WS9326A, A NOVEL TACHYKININ ANTAGONIST ISOLATED FROM STREPTOMYCES-VIOLACEUSNIGER NO-9326 .2. BIOLOGICAL AND PHARMACOLOGICAL PROPERTIES OF WS9326A AND TETRAHYDRO-WS9326A (FK224)
WS9326A, A NOVEL TACHYKININ ANTAGONIST ISOLATED FROM STREPTOMYCES-VIOLACEUSNIGER NO-9326 .2. BIOLOGICAL AND PHARMACOLOGICAL PROPERTIES OF WS9326A AND TETRAHYDRO-WS9326A (FK224)
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DOI：
10.7164/antibiotics.45.1064
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发表时间：
1992-07-01
影响因子：
3.3
通讯作者：
IMANAKA, H
中科院分区：
文献类型：
--
作者：
HASHIMOTO, M;HAYASHI, K;IMANAKA, H
WS9326A binds competitively to [H-3]substance P (NK-1 receptor) binding sites on guinea-pig lung membranes (IC50 = 3.6 x 10(-6) M), and acts as a tachykinin antagonist in various functional assays.WS9326A inhibited tracheal constrictions produced by exogenously added substance P and neurokinin A, with IC50 values of 9.7 x 10(-6) M and 3.5 x 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).FK224 (tetrahydro-WS9326A; catalytic hydrogenation of WS9326A gave FK224) was more potent than WS9326A in the [H-3]substance P receptor binding assay using guinea-pig lung membrane (IC50 = 1.0 x 10(-7) M).
