Information Netupitant Netupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity. Targets Neurokinin-1 receptor In vitro In CHO NK1 cells, Netupitant concentration-dependently antagonizes the stimulatory effects of substance P (SP) showing insurmountable antagonism (pKB 8.87). In cells expressing NK2 or NK3 receptors, Netupitant is inactive. In vivo Netupitant behaves as a brain penetrant, orally active, potent and selective NK1 antagonist. In mice the intrathecal injection of SP elicited the typical scratching, biting and licking response that is dose-dependently inhibited by Netupitant given intraperitoneally in the 1-10 mg/kg dose range. In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of a NK1 agonist is dose-dependently counteracted by Netupitant given intraperitoneally (ID50 1.5 mg/kg) or orally (ID50 0.5 mg/kg). In time course experiments in gerbils Netupitant displayed long lasting effects. Cell Research(from reference) Cell lines：NG108-15 cells Concentrations：1, 3, 10, 30 nM Incubation Time：1 h
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Netupitant
CAS number：290297-26-6 molecular formula：C30H32F6N4O
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| Chinese alias | 奈妥匹坦 | ||
| English alias | KZVBBVPCVQEVQK-UHFFFAOYSA-N | UNII-7732P08TIR | NSC68808 | 1,3,3-Tetraethoxypropane | 2-(3,5-Bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-O-tolylpyridin-3-yl)propanamide, AldrichCPR | BENZENEACETAMIDE, N,.ALPHA.,.ALPHA.-TRIMETH | ||
| CAS number | 290297-26-6 | molecular formula | C30H32F6N4O |
| molecular weight | 578.59 g/mol | Exact mass | - |
| PSA | 39.700 Ų | logp | 6.8 |
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