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Netupitant

CAS No. : 290297-26-6

MCE 站：Netupitant

产品活性：Netupitant (CID-6451149) 是高效、选择性、具有口服活性的 Neurokinin-1 受体 (NK₁) 拮抗剂，在 CHO 细胞中对 hNK₁ 的 K_i 值为 0.95 nM。Netupitant 具有止吐作用。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Neurokinin Receptor

In Vitro: Netupitant (CID-6451149) binds with high affinity the human NK₁ receptor (pK_i=9.0) with more than 1000 fold selectivity over the NK₂ ａnd NK₃ (pK_i=5.8 for both sites).
Netupitant (1, 10, 100 nM) concentration-dependently antagonizes the stimulatory effects of substance P (SP) showing insurmountable antagonism (pK_B=8.87) in CHO NK₁ cells.

In Vivo: Netupitant (CID-6451149; 1-10 mg/kg; ip) dose-dependently inhibits SP-elicited the typical scratching, biting ａnd licking response in mice. In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of a NK₁ agonist is dose-dependently counteracted by Netupitant given intraperitoneally (ID₅₀ 1.5mg/kg) or orally (ID₅₀ 0.5mg/kg).
Netupitant (0.1-3 mg/kg; i.v.) produces a concentration-dependent inhibition (mean pK_B=9.24) of the responses to SP-methylester (SP-OMe) in the detrusor muscle. Netupitant decreases the frequency of reflex bladder contractions.

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