Affinity of Mosapride Citrate, a New Gastroprokinetic Agent,for 5-HT4 Receptors in Guinea Pig Ileum

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We examined the binding affinity of mosapride citrate (mosapride) (4-amino-5-chloro-2-ethoxy-<I>N</I>-{[4-(4-fluorobenzyl)-2-morpholinyl]methyl}benzamide citrate), a novel gastroprokinetic agent, for the 5-hydroxytryptamine (5-HT) 4 receptors in guinea pig ileum using a selective 5-HT<SUB>4</SUB>-receptor radioligand, [<SUP>3</SUP>H]GR113808. In membrane preparations from longitudinal muscle with myenteric plexus in guinea pig ileum, specific [<SUP>3</SUP>H]GR113808 binding revealed a single saturable site of high affinity (K<SUB>d</SUB>=0.28±0.02 nM, B<SUB>max</SUB>=45±3 fmol/mg protein). Mosapride and other 5-HT<SUB>4</SUB>-receptor agonists inhibited the specific binding of [<SUP>3</SUP>H]GR113808 in guinea pig ileum. The 5-HT<SUB>4</SUB> agonists examined displayed the following inhibition potency order: BIMU-8 > cisapride > mosapride > renzapride > 5-HT > zacopride > metoclopramide. Mosapride exhibited monophasic inhibition of the specific [<SUP>3</SUP>H]GR113808 binding in the ileum (K<SUB>i</SUB> value: 84.2 nM). The presence of mosapride (30 nM) significantly increased the K<SUB>d</SUB> value to 0.44±0.05 nM in the Scatchard analysis of [<SUP>3</SUP>H]GR113808 binding. B<SUB>max</SUB> of [<SUP>3</SUP>H]GR113808, however, was not affected (48±4 fmol/mg protein) by mosapride. As for the affinity of mosapride, the addition of GppNHp (100 μM) slightly increased the K<SUB>i</SUB> value to 104 nM. These results indicate that mosapride has an affinity for 5-HT<SUB>4</SUB> receptors in guinea pig ileum in the radioligand binding study.

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  • The Japanese journal of pharmacology

    The Japanese journal of pharmacology 77(1), 53-59, 1998-05-01

    The Japanese Pharmacological Society

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各種コード

  • NII論文ID(NAID)
    10008680158
  • NII書誌ID(NCID)
    AA00691188
  • 本文言語コード
    ENG
  • 資料種別
    ART
  • ISSN
    00215198
  • NDL 記事登録ID
    4503674
  • NDL 雑誌分類
    ZS51(科学技術--薬学)
  • NDL 請求記号
    Z53-D199
  • データ提供元
    CJP書誌  CJP引用  NDL  J-STAGE 
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