Facilitation of Acetylcholine Release by SK-951, a Benzofuran Derivative, via the 5-Hydroxytryptamine_4 Receptor in Guinea Pig Stomach

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Facilitation of acetylcholine(ACh) release by SK-951((−)4-amino-N-[2-(1-azabicyclo[3.3.0]octan-5-yl)ethyl]-5-chloro-2, 3-dihydro-2-methylbenzo[b]furan-7-carboxamine hemifumarate), a benzofuran derivative, via the 5-hydroxytryptamine(5-HT)<SUB>4</SUB> receptor in guinea pig stomach was examined by in vitro receptor autoradiography and functional studies.[<SUP>125</SUP>I]SB207710 binding was detected in the myenteric plexus of the gastric corpus.High densities of binding sites were observed in the myenteric plexus and a moderate density in the muscle layer.SK-951 inhibited the binding of [<SUP>125</SUP>I]SB207710, a specific 5-HT<SUB>4</SUB>-receptor ligand, as in the case of SB204070, a specific 5-HT<SUB>4</SUB>-receptor antagonist, thus indicating the presence of 5-HT<SUB>4</SUB> receptors in guinea pig stomach.SK-951 as well as 5-HT enhanced the electrically stimulated twitch contractions of gastric corpus strips, which were sensitive to tetrodotoxin and atropine, and enhanced electrically stimulated release of ACh from corporal strips, which was tetrodotoxin-sensitive and Ca<SUP>2+</SUP>-dependent.The enhancements of twitch contractions and ACh release by SK-951 were antagonized by GR113808, a selective 5-HT<SUB>4</SUB>-receptor antagonist.Thus, SK-951 binds to 5-HT<SUB>4</SUB> receptors of the guinea pig gastric corpus and may accelerate gastric motility due to facilitation of ACh release.

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  • The Japanese journal of pharmacology

    The Japanese journal of pharmacology 82(2), 138-143, 2000-02-01

    公益社団法人 日本薬理学会

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各種コード

  • NII論文ID(NAID)
    10008183134
  • 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
    5283944
  • 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  NDL  J-STAGE 
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