Liu S Y, Zhong M N, Dong Y X, Li Y L, Yuan X M
Institute of Parmaceutical Chemistry, PLA, Beijing 102205.
Yao Xue Xue Bao. 1997 Dec;32(12):938-42.
Substance P (SP) and its three analogs were synthesized through solid-phase procedure. The fully-protected peptide-resin was cleaved with anhydrous HF.--SH of Cys in [Cys5,9] SP(4-11) was protected with Acm, then deprotected through Iodine oxidation method, the disulfide bridge cyclization was formed subsequently. The crude product was purified on C18 RP-HPLC. The results of guinea-pig isolated ileum test (GPI) showed that the potency of the analogs was as follows: [AcGln5, Pro9] SP(5-11) > SP > SP(4-11) > [Cys5,9] SP(4-11). They induced GPI to contract very fast and showed the characteristics of tachykinin. On the writing test in mice, the results showed: [Cys5,9] SP(4-11) > SP > SP(4-11) > [AcGln5, Pro9] SP(5-11). The biological tests showed that the SP analogs have some extent of selectivity.
通过固相法合成了P物质（SP）及其三种类似物。用无水HF切割完全保护的肽树脂。[Cys5,9] SP(4-11)中Cys的--SH用Acm保护，然后通过碘氧化法脱保护，随后形成二硫键环化。粗产物在C18反相高效液相色谱上纯化。豚鼠离体回肠试验（GPI）结果表明，类似物的效价如下：[AcGln5, Pro9] SP(5-11) > SP > SP(4-11) > [Cys5,9] SP(4-11)。它们能非常迅速地诱导GPI收缩，并表现出速激肽的特性。在小鼠书写试验中，结果显示：[Cys5,9] SP(4-11) > SP > SP(4-11) > [AcGln5, Pro9] SP(5-11)。生物学试验表明，SP类似物具有一定程度的选择性。
