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  • 1990-1994  (3)
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  • 1
    Electronic Resource
    Electronic Resource
    Characterization of a Human NK1 Tachykinin Receptor in the Astrocytoma Cell Line U 373 MG (1993)
    Oxford, UK : Blackwell Publishing Ltd
    Journal of neurochemistry 60 (1993), S. 0 
    Details
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract: The human NK1 tachykinin receptor in the astrocytoma cell line U 373 MG was characterized using selective agonists and antagonists described for this receptor in the rat. Specific [3H]substance P binding sites were present on cell homogenates, whereas [3H]neurokinin A or [3H]-senktide binding sites were absent. The binding was saturable and reversible. The binding of [3H]substance P was inhibited by very low concentrations of [L-Pro9]substance P and [Sar9,Met(O2)11]substance P; septide was ∼ 1,000-fold less potent. The most potent peptide antagonist was trans-4-hydroxy-1-(1 H-indol-3-ylcarbonyl)-L-prolyl-N-methyl-N-(phenylmethyl)-L-tyrosineamide. The rank order of potency for the nonpeptide antagonists was (S,S)-CP 96,345 〉 (±)-CP 96,345 〉 (±)-2-chlorobenzylquinuclidinone 〉 (R,R)-CP 96,345 〉 RP 67580 〉 RP 68651. In [3H]-inositol-labeled cells, substance P stimulated phosphatidylinositol turnover. A good correlation was found when the abilities of NK1 receptor agonists for stimulating inositol phosphate production and for inhibiting [3H]substance P binding were compared. Similarly, the binding and functional assays were well correlated for the antagonists. As a result of its high sensitivity and selectivity, the U 373 MG cell line thus appears an excellent tool for investigating the pharmacology of the human NK1 receptor.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1471-4159.1993.tb03231.x
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Radar mapping of Mercury's polar anomalies (1994)
    [s.l.] : Nature Publishing Group
    Nature 369 (1994), S. 213-215 
    Details
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] In a preliminary report of Arecibo radar results2 we showed that the south polar anomaly was mostly confined to the large crater Chao Meng-Fu. At the north pole the evidence was not so tidy. The north polar anomaly was clearly too large to fit within a single crater and had an offset from the pole ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/369213a0
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Use of scanning cytometry in studying bradykinin binding in MRC-5 cells (1994)
    Springer
    Cell biology and toxicology 10 (1994), S. 317-322 
    Details
    ISSN: 1573-6822
    Keywords: bradykinin ; calcium ; ionomycin ; scanning cytometry
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract Ligand-receptor affinity is classically demonstrated by measuring ligand binding density to a specific site on membrane preparations, and receptor function is studied by measuring calcium flux, cell by cell, using microspectrofluorimetry. In order to study these phenomena in a larger cell population, calcium flux was measured in MRC-5 cell line expressing the B2 receptor for bradykinin using an ACAS 570 scanning cytometer. Following incorporation of fluo3/AM, different ligands were studied, singly or in association with bradykinin. This study confirmed that only the B2 receptor is present on the plasma membrane of MRC-5 cells. Bradykinin binding to the B2 receptor was not modified by a B1 agonist (Des-Arg9-bradykinin) or by a B1 antagonist (Des-Arg9-[Leu8]-bradykinin) but was inhibited by a B2 agonist ([Hyp3]-bradykinin) and a B2 antagonist (HOE 140). The source of free calcium was also studied in comparison with ionomycin. The intensity of the calcium peak after binding of bradykinin is independent of the concentration of extracellular calcium. Preincubation with diltiazem or TMB-8 did not modify calcium flux indicating that transduction of the signal after bradykinin binding in this cell line is independent of voltage-dependent channels and does not require mobilization of intracellular calcium blocked by TMB-8. In conclusion, scanning cytometry can be used to study ligand-receptor binding and to obtain results rapidly from multiple cells. Recording of individual cell variations and kinetics enables identification of active agonists or antagonists and consequently the selection of new compounds.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00755777
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    Paper (German National Licenses)
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