Catalog Number: 4013
Chemical Name: 5-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl-N,N-dimethyl-1H-1,2,3-triazole-4-methanamine hydrochloride
Biological Activity
High affinity NK1 receptor antagonist (IC50 = 0.19 nM at human NK1 receptors). Selective (>300-fold) over h-NK2 and h-NK3 receptors. Exhibits anxiolytic and antidepressant-like effects. Orally active.
Technical Data
  • M.Wt:
    611.98
  • Formula:
    C26H28F7N5O2.HCl
  • Solubility:
    Soluble to 30 mM in water and to 50 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    188923-01-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Correlation of neurokinin (NK) 1 receptor occupancy in gerbil striatum with behavioral effects of NK1 antagonists.
    Duffy et al.
    J.Pharmacol.Exp.Ther., 2002;301:536
  2. An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.
    Harrison et al.
    J.Med.Chem., 2001;44:4296

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