Piotrowski W, Devoy M A, Jordan C C, Foreman J C
Agents Actions. 1984 Apr;14(3-4):420-4. doi: 10.1007/BF01973842.
(D-Pro4 D- Trp7 ,9,10)SP4-11 (SPA) has been shown to be a competitive antagonist of the histamine releasing action of substance P in rat peritoneal mast cells. Antagonist activity of SPA is expressed in the concentration range 1 to 10 microM, but at higher concentrations SPA releases histamine. SPA inhibits the flare response induced by substance P in human skin but is without effect on the wheal response. Up to 12.5 pmol SPA produces neither wheal nor flare response by itself. The structurally related peptide, kassinin , does not cause histamine release from rat mast cells at concentrations up to 10 microM whereas the methyl ester of substance P was found to 1.6 times more active than substance P in this respect. The findings are discussed in terms of the classification of substance P receptors and the mechanism of wheal and flare in human skin.
（D-脯氨酸4、D-色氨酸7、9、10）SP4-11（SPA）已被证明是大鼠腹膜肥大细胞中P物质组胺释放作用的竞争性拮抗剂。SPA的拮抗活性在1至10微摩尔浓度范围内表现出来，但在更高浓度下SPA会释放组胺。SPA抑制P物质在人体皮肤中诱导的风团反应，但对红斑反应无影响。高达12.5皮摩尔的SPA自身既不产生风团反应也不产生红斑反应。结构相关肽蛙皮素在浓度高达10微摩尔时不会引起大鼠肥大细胞释放组胺，而P物质甲酯在这方面的活性比P物质高1.6倍。根据P物质受体的分类以及人体皮肤中风团和红斑的机制对这些发现进行了讨论。
