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  • 1995-1999  (5)
  • 1955-1959  (1)
  • 1935-1939
  • Cerebral membranes  (2)
  • Polymer and Materials Science  (2)
  • thrombolytic therapy  (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
    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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  • 3
    ISSN: 1573-742X
    Keywords: thrombolytic therapy ; saruplase ; myocardial infarction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Saruplase (unglycosylated human-type high molecular weight single-chain urokinase-type plasminogen activator) was given to 1698 patients in the open-label Practical Applicability of Saruplase Study (PASS), which assessed the safety and efficacy of saruplase in the treatment of acute myocardial infarction. Thirty-seven hospitals in Europe participated in the study. All patients received 20 mg saruplase as a bolus followed by an infusion of 60 mg saruplase over 1 hour. Prior to the infusion of saruplase, 62% of the patients received a bolus of 5000 U of heparin, and after saruplase a 24-hour intravenous infusion of heparin was given to 95% of patients. The mean age of the patients was 59 years and 80.1% were male. The median delay from the onset of chest pain to the start of saruplase infusion was 145 minutes. Acute angiography was performed in 8 of the participating 37 centers in 350 patients (20.6%), on average 85 minutes (median) after the start of the saruplase infusion. TIMI 3 flow was obtained in 186 patients (53.1%) and TIMI 2 flow in 61 patients (17.4%). Patency rates were similar for patients with anterior and inferior infarction. ECG signs suggestive of reperfusion were seen in 63% of the patients. In-hospital mortality was low (92 patients; 5.4%), and nonfatal recurrent myocardial infarction was seen in 60 patients (3.5%). Severe bleeding complications occurred in 92 patients (5.4%), 21 of whom (1.2%) needed a blood transfusion. An intracerebral hemorrhage was observed in eight patients (0.5%), and seven patients (0.4%) suffered from a thromboembolic stroke. At discharge 85.9% of the patients were in NYHA functional class I. One-year mortality was low (142 patients; 8.4%). Mortality was high in patients with TIMI 0 or 1 flow at the acute angiography who did not undergo rescue PTCA (9/39; 23.1%), lower in patients with TIMI 0 or 1 flow followed by successful rescue PTCA (7/64; 10.9%), and low in patients with TIMI 2 flow (1/61; 1.6%) or with TIMI 3 flow (2/186; 1.1%). Patency rates and (bleeding) complications did not differ between patients with a body weight greater than or less than 70 kilograms. No antibodies against saruplase were detected in samples from 455 patients. In conclusion, it can be stated that saruplase, given in combination with aspirin and intravenous heparin, can be given safely and effectively to patients with acute myocardial infarction.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1573-742X
    Keywords: thrombolytic therapy ; acute myocardial infarction ; patency
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract To study the safety and efficacy of the thrombolytic agent saruplase as a bolus, the angiographic and clinical outcomes of three bolus regimens were investigated in a pilot study conducted in 192 patients with an acute myocardial infarction and were compared with the standard regimen. Fifty-two patients received a double bolus of 40 mg and 40 mg after 30 minutes, 51 patients a bolus of 80 mg, and 36 patients a bolus of 60 mg. Fifty-three patients received the standard regimen (a bolus of 20 mg and 60 mg IV infusion over 1 hour). At 60 minutes TIMI 2 and 3 flow were, respectively, 9.6% and 61.5% with the 40/40-mg bolus, 15.7% and 51.0% with the 80-mg bolus, 16.7% and 30.6% with the 60-mg bolus, and 7.5% and 54.7% with the standard 20/60-mg infusion. At 90 minutes TIMI 2 and 3 flow improved to 9.6% and 73.1%, 15.7% and 56.9%, 13.9% and 36.1%, and 5.7% and 71.7%, respectively. The primary endpoint, persistent patency (TIMI 2 + 3) at 24–45 hours, was seen in 69.2%, 64.7%, 44.4%, and 67.9% of patients who had no rescue PTCA, respectively. Inclusion in the 60-mg bolus group was prematurely stopped because of their low patency rates. The 40/40-mg bolus group had the highest mortality rate (13.5%), whereas the 60-mg bolus group had no deaths. Other adverse event rates were similar in the four groups. This clinical outcome is highly influenced by rescue PTCA of patients with insufficient TIMI flow. This pilot study indicates that in patients with an acute myocardial infarction, a double bolus of 40/40 mg resulted in the highest patency but also had the highest complication rate. The 80-mg single bolus is an attractive alternative for further evaluation because of its acceptable patency and event profile, and its easy form of administration.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Advanced Materials for Optics and Electronics 6 (1996), S. 239-244 
    ISSN: 1057-9257
    Keywords: molecular semiconductors ; organic semiconductors ; phthalocyanines ; conductivity ; thermopower ; seebeck effect ; Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Electrical Engineering, Measurement and Control Technology , Physics
    Notes: By changing the chemical composition of phthalocyanine molecules, the electrical properties of the ensemble in the solid state can be influenced directly. This is shown for phthalocyaninatomanganese (PcMn) as compared with purely divalent central metals and for complexes in which the ligand system has been modified by either electron-withdrawing heteroatoms such as N instead of CH leading to tetrapyridotetraazaporphyrinatozinc (TPyTAPZn) or substituents such as F instead of H leading to hexadecafluorophthalocyaninatozinc (F16PcZn). The accessibility of additional oxidation states of Mn or the stabilisation of frontier orbital states by the ligand leads to a lower ionisation potential and interactions with impurities or dopant molecules are changed. A change in the observed majority carrier (n-type behaviour) is seen even under UHV conditions. Measurements of the thermoelectric power and electrical conductivity are presented of the pure films and after exposure to oxidising ambient. During film growth either island growth or a growth following the Stranski-Krastanov mechanism was observed. The comparison of the temperature dependence of thermopower and electrical conductivity leads to a discussion of the type of majority carriers, their generation as well as their transportation. For the materials investigated in this study the band model fails to explain the observed properties and a localised transport mechanism has to be considered. A transport in localised states close to the Fermi edge is discussed for TPyTAPZn and F16PcZn.
    Additional Material: 5 Ill.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Hoboken, NJ : Wiley-Blackwell
    Journal of Polymer Science 17 (1955), S. 417-421 
    ISSN: 0022-3832
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Physics
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
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