Signal Transduction
Stem Cells
Signaling Pathways
Product Type
All Products
New Products
Small Molecules
Peptides
Controlled Substances
Toxins
Caged Compounds
Fluorescent Probes
Screening Libraries
Ligand Sets
Other Product Types
Research Area
Cancer
Cardiovascular System
Endocrinology
Immunology
Neuroscience
Pain & Inflammation
Respiratory System
GR 159897Cat. No. 1274 |
Price and AvailabilityBy clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy. |
|
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.Licensing Information
Sold with the permission of GlaxoSmithKlineCertificate of Analysis / Safety Data Sheet
References
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.
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.
If you know of a relevant citation for this product please let us know.
View Related Products by Target
Keywords: GR 159897, supplier, Non-peptide, potents, NK2, antagonist, Tachykinin, Receptors, Neurokinin, GR159897, GlaxoSmithKline, GSK
Quick Order
Find multiple products by catalog number
Appetite Modulation
Written by Sonia A. Tucci, Lynsay Kobelis & Tim Kirkham. Request a copy or view PDF today.
Regulation of Vascular Reactivity by GPCRs
Written by J.J. Maguire and A.P. Davenport
'Regulation of Vascular Reactivity by G-protein-coupled Receptors' summarizes the key GPCRs regulating vascular reactivity.
7-TM Receptor Signaling
Written by T. Kenakin et al
'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy
Antidepressants - Current and Future Targets
Written by P. Skolnich et al
'Antidepressants - Current and Future Targets' provides an overview of the current and future targets for the treatment of major depressive disorder.
New Products in this Area
Potent NK1 receptor antagonist
20% Discount*
Potent, selective LRRK2 inhibitor
Tocris is the first to launch GSK2578215A, licensed from GlaxoSmithKline, for the study of Parkinson's Disease.