Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no effect in bioassays for NK2 and NK3 receptors. The antagonism exerted by Nolpitantium toward NK1 receptors was apparently non-competitive, with pD2' values between 9.65 and 10.16 in the different assays. Nolpitantium also blocked in vitro [Sar9, Met(O2)11]substance P-induced release of acetylcholine from rat striatum. In vivo, Nolpitantium exerted highly potent antagonism toward [Sar9, Met(O2)11]substance P-induced hypotension in dogs, bronchoconstriction in guinea-pig) and plasma extrava......
Cimicifugic acid D (2-Caffeoylpiscidic acid) 是一种苄基酒石酸酯,能够诱导预收缩的大鼠主动脉条血管扩张,并启动内皮依赖性舒张机制。在Norepinephrine引起的大鼠主动脉条收缩过程中,Cimicifugic acid D 通过抑制受体操纵的Ca2+通道(ROC)的胞外Ca2+内流发挥作用,而不影响电压依赖性Ca2+通道(VDC)或K+诱导的收缩。