[D-Arg1,D-Trp5,7,9,Leu11]-Substance P 是一种有效的小细胞肺癌 (SCLC) 细胞生长抑制剂,也作为神经肽拮抗剂,阻断多种神经肽(如血管加压素和缓激肽)刺激的集落形成。[D-Arg1,D-Trp5,7,9,Leu11]-Substance P 能够抑制血管加压素或缓激肽诱导的Ca2+动员及丝裂原活化蛋白激酶的活性。此外,[D-Arg1,D-Trp5,7,9,Leu11]-Substance P 在裸鼠体内能够抑制H-69异种移植瘤的生长。
YM49598 is a tachykinin receptor antagonist. YM49598 exhibited high binding affinities at NK(1) (pK(i) = 9.09 +/- 0.02) and NK(2) (pK(i) = 9.94 +/- 0.03) receptors, respectively. YM49598 was almost inactive but produced a potent inhibition (IC(50) = 11 +/