Comparative Study of [^3H]Ramosetron and [^3H]Granisetron Binding in the Cloned Human 5 : Hydroxytryptamine_3 Receptors

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Author(s)

    • Ito Hiroyuki ITO Hiroyuki
    • Neuroscience Research, Pharmacology Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

Abstract

Characteristics of the binding of [<SUP>3</SUP>H]ramosetron to cloned human 5-hydroxytryptamine<SUB>3</SUB> (5-HT<SUB>3</SUB>) receptors were investigated and directly compared to those of [<SUP>3</SUP>H]granisetron binding. Saturation studies revealed that [<SUP>3</SUP>H]ramosetron labeled more sites with high affinity (K<SUB>d</SUB>=0.15±0.01 nM, B<SUB>max</SUB>=653±30 fmol/mg protein) than [<SUP>3</SUP>H]granisetron (K<SUB>d</SUB>=1.17±0.25 nM, B<SUB>max</SUB>=427±43 fmol/mg protein). Kinetic studies revealed that dissociation of [<SUP>3</SUP>H]ramosetron was slower than that of [<SUP>3</SUP>H]granisetron. These results suggest that ramosetron is a highly potent 5-HT<SUB>3</SUB>-receptor antagonist.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 78(3), 381-384, 1998-11-01

    The Japanese Pharmacological Society

References:  15

Cited by:  1

Codes

  • NII Article ID (NAID)
    10008681453
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    Journal Article
  • ISSN
    00215198
  • NDL Article ID
    4610828
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  CJPref  NDL  J-STAGE 
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