Synonyms: 2-(3,5-bis(Trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-o-tolylpyridin-3-yl)propanamide; 2-[3,5-bis(Trifluoromethyl)phenyl]-N-[6-(4-methylpiperazin-1-yl)-4-o-tolylpyridin-3-yl]-N-methylisobutyramide; AGE 94200; AGE-94200; AGE94200; CID 6451149; CID-6451149; CID6451149; N,a,a-Trimethyl-N-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]-3,5-bis(trifluoromethyl)benzeneacetamide; Ro 67-31898; Ro 67-31898/000
Molecular Formula: C30H32F6N4O
Molecular Weight: 578.59
Linear Structural Formula: C30H32F6N4O
MDL Number: MFCD25976831
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: Netupitant is a brain-penetrant, orally active, potent and selective neurokinin-1 (NK1) receptor (NK1R; Tachykinin receptor 1) antagonist (Ca+2 mobilization IC50 = 11.2 nM/hNK1 vs. >1 muM/rNK1 & hNK2/3; hNK1/2/3 Ki = 0.95 nM/1.6 muM/1.6 muM) that effectively blocks agonist GR73632-induced foot tapping in gerbils (ID50 = 0.5 mg/kg po 2h prior to 3 pmol/5 muL GR73632/gerbil icv). In addition to antiemetic efficacy against substance P-associated vomiting reflexes, netupitant is also reported to enhance the analgesic effects of electroacupuncture (EA) among humanized mice with sickle cell disease in response to pain in vivo (10 mg/kg/day, i.p.).