases ; Histamine presynaptic receptor ; Dexamethasone
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The sensitivity of mast cells to H3-receptor modulation was studied in rat lung under various hormonal conditions. The heterogeneity of mast cell subpopulations in rat lung was assessed by the tissue content of rat mast cell protease I (RMCP I) and rat mast cell protease II (RMCP II). After 24 h fasting, concentrations of RMCP I were unchanged whereas the concentration of RMCP II was significantly reduced by 49%. The [3H]histamine (HA) synthesis was concomitantly decreased by 35%. In addition, the modulation of [3H]HA, synthesis by the H3 receptor agonist, (R)α-methylHA and by the antagonist, thioperamide, observed in control rats, was lost in fasted rats. Single and repeated, administrations of dexamethasone did not influence RMCPI concentrations, but decreased the concentrations of RMCP II with a parallel decrease in [3H]HA synthesis. The inhibitory effect of (R)α-methylHA on [3H]HA synthesis was also reduced. These results suggest that a subpopulation of RMCP II-containing mast cells, very sensitive to environmental factors, could be the mast cells synthesizing HA in an H3-receptor-dependant manner.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 308 (1979), S. 231-237 
    ISSN: 1432-1912
    Keywords: 3H-Domperidone ; Dopamine receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary 3H-Domperidone, a potent antagonist of dopamine but less lipophilic than neuroleptic drugs, was studied as a potential ligand for cerebral dopamine receptors. It labeled with high affinity an apparently homogeneous population of non-interacting sites in a particulate fraction of mouse striatum. Association occurred rapidly and dissociation was relatively slow (t1/2≃4min); this allowed extensive washing of membranes which reduced the non-specific binding to values as low as 5% of the total binding. Consistent Kd values of 0.7 nM were obtained by analysing by various methods either the kinetics of binding or the saturation of binding sites at equilibrium. The relative potencies of various dopamine receptor agonists or antagonists to inhibit 3H-domperidone binding, paralleled their pharmacological activity. On the other hand, a variety of non-dopaminergic agents failed to inhibit 3H-domperidone binding. The findings indicate that striatal dopamine receptors are selectively labeled by this 3H-ligand. In various non-striatal regions of mouse brain the saturable binding of 3H-domperidone was almost entirely inhibited by apomorphine indicating its selectivity for dopamine receptors in spite of the low density of the latter. This was not the case for the binding of 3H-spiperone, evaluated on the same preparations, indicating that 3H-domperidone probably represents the most selective ligand presently available.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Chichester : Wiley-Blackwell
    Biological Mass Spectrometry 23 (1988), S. 579-584 
    ISSN: 0030-493X
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: A type of tandem mass spectrometric scan is described in which m1 +, m2 + and m3, defined in terms of the process m1 + → m2 + + m3, are all varied while maintaining some prescribed relationship between them. The scan can be viewed as a variant upon the neutral loss scan in which the constant mass difference between parent and daughter ion masses is replaced by some other functional relationship. Specific examples of this scan are provided in two simple applications: (i) symmetrical proton-bound dimers are recognized using the functional scan m2 = (m1 + 1)/2; and (ii) symmetrical Diels-Alder adducts comprised of diene and dienophile of equal masses are recognized in mixtures using the scan function m2 = (1/2)m1.
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
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