Shelf life (days): 1460.0
Formulation: A solid
Formal Name: (2R,4S)-N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-4-[(8aS)-hexahydro-6-oxopyrrolo[1,2-a]pyrazin-2(1H)-yl]-N-methyl-1-piperidinecarboxamide, (2Z)-2-butenedioate
Purity: ≥98%
Formula Markup: C31H35F7N4O2 / C4H4O4
Formula Weight: 744.707822
CAS Number: 579475-24-4
Notes: An NK1 receptor antagonist (Ki = 0.06 nM for the human receptor); selective for the NK1 receptor over a panel of 67 transporters, ion channels, and enzymes at 10 µM; inhibits substance P-induced calcium release in CHO cells expressing recombinant human NK1 (apparent pKB = 10.3); inhibits GR73632-induced foot tapping in gerbils (ID50 = 0.11, 0.09, 0.09, and 3.36 mg/kg when administered 1, 4, 8, or 24 hours prior to GR73632, respectively); inhibits GR73632-induced hindlimb scratching in gerbils; reduces the number of territorial postures in the human threat test, indicating anxiolytic-like activity, in marmosets at 1, 3, and 10 mg/kg