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  • 1990-1994  (2)
  • Prostaglandin  (1)
  • muscarinic receptor subtype  (1)
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  • 1990-1994  (2)
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Keywords
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Journal of cancer research and clinical oncology 116 (1990), S. 629-632 
    ISSN: 1432-1335
    Keywords: Methotrexate ; diarrhea ; Small intestine ; Prostaglandin ; rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Intraperitoneal administration of methotrexate in a single dose of 40 mg/kg induces fluid accumulation in the small intestine of rats, significantly increasing jejunal PGE2 formation and simultaneously the amounts of PGE2 in the intestinal contents in vivo. Concomitantly, jejunal PGD2 and 6-keto-PGF1α generation and the amounts of these prostaglandins in the intestinal contents were significantly lowered. However, PGD2 and 6-keto-PGFα jejunal release, and the amounts of these prostaglandins found in the intestinal contents, were already low after a subletal dose (4 mg/kg) of methotrexate, whereas the jejunal release as well as the amounts in the intestinal contents of PGE2 were not altered. Fluid accumulation, the amounts of prostaglandins in the intestinal contents and jejunal release of prostaglandins are siginificantly inhibited by indomethacin. The increased jejunal synthesis of PGE2, with its enteropooling effect, may play a significant role in methotrexate-induced diarrhea in rats.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1573-2568
    Keywords: stomach ; human gastric mucosa ; muscarinic receptor subtype ; acid secretion ; glandular M3 receptor
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Five subtypes of muscarinic receptors have been distinguished by pharmacological and molecular biological methods. This report characterizes the muscarinic subtype present in human gastric mucosa by radioligand binding studies. The receptor density was 27 ±6 fmollmg protein and the tritiated ligand N-methylscopolamine had an affinity of (KD)0.39±0.08 nM (n=11). The M1 receptor selective antagonist pirenzepine and the M2 receptor selective ligand AF-DX 116 had low affinities of 148±32 nM (n=13) and 4043±1011 nM (n=3) KD,respectively. The glandular M3 antagonists hexahydrosiladifenidol and silahexocyclium had high affinities of KD 78±23 nM (n=5) and 5.6±1.8 nM (n=3). The agonist carbachol interacted with a single low-affinity site and binding was insensitive to modulation by guanine nucleotides. Antagonist and agonist binding studies thus showed an affinity profile typical of M3 receptors of the glandular type.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
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