SNX-482 (ammonium salt)

肽类E/R型钙通道阻滞剂（在表达人类E类通道的192C细胞中IC50=30nM）；对E/R型钙通道具有选择性，而对A类和B类钙通道（IC50分别为>280和~800nM）以及电压门控钾通道Kv1.1、Kv1.2和Kv1.4（所有IC50=>140nM）则无选择性；抑制大鼠分离垂体后叶中的E/R型钙电流（IC50=4nM）；鞘内给药可抑制福尔马林诱导的NK1受体内化和同侧背角cfos表达，并减少福尔马林诱导的大鼠爪子退缩（0.5µg/只）。A peptide class E/R-type calcium channel blocker (IC50 = 30 nM in 192C cells expressing human class E channels); selective for class E/R-type over class A and class B calcium channels (IC50s = >280 and ~800 nM, respectively), as well as the voltage-gated potassium channels Kv1.1, Kv1.2, and Kv1.4 (IC50s = >140 nM for all); inhibits class E/R-type calcium currents in isolated rat posterior pituitary (IC50 = 4 nM); intrathecal administration inhibits formalin-induced NK1 receptor internalization and cfos expression in the ipsilateral dorsal horn and reduces formalin-induced paw flinching in rats at 0.5 µg/animal.分子式C192H274N52O60S7分子量4495O=C(N[C@@H](C(C)C)C(N[C@@H](CC(O)=O)C(N[C@@H](CCCCN[H])C(N[C@H](C(NCC(N[C@@H](CSSC[C@H](N1)C(N2CCC[C@H]2C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(NCC3=O)=O)CC(C)C)=O)=O)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC4=CC=C(O)C=C4)C(N[C@@H](CCSC)C(N[C@H](C(NCC(NCC(N[C@@H](CSSC[C@H](N3)C(N[C@@H](CC5=CNC=N5)C(N[C@@H](CO)C(N[C@H](C(N[C@H](C(N[C@@H](CO)C(N[C@@H](CC6=CC=C(O)C=C6)C7=O)=O)=O)CC8=CC=CC=C8)=O)CC(C)C)=O)=O)=O)C(N[C@@H](CO)C(N[C@@H](C(C)C)C(N[C@@H](CC(N)=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CSSC[C@H](N7)C(N[C@H](C(N[C@@H](CC9=CNC%10=C9C=CC=C%10)C(N[C@@H](CC(O)=O)C(N[C@H](C(N[C@]([C@H](O)C)([H])C(N[C@H](C(N[C@@H](CO)C(N[C@@H](CC(O)=O)C(O)=O)=O)=O)CC%11=CC=CC=C%11)=O)=O)CC(C)C)=O)=O)=O)C)=O)C1=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC%12=CC=CC=C%12)=O)=O)=O)=O)=O)=O)C)=O)=O)=O)CN[H]