Abstract:
Substance P (SP) and its three analogs were synthesized through solid-phase procedure. The fully-protected peptideresin was cleaved with anhydrous HF. -SH of Cys in Cys
5,9 SP(4-11) was protected with Acm, then deprotected through Iodine oxdation method, the disulfide bridge cyclization was formed subsequently. The crude product was purified on C
18 RP-HPLC. The results of guinea-pig isolated ileum test (GPI) showed that the potency of the analogs was as follows: AcGln
5,Pro
9 SP(5-11) > SP > SP(4-11) > Cys
5,9 SP(4-11). They induced GPI to contract very fast and showed the characteristics of tachykinin. On the writhing test in mice, the results showed: Cys
5,9 SP(4-11) > SP > SP(4-11) > AcGln
5,Pro
9 SP(5-11). The biological tests showed that the SP analogs have some extent of selectivity.