WS9326A, a novel tachykinin antagonist isolated from Streptomyces violaceusniger No. 9326. II. Biological and pharmacological properties of WS93326A and terahydro-WS9326A (FK224)
-
- HASHIMOTO MICHIZANE
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
-
- HAYASHI KENICHI
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
-
- MURAI MASAKO
- New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
-
- FUJII TAKASHI
- New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
-
- NISHIKAWA MOTOAKI
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
-
- KIYOTO SUMIO
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
-
- OKUHARA MASAKUNI
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
-
- KOHSAKA MASANOBU
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
-
- IMANAKA HIROSHI
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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
この論文をさがす
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).
収録刊行物
-
- The Journal of Antibiotics
-
The Journal of Antibiotics 45 (7), 1064-1070, 1992
公益財団法人 日本感染症医薬品協会

