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  • 1
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Metiamide has been found to be about 10 times more active than burimamide in vitro in antagonizing histamine H2-receptors and nearly 5 times more active in vivo as an antagonist of histamine or pentagastrin-stimulated secretion. Effective oral ED50 doses for inhibition have been estimated as 25 μmole kg−1 against basal secretion in rats and 16 μmole kg−1 against maximal histamine-stimulated secretion in dogs. Administration of metiamide orally daily for 90 days with doses of 1,500 μmole kg−1 to rats and 700 μmole kg−1 to dogs produced signs of kidney damage as the dominant lesion in both species. These toxic doses are roughly 60 and 44 times greater than the ED50 doses in the rat and dog, respectively. These results show that metiamide has the degree of activity and safety needed for a compound to be a candidate for through clinical evaluation.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Inflammation research 9 (1979), S. 72-73 
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Inflammation research 8 (1978), S. 383-384 
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Metiamide has been found to be about 10 times more active than burimamide in vitro in antagonizing histamine H2-receptors and nearly 5 times more active in vivo as an antagonist of histamine or pentagastrin-stimulated secretion. Effective oral ED50 doses for inhibition have been estimated as 25 μmole kg−1 against basal secretion in rats and 16 μmole kg−1 against maximal histamine-stimulated secretion in dogs. Administration of metiamide orally daily for 90 days with doses of 1,500 μmole kg−1 to rats and 700 μmole kg−1 to dogs produced signs of kidney damage as the dominant lesion in both species. These toxic doses are roughly 60 and 44 times greater than the ED50 doses in the rat and dog, respectively. These results show that metiamide has the degree of activity and safety needed for a compound to be a candidate for thorough clinical evaluation.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Journal of molecular medicine 54 (1976), S. 911-914 
    ISSN: 1432-1440
    Keywords: Histamin-H2-Receptorantagonisten ; Gastrin ; Acetylcholin ; Zollinger-Ellison-Syndrom ; Peptisches Ulcus ; Histamine H2-receptor antagonists ; Gastrin ; Acetylcholine ; Zollinger-Ellison syndrome ; Peptic ulcer
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Summary Histamine H2-receptor antagonists, including burimamide, metiamide and cimetidine, are effective antagonists of histamine-stimulated acid secretion from mammalian, avian or reptilian gastric mucosa. Acid secretion stimulated by gastrin or pentagastrin is also inhibited by these drugs, but there is disagreement about the effects of these drugs on acid secretion resulting from activation of acetylcholine receptors. Based on the pharmacological evidence possibilities of treatment by these drugs were discussed in cases with excessive stimulation of acid secretion due to high blood levels of histamine or gastrin. The positive results in several trials on Zollinger-Ellison syndrome and peptic ulcer were very impressive. Some practical problems have still to be solved, for example the appropriate phase for applying the drugs. The demonstrated clinical effectiveness, however, against peptic ulceration offers a clear alternative to surgery for many patients.
    Notes: Zusammenfassung Histamin-H2-Receptorantagonisten, wie Burimamide, Metiamide und Cimetidine, sind wirkungsvolle Hemmstoffe der histaminstimulierten Magensäuresekretion bei Säugern, Vögeln und Reptilien. Auch die gastrinstimulierte Magensaftsekretion läßt sich durch diese Stoffe blocken, während die durch Aktivierung der Acetylcholinreceptoren teilweise, aber nicht in allen Fällen und nicht in ähnlich niedrigen Dosen wie bei Histamin und Gastrin durch die H2-Rezeptorantagonisten beeinflußt wird. Auf dieser pharmakologischen Basis werden Möglichkeiten zur Behandlung von Krankheiten mit H2-Receptorantagonisten diskutiert, die auf erhöhten Blutspiegeln von Histamin und Gastrin beruhen. Die Erfolge in verschiedenen Studien beim Zollinger-Ellison-Syndrom, aber auch bei chronischen Ulcus duodeni sind beeindruckend. Probleme ergeben sich noch aus der Pharmakokinetik, der richtige Zeitpunkt für die Einnahme der Mittel muß erprobt werden. Die erwiesene klinische Wirksamkeit dieser Stoffe beim peptischen Ulcus stellt aber eine klare Alternative zur chirurgischen Therapie bei vielen Patienten dar.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 180 (1957), S. 1127-1127 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] Infused 5-hydroxytryptamine rapidly lowers the secretory-rate induced by histamine while with 5-hydroxytryptophan there is a latency before secretory and blood-pressure changes. Whereas 5-hydroxytryptamine led to changes in blood pressure and secretion within 2 min. after starting the infusion, ...
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] FIG. 1 Three species of imidazole with a side chain R at position 4(5). In aqueous solution at physiological pll (7.4) burimamide exists as an equilibrium mixture of mainly three different imidazole species: the two uncharged tautomers A and B, and the cation C (Fig. 1, R = - (CH8),NHCSNHCHa). ...
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 11 (1875), S. 285-285 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] IN reference to the report in NATURE, vol. xi. p. 258, on Mr. Mallet's communication to the Royal Society, respecting the hexagonal crystallisation of basalt, I beg to offer to your readers a similar explanation of the columnar formation in some mud banks on the shores of some of the rivers in ...
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 11 (1875), S. 444-445 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] IN reference to the letter in NATURE, vol. xi. p. 386, respecting the “Height of Waves,” it may be noted that the data presented would give about 110 ft. for the height above the sea underneath the observer, and the distance from crest to crest 1,125 ft., and so the one would be one-tenth of ...
    Type of Medium: Electronic Resource
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