シサプリドの５‐ＨＴ４受容体への親和性

• 片山 謙一

  吉富製薬(株)創薬第二研究所

• 森尾 保徳

  吉富製薬(株)創薬第二研究所

• 芳賀 慶一郎

  吉富製薬(株)創薬第二研究所

• 福田 武美

  吉富製薬(株)創薬第二研究所

書誌事項

タイトル別名

• Cisapride, a gastroprokinetic agent, binds to 5-HT4 receptors.
• シサプリド ノ 5-HT4 ジュヨウタイ エ ノ シンワセイ

抄録

The affinity of cisapride for 5-HT₄ receptors was investigated in comparison with those of other 5-HT₄ receptor agonists and antagonists, such as 5-HT, 5-MeOT, mosapride, zacopride, metoclopramide, BIMU8, GR113808, SDZ 205-557 and ICS 205-930. Cisapride and the other compounds dose-dependently inhibited specific ³H-GR 113808 binding to 5-HT₄ receptors in guinea pig striatal membranes, and complete inhibition of specific ³H-GR1 13808 binding was achieved at the high concentrations of these compounds. Cisapride was 1.9-, 7.3-, 4.3-, 11 and 26-fold more potent than 5-HT, 5-MeOT, mosapride, zacopride and metoclopramide, respectively, in competing for 5-HT₄ receptors. To determine the manner of interaction between cisapride and 5-HT₄ receptors, Scatchard analysis of ³H-GR113808 specific binding to striatal membranes was performed. Cisapride increased the Kd value of ³H-GR 113808 in striatal membranes in a dose-dependent manner without any influence on the binding density (B_max) of ³H-GR1 13808. These findings indicate that cisapride binds to 5-HT4 receptors competing with ³H-GR 113808 in guinea pig striatal membranes.

収録刊行物

• 日本薬理学雑誌

  日本薬理学雑誌 105 (6), 461-468, 1995

  公益社団法人 日本薬理学会

キーワード

• Pharmacology

詳細情報

• CRID: 1390282679248877952
• NII論文ID: 10005706788
• NII書誌ID: AN00198335
• DOI: 10.1254/fpj.105.461
• COI: 1:CAS:528:DyaK2MXmtlantrg%3D
• ISSN: 13478397
• ISSN: 00155691
• NDL書誌ID: 3620374
• PubMed: 7557734
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I3620374
• Web Site: https://search.jamas.or.jp/link/ui/1996010468
• 本文言語コード: ja
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