The Selective 5 : Hydroxytryptamine (5 : HT)_4 : Receptor Agonist RS67506 Enhances Lower Intestinal Propulsion in Mice

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Author(s)

    • Ito Hiroyuki ITO Hiroyuki
    • Neuroscience Research, Pharmacological Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
    • Kiso Tetsuo [他] KISO Tetsuo
    • Neuroscience Research, Pharmacological Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
    • NAITOH Yuki
    • Neuroscience Research, Pharmacological Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
    • MIYATA Keiji
    • Neuroscience Research, Pharmacological Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

Abstract

Interactions of gastrointestinal prokinetic benzamides with 5-hydroxytryptamine (5-HT)<SUB>3</SUB> and 5-HT<SUB>4</SUB> receptors and the relation to their effects on gastrointestinal propulsion were investigated. Renzapride and zacopride potently inhibited 5-HT<SUB>3</SUB>-receptor-mediated contractions in the guinea pig colon, whereas RS67506 (1-(4-amino-5-chloro-2-methoxyphenyl)-3-[1-(2-methyl sulphonylamino)ethyl-4-piperidinyl]-1-propanone hydrochloride), a selective 5-HT<SUB>4</SUB>-receptor agonist, showed no inhibition. RS67506, renzapride and zacopride all exerted 5-HT<SUB>4</SUB> receptor-mediated relaxation in the carbachol-precontracted rat oesophagus. In mice, RS67506 shortened the whole gut transit time, whereas renzapride and zacopride were reported to prolong it. Gastrointestinal prokinetic benzamides, which are selective for 5-HT<SUB>4</SUB>-receptor agonistic over 5-HT<SUB>3</SUB>-receptor antagonistic action, may be useful in treating gastrointestinal disorders associated with impaired lower intestinal propulsion such as constipation.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 74(2), 209-212, 1997-06-01

    The Japanese Pharmacological Society

References:  15

Codes

  • NII Article ID (NAID)
    10008679040
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    SHO
  • ISSN
    00215198
  • NDL Article ID
    4260351
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  NDL  J-STAGE 
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