86 放線菌の産生する新規Substance P受容体拮抗物質WS9326Aに関する研究(口頭発表の部)
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概要
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Substance P is the member of the family of structurally related peptides known as tachykinins and is widely distributed in the body. Several studies suggest that tachykinins are involved in numerous physiolosical activities. In the course of our screening program for tachykinin antagonist, WS9326A was isolated as a Substance P receptor antagonist from Streptomyces violaceoniger No.9326. The structure of WS9326A was elucidated as (1), by spectroscopic analyses and chemical reactions, and finally established by the success of total synthesis. WS9326A has the following remarkable structural features: (i) to posses the new ΔMeTyr unit, (ii) the geometry of its α,β dehydro amino acid is (E)(usually (Z)-configuration), (iii) to have the novel cinnamic acid derivative as acyl group. So far WS9326A has been found to antagonize the tracheal constrictions produced by exogenously added substance P(NK_1) and neurokinin A(NK_2), with IC_<50> values of 9.7×10^<-6>M and 3.5×10^<-6>M, respectively.
- 天然有機化合物討論会の論文
- 1991-09-07
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