High Affinity Binding of Azasetron Hydrochloride to 5-Hydroxytryptamine3 Receptors in the Small Intestine of Rats

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Author(s)

Abstract

The binding affinity of azasetron hydrochloride (azasetron)for the 5-hydroxytryptamine3 (5-HT<SUB>3</SUB>)receptor in a tissue preparation of rat small intestine was investigated by using [<SUP>3</SUP>H]granisetron as a radioligand. Scatchard analysis of specific [<SUP>3</SUP>H]granisetron binding revealed a single population of saturable binding sites in the tissue preparation. At this site, azasetron was concentration-dependently competitive with [<SUP>3</SUP>H]granisetron, and it inhibited the specific [<SUP>3</SUP>H]granisetron binding with a K<SUB>i</SUB> value of 0.33 nM. Azasetron has a high affinity for 5-HT<SUB>3</SUB> receptor in the gastrointestinal organ, the very site of its antiemetic action against chemotherapy-induced emesis.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 73(4), 357-360, 1997-04-01

    The Japanese Pharmacological Society

References:  15

Codes

  • NII Article ID (NAID)
    10008677925
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    SHO
  • ISSN
    00215198
  • NDL Article ID
    4196934
  • 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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