Date published: 2026-5-20

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GR 231118 (CAS 158859-98-4)

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Application:
GR 231118 is a potent NPY1-R antagonist and NPY4-R agonist
CAS Number:
158859-98-4
Molecular Weight:
2352.77
Molecular Formula:
C110H170N34O24
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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GR 231118 is a synthetic compound known for its role as a selective antagonist and partial agonist for the neurokinin-1 (NK1) and neurokinin-2 (NK2) receptors, respectively. These receptors are part of the tachykinin receptor family, which primarily bind neuropeptides like substance P and neurokinin A, involved in mediating various physiological responses including inflammation, pain perception, and vascular responses. GR 231118 has been particularly instrumental in research focusing on the neurochemical pathways of pain and inflammation. By blocking the NK1 receptor, GR 231118 inhibits the binding of substance P, a neuropeptide associated with pain transmission and inflammatory processes, thereby providing insights into potential mechanisms for new analgesic and anti-inflammatory drugs. Its partial agonistic effect on NK2 receptors, which primarily interact with neurokinin A, allows researchers to explore the balance between receptor inhibition and activation, offering a nuanced understanding of receptor dynamics in biological systems. This dual functionality makes GR 231118 a valuable tool in neuropharmacological research, aiding in the elucidation of complex signaling pathways that can lead to novel therapeutic strategies for managing pain and inflammatory diseases, strictly within a research context without implying clinical or pharmaceutical applications.


GR 231118 (CAS 158859-98-4) References

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  2. 8-Amino-5-nitro-6-phenoxyquinolines: potential non-peptidic neuropeptide Y receptor ligands.  |  Wielgosz-Collin, G., et al. 2002. J Enzyme Inhib Med Chem. 17: 449-53. PMID: 12683683
  3. Activation of neuropeptide Y Y1 receptors inhibits glutamate release through reduction of voltage-dependent Ca2+ entry in the rat cerebral cortex nerve terminals: suppression of this inhibitory effect by the protein kinase C-dependent facilitatory pathway.  |  Wang, SJ. 2005. Neuroscience. 134: 987-1000. PMID: 16026936
  4. Metastin (KiSS-1) mimetics identified from peptide structure-activity relationship-derived pharmacophores and directed small molecule database screening.  |  Orsini, MJ., et al. 2007. J Med Chem. 50: 462-71. PMID: 17266198
  5. NPY family of hormones: clinical relevance and potential use in gastrointestinal disease.  |  Vona-Davis, LC. and McFadden, DW. 2007. Curr Top Med Chem. 7: 1710-20. PMID: 17979780
  6. Role of the ventromedial hypothalamic orexin-1 receptors in regulation of gastric Acid secretion in conscious rats.  |  Eliassi, A., et al. 2009. J Neuroendocrinol. 21: 177-82. PMID: 19207823
  7. Gastric acid secretion induced by paraventricular nucleus microinjection of orexin A is mediated through activation of neuropeptide Yergic system.  |  Kermani, M. and Eliassi, A. 2012. Neuroscience. 226: 81-8. PMID: 22986171
  8. Neuropeptide Y activity in the nucleus accumbens modulates feeding behavior and neuronal activity.  |  van den Heuvel, JK., et al. 2015. Biol Psychiatry. 77: 633-41. PMID: 25109664
  9. Orexin-A signaling in the paraventricular nucleus promote gastric acid secretion and gastric motility through the activation neuropeptide Y Y1 receptors and modulated by the hypothalamic lateral area.  |  Wang, C., et al. 2019. Neuropeptides. 74: 24-33. PMID: 30700376
  10. GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists.  |  Parker, EM., et al. 1998. Eur J Pharmacol. 349: 97-105. PMID: 9669502

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

GR 231118, 500 µg

sc-361194
500 µg
$345.00