GR 159897

Pricing Availability   Qty
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% (HPLC)
Citations (4)
Literature (2)

Biological Activity for GR 159897

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.

Licensing Information

Sold with the permission of GlaxoSmithKline

Technical Data for GR 159897

M. Wt 414.54
Formula C23H27FN2O2S
Storage Desiccate at -20°C
Purity ≥97% (HPLC)
CAS Number 158848-32-9
PubChem ID 9953599
Smiles FC1=CC=C2C(C(CCN3CCC(C[S@@+]([O-])C4=CC=CC=C4)(OC)CC3)=CN2)=C1

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.

Solubility Data for GR 159897

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 20.73 50
ethanol 4.15 10

Preparing Stock Solutions for GR 159897

The following data is based on the product molecular weight 414.54. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.82 mL 24.12 mL 48.25 mL
2.5 mM 0.96 mL 4.82 mL 9.65 mL
5 mM 0.48 mL 2.41 mL 4.82 mL
25 mM 0.1 mL 0.48 mL 0.96 mL

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Product Datasheets for GR 159897

Certificate of Analysis / Product Datasheet
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References for GR 159897

References are publications that support the biological activity of the product.

Beresford et al (1995) GR 159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur.J.Pharmacol. 272 241 PMID: 7713168

Walsh et al (1995) The anxiolytic-like activity of GR 159897, a non-peptide NK2 receptor antagonist, in rodent and primate models of anxiety. Psychopharmacology 121 186 PMID: 8545524

Cooper et al (1994) GR 159897 and related analogues as highly potent, orally active non-peptide neurokinin NK2 receptor antagonists. Bioorg.Med.Chem.Lett. 4 1951

If you know of a relevant reference for GR 159897, please let us know.

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Keywords: GR 159897, GR 159897 supplier, Non-peptide, potents, NK2, antagonist, Tachykinin, Receptors, Neurokinin, GR159897, GlaxoSmithKline, GSK, Receptor, 1274, Tocris Bioscience

4 Citations for GR 159897

Citations are publications that use Tocris products. Selected citations for GR 159897 include:

Cunin et al (2011) 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. J Immunol 186 4175 PMID: 21368235

Grant (2012) Tachykinins stimulate a subset of mouse taste cells. Cell Commun Signal 7 e31697 PMID: 22363709

Kojima et al (2012) A role for endogenous peptide YY in tachykinin NK(2) receptor-triggered 5-HT release from guinea pig isolated colonic mucosa. Br J Pharmacol 167 1362 PMID: 22758653

Hegde et al (2010) Neurokinin-1 receptor antagonist treatment in polymicrobial sepsis: molecular insights. Int J Inflam 2010 601098 PMID: 21188216

Do you know of a great paper that uses GR 159897 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Peptides Involved in Appetite Modulation Scientific Review

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Depression Poster

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.