Netupitant (CID 6451149) is a specific neurokinin 1 (NK1) receptor antagonist (Ki: 0.95 nM).

NK1:0.95 nM(Ki)

Netupitant 在 CHO NK1 细胞中依赖浓度地对抗物质 P (SP) 的刺激效果，并展现出不可逾越的对抗作用（pKb：8.87）。在表达 NK2/3 受体的细胞中，Netupitant 无活性。

在小鼠中，SP的脊髓内注射引起的典型抓挠、咬合和舔舐反应可被Netupitant（1-10 mg/kg, i.p.）剂量依赖性地抑制。在沙鼠中，通过脑室内注射NK1激动剂引发的脚踏行为，可以通过腹腔内（ID50 1.5 mg/kg）或口服（ID50 0.5 mg/kg）给予Netupitant剂量依赖性地逆转。在沙鼠的时间进程实验中，Netupitant显示出了长效的作用。

zotarolimus (10 pM-1 μM) in buffer A (2% BSA and 0.2% Tween-20 in D-PBS) is used in the assay of Binding Affinity to FKBP12.

Cell lines: NG108-15 cells. Concentrations: 1,3,10,30 nM. Method:cells are preincubated for 1 h at 37℃ with either growth media alone(control) or media containing antagonists.Antagonist concentrations are at least 30-fold the Kd value to ensure receptor saturation.After preincubation,antagonists are removed and cells are rinsed with growth media alone for an additional hour to allow for dissociation of antagonists still bound to the receptor.Cell media are then replaced with isosmotic HEPES buffer (pH 7.4,20 mM) containing NaCl (130 mM),KCl (2 mM),MgCl2 (1 mM) CaCl2 (2 mM),Fluo-4 acetoxymethyl (AM) ester (2 mM),pluronic acid (0.04%) and SP at various concentrations in the 3 nM to 1 mM range.The final incubation lasted for 1 h at 37 ℃.Pluronic acid is added as a nonionic surfactant to sequester the AM ester molecules into micelles for cellular uptake.

Animal Models: Male Swiss mice. Formulation: Saline containing 5% DMSO and 5% Tween 80. Dosages: 1 and 10 mg/kg. Administration: i.p.