Catalog Number: 2394
Chemical Name: 1-[[(2-Nitrophenyl)amino]carbonyl]-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-L-alaninamide
Biological Activity
Highly selective human tachykinin NK1 receptor antagonist (IC50 values are 0.62 and 451 nM for human and rat receptors respectively) that displays > 130-fold selectivity over human NK2 and NK3 receptors. Potently antagonizes SP-induced Ca2+ efflux in vitro and inhibits mechanical hyperalgesia in vivo.
Technical Data
  • M.Wt:
    579.65
  • Formula:
    C33H33N5O5
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    180046-99-5
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. Comparative, general pharmacology of SDZ NKT 343, a novel, selective NK1 receptor antagonist.
    Walpole et al.
    Br.J.Pharmacol., 1998;124:83
  2. 2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N-methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models.
    Walpole et al.
    J.Med.Chem., 1998;41:3159
  3. Selective neurokinin-1 receptor antagonists are anti-hyperalgesic in a model of neuropathic pain in the guinea-pig.
    Campbell et al.
    Neuroscience., 1998;87:527

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