Home / NK2 Receptor Antagonists / GR 159897

GR 159897

Catalog #: 1274
4 Citations Datasheet / COA / SDS

Discontinued Product

1274 has been discontinued.
View all NK2 Receptor Antagonists products.
GR 159897 | CAS No. 158848-32-9 | NK2 Receptor Antagonists
1 Image
Description: Non-peptide, potent NK2 antagonist

Chemical Name: 5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole

Purity: ≥97%

Product Details
Citations (4)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

GR 159897 is 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of GlaxoSmithKline

Background References

  1. Neuropeptide signaling activates dendritic cell-mediated type 1 immune responses through neurokinin-2 receptor.
    Kitamura H, Kobayashi M, Wakita D, Nishimura T
    J. Immunol., 2012;188(9):4200-8.
  2. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  3. GR 159897, a potent non-peptide antagonist at tachykinin NK2 receptors.
    Beresford et al.
    Eur.J.Pharmacol., 1995;272:241
  4. 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
  5. 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
  6. The neuropeptide substance P regulates aldosterone secretion in human adrenals
    J Wils, C Duparc, AF Cailleux, AG Lopez, C Guiheneuf, I Boutelet, HG Boyer, C Dubessy, S Cherifi, B Cauliez, F Gobet, G Defortescu, JF Ménard, E Louiset, H Lefebvre
    Nat Commun, 2020;11(1):2673.

Product Datasheets

COA view current batch
Or select another batch:
View Batch
SDS
Reconstitution Calculator
Molarity Calculator

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Molarity Calculator

=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Citations for GR 159897

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

4 Citations: Showing 1 - 4

  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

FAQs

No product specific FAQs exist for this product, however you may

View all Small Molecule FAQs

Reviews for GR 159897

There are currently no reviews for this product. Be the first to review GR 159897 and earn rewards!

Have you used GR 159897?

Submit a review and receive an Amazon gift card.

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review
Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.