WS9326A, a novel tachykinin antagonist isolated from Streptomyces violaceusniger No. 9326. II. Biological and pharmacological properties of WS93326A and terahydro-WS9326A (FK224)

書誌事項

タイトル別名
  • WS9326A, a novel tachykinin antagonist isolated from Streptomyces violaceusniger No. 9326. II Biological and pharmacological properties of WS9326A and tetrahydro-WS9326A (FK224).
  • II. BIOLOGICAL AND PHARMACOLOGICAL PROPERTIES OF WS9326A AND TETRAHYDRO-WS9326A (FK224)
公開日
1992
資源種別
journal article
DOI
  • 10.7164/antibiotics.45.1064
公開者
公益財団法人 日本感染症医薬品協会

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説明

WS9326A binds competitively to [3H]substance P (NK-1 receptor) binding sites on guinea-pig lung membranes (IC50 = 3.6 × 10-6 M), and acts as a tachykinin antagonist in various functional assays.<br> WS9326A inhibited tracheal constrictions produced by exogenously added substance P and neurokinin A, with IC50 values of 9.7 × 10-6 M and 3.5 × 10-6 M, respectively. WS9326A inhibited neurokinin A-induced bronchoconstriction in a dose dependent manner when administered to guinea-pigs intravenously together with neurokinin A, and was also effective in preventing capsaicin-induced bronchoconstriction, which is known to be caused by release of endogenous tachykinins (substance P and neurokinin A).<br> FK224 (tetrahydro-WS9326A; catalytic hydrogenation of WS9326A gave FK224) was more potent than WS9326A in the [3H]substance P receptor binding assay using guinea-pig lung membrane (IC50 = 1.0 × 10-7 M).

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詳細情報 詳細情報について

  • CRID
    1390282679121947136
  • NII論文ID
    130003502314
  • DOI
    10.7164/antibiotics.45.1064
  • COI
    1:CAS:528:DyaK38Xls1eltr8%3D
  • ISSN
    18811469
    00218820
    http://id.crossref.org/issn/00218820
  • PubMed
    1381344
  • 本文言語コード
    en
  • 資料種別
    journal article
  • データソース種別
    • JaLC
    • Crossref
    • PubMed
    • CiNii Articles
  • 抄録ライセンスフラグ
    使用不可

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