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  • 2000-2004
  • 1995-1999  (3)
  • 1975-1979  (1)
  • Calcification  (2)
  • Cerebral membranes  (2)
  • 1
    ISSN: 1432-1912
    Keywords: µ-, δ-, κ-Opioid-Receptor ; Morphine ; Morphine-3-O-β-D-Glucuronide ; Morphine-6-O-β-D-Glucuronide ; Cerebral membranes ; In-vitro-binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We investigated the nature of interaction of morphine-3-O-β-D-glucuronide (M3G) and morphine6-O-β-D-glucuronide (M6G) with opioid binding sites at the µ-, δ- and κ-opioid receptors (µ-OR, δ-OR and κ-OR) in cerebral membranes. Saturation binding experiments revealed a competitive interaction of M6G with all three opioid receptors. Inhibition binding experiments at the µ-OR employing combinations of morphine and M6G resulted in a rightward shift of the IC50 for morphine proportional to the M6G concentration, thus strengthening the finding of competitive interaction of M6G at the µ-opioid binding site. Data in absence and presence of M6G were included in a three-dimensional model. Compared to a model with one binding site a model with two binding sites significantly improved the fits. This might indicate that different µ-OR subtypes are involved. Hydrolysis of M6G to morphine was investigated and did not occur. Therefore the effects of M6G on binding to the μ-OR were due to M6G and not due to morphine. In contrast, M3G at the three opioid receptors was found to inhibit binding being about 300 times weaker than morphine. This effect was well explained by the amount of contaminating morphine (about 0.3%) identified by HPLC. We conclude that M6G binds to µ-, δ- and κ-OR in a competitive manner. Some of our results on the µ-OR suggest two binding sites for agonists at the μ-OR and that M6G binds to both sites. Our results suggest that the high potency of M6G as an analgesic is mediated through opioid receptors. In contrast, M3G does not interact with the µ-, δ- or κ-OR. We therefore doubt that any effect of M3G is mediated via opioid receptors.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Calcified tissue international 23 (1977), S. 259-269 
    ISSN: 1432-0827
    Keywords: Amorphous calcium phosphate ; Apatite ; Calcification ; Octacalcium phosphate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary The maturation of calcium phosphate crystals formed by the conversion of spontaneously precipitated amorphous calcium phosphate (ACP) was studied in aqueous media at temperatures ranging from 20° to 37°. Reaction pH was kept at 7.4 with either Hepes buffer or by the pH-stat addition of base. Reaction kinetics were followed by monitoring solution calcium and total phosphate, and, in the pH-stat controlled reaction, by recording the amount of KOH needed to maintain pH. Reaction products were examined chemically and by X-ray diffraction and transmission electron microcopy. The first crystals to form deviated markedly from apatite in morphology, composition, structure, and solubility. They were extremely thin and flaky in appearance, had a low Ca/P molar ratio (1.4), contained an appreciable amount of acid phosphate (16%), and had an exceptionally largea-axis (10.5 Å vs. 9.4 Å for apatite). With maturation, the crystals became thicker but smaller in lateral dimensions, more apatitelike in structure and composition, and less soluble. However, this ripening of the crystals was accompanied by unusual inflections in the solution Ca and total PO4 curves, and, in the case of the pH-stat experiments, in the OH consumption profiles as well. These anomalous post-ACP solution changes suggest that a phase change had taken place during crystal maturation. Although the observed structural and compositional changes are not inconsistent with the perfection of an initially defective apatite, the changes in crystal morphology and the anomalous behavior of the reaction solution may more accurately reflect a conversion of the ACP first into an OCP-like crystalline phase which subsequently hydrolyzes into apatite.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-1912
    Keywords: Key words μ- ; δ- ; κ-Opioid-Receptor ; Morphine ; Morphine-3-O-β-D-Glucuronide ; Morphine-6-O-β-D-Glucuronide ; Cerebral membranes ; In-vitro-binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  We investigated the nature of interaction of morphine-3-O-β-D-glucuronide (M3G) and morphine-6-O-β-D-glucuronide (M6G) with opioid binding sites at the μ-, δ- and κ-opioid receptors (μ-OR, δ-OR and κ-OR) in cerebral membranes. Saturation binding experiments revealed a competitive interaction of M6G with all three opioid receptors. Inhibition binding experiments at the μ-OR employing combinations of morphine and M6G resulted in a rightward shift of the IC50 for morphine proportional to the M6G concentration, thus strengthening the finding of competitive interaction of M6G at the μ-opioid binding site. Data in absence and presence of M6G were included in a three-dimensional model. Compared to a model with one binding site a model with two binding sites significantly improved the fits. This might indicate that different μ-OR subtypes are involved. Hydrolysis of M6G to morphine was investigated and did not occur. Therefore the effects of M6G on binding to the μ-OR were due to M6G and not due to morphine. In contrast, M3G at the three opioid receptors was found to inhibit binding being about 300 times weaker than morphine. This effect was well explained by the amount of contaminating morphine (about 0.3%) identified by HPLC. We conclude that M6G binds to μ-, δ- and κ-OR in a competitive manner. Some of our results on the μ-OR suggest two binding sites for agonists at the μ-OR and that M6G binds to both sites. Our results suggest that the high potency of M6G as an analgesic is mediated through opioid receptors. In contrast, M3G does not interact with the μ-, δ- or κ-OR. We therefore doubt that any effect of M3G is mediated via opioid receptors.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1432-1084
    Keywords: Key words: Coronary vessels ; Calcification ; CT ; Stenosis ; Coronary heart disease ; Coronary angiography ; Helical CT
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract. The aim of this study was to evaluate the clinical relevance of coronary artery calcifications detected by spiral CT, congruence with fluoroscopy (FS) and coronary angiography, and comparison with studies reporting on application of double-helical CT and ultrafast CT. Forty patients underwent spiral CT (2-mm slice thickness, table feed 3 mm/s), coronary angiography, and FS (performed in the usual manner). Stenosis and calcifications were evaluated semiquantitatively. Nineteen patients suffering from a stenosis ≥ 75 % were verified at coronary angiography. All had coronary artery calcification on spiral CT. Fluoroscopy did not detect 8 of 19 patients with a stenosis ≥ 75 % (1 vessel: n = 1; 2 vessels: n = 3; 3 vessels: n = 4). In spiral CT sensitivity was 100 % and specificity was 33 % (FS: 58 and 48 %). Positive predictive value was 83 % for spiral CT (FS: 50 %), and negative predictive value was 100 % (FS: 56 %). A significant linear increase in the calcification score was found for increasing maximal stenosis (p 〈 0.005). Spiral CT is more sensitive than FS in the recognition of hemodynamic relevant stenoses using the detection of coronary artery calcifications. Statistical parameters are comparable to ultrafast-CT. Spiral CT is a suitable non-invasive diagnostic technique in coronary heart disease. Coronary calcifications found incidentally in symptomatic patients at chest CT should be reported to the referring physician for further cardiological workup.
    Type of Medium: Electronic Resource
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