Catalog Number: 1274
Chemical Name: 5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole
Biological Activity
A potent, selective, non-peptide, orally active neurokinin NK2 receptor antagonist. Competes for binding of [3H]GR100679 to hNK2-transfected CHO cells with a pKi of 9.5. Inhibits NK2 receptor-mediated contraction of guinea pig trachea with a pA2 of 8.7. Anxiolytic in vivo.
Technical Data
  • M.Wt:
    414.54
  • Formula:
    C23H27FN2O2S
  • Solubility:
    Soluble to 50 mM in DMSO and to 10 mM in ethanol
  • Purity:
    >97%
  • Storage:
    Desiccate at -20°C
  • CAS No:
    158848-32-9
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.
Additional Information
Licensing Caveats:
Sold with the permission of GlaxoSmithKline
Background References
  1. GR 159897, a potent non-peptide antagonist at tachykinin NK2 receptors.
    Beresford et al.
    Eur.J.Pharmacol., 1995;272:241
  2. The anxiolytic-like activity of GR 159897, a non-peptide NK2 receptor antagonist, in rodent and primate models of anxiety.
    Walsh et al.
    Psychopharmacology, 1995;121:186
  3. GR 159897 and related analogues as highly potent, orally active non-peptide neurokinin NK2 receptor antagonists.
    Cooper et al.
    Bioorg.Med.Chem.Lett., 1994;4:1951
Citations:

The citations listed below are publications that use Tocris products. Selected citations for GR 159897 include:

4 Citations: Showing 1 - 4
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  1. Tachykinins stimulate a subset of mouse taste cells.
    Authors: Grant
    Cell Commun Signal 2012;7:e31697
  2. A role for endogenous peptide YY in tachykinin NK(2) receptor-triggered 5-HT release from guinea pig isolated colonic mucosa.
    Authors: Kojima Et al.
    Br J Pharmacol 2012;167:1362
  3. The tachykinins substance P and hemokinin-1 favor the generation of human memory Th17 cells by inducing IL-1β, IL-23, and TNF-like 1A expression by monocytes.
    Authors: Cunin Et al.
    J Immunol 2011;186:4175
  4. Neurokinin-1 receptor antagonist treatment in polymicrobial sepsis: molecular insights.
    Authors: Hegde Et al.
    Int J Inflam 2010;2010:601098

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