Netupitant (CID-6451149) is a highly potent, selective and orally activeneurokinin-1 (NK₁)receptor antagonist with aK_iof 0.95 nM for hNK₁in CHO cells. Netupitant has antiemetic affect^[1][2][3].

Netupitant (CID-6451149) binds with high affinity the human NK₁receptor (pK_i=9.0) with more than 1000 fold selectivity over the NK₂and NK₃(pK_i=5.8 for both sites)^[2].
Netupitant (1, 10, 100 nM) concentration-dependently antagonizes the stimulatory effects of substance P (SP) showing insurmountable antagonism (pK_B=8.87) in CHO NK₁cells^[2].

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 NK₁agonist is dose-dependently counteracted by Netupitant given intraperitoneally (ID₅₀1.5mg/kg) or orally (ID₅₀0.5mg/kg)^[2].
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^[3].

578.59

Solid

C₃₀H₃₂F₆N₄O

290297-26-6

奈妥吡坦；萘妥吡坦

Room temperature in continental US; may vary elsewhere.

DMSO : 9.09 mg/mL(15.71 mM;ultrasonic and warming and heat to 60℃)

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