Molecular structure of GR 159897, CAS Number: 158848-32-9
GR 159897 (CAS 158848-32-9)
See product citations (6)
Application:
GR 159897 is a compound that acts as an effective and selective NK2 receptor antagonist
CAS Number:
158848-32-9
Molecular Weight:
414.54
Molecular Formula:
C23H27FN2O2S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
GR 159897 is a compound that acts as an effective and selective NK-2R (NK2 receptor) antagonist. It has been demonstrated to compete for binding of [3H]GR100679 to hNK2-transfected CHO cells. Guinea pig studies have shown that the compound inhibits NK-2R-mediated contractions of the trachea.
GR 159897 (CAS 158848-32-9) References
- Relevance of aromatic residues in transmembrane segments V to VII for binding of peptide and nonpeptide antagonists to the human tachykinin NK(2) receptor. | Renzetti, AR., et al. 1999. J Pharmacol Exp Ther. 290: 487-95. PMID: 10411554
- NK(2)-receptor mediated contraction in monkey, guinea-pig and human airway smooth muscle. | Rizzo, CA., et al. 1999. Neuropeptides. 33: 27-34. PMID: 10657468
- Effect of YM-44781, YM-44778 and YM-49598, novel tachykinin antagonists, in a drug-induced bladder contraction model. | Choppin, A., et al. 2002. Pharmacology. 65: 96-102. PMID: 11937780
- Effects of neuropeptides on the sumatriptan-disturbed circulation in the optic nerve head of rabbits. | Gaspar, MN., et al. 2004. Pharmacology. 70: 152-9. PMID: 14752235
- Postsynaptic actions of substance P on rat periaqueductal grey neurons in vitro. | Drew, GM., et al. 2005. Neuropharmacology. 49: 587-95. PMID: 15921708
- Expression and coupling of neurokinin receptor subtypes to inositol phosphate and calcium signaling pathways in human airway smooth muscle cells. | Mizuta, K., et al. 2008. Am J Physiol Lung Cell Mol Physiol. 294: L523-34. PMID: 18203813
- A1 and A2a receptors mediate inhibitory effects of adenosine on the motor activity of human colon. | Fornai, M., et al. 2009. Neurogastroenterol Motil. 21: 451-66. PMID: 19019012
- Alteration of colonic excitatory tachykininergic motility and enteric inflammation following dopaminergic nigrostriatal neurodegeneration. | Pellegrini, C., et al. 2016. J Neuroinflammation. 13: 146. PMID: 27295950
- Role of transient receptor potential vanilloid 1 in the modulation of airway smooth muscle tone and calcium handling. | Yocum, GT., et al. 2017. Am J Physiol Lung Cell Mol Physiol. 312: L812-L821. PMID: 28336810
- NK2 and NK1 receptor-mediated effects of NKA and analogs on colon, bladder, and arterial pressure in anesthetized dogs. | Rupniak, NMJ., et al. 2018. Naunyn Schmiedebergs Arch Pharmacol. 391: 299-308. PMID: 29279967
- Differential consequences of neurokinin receptor 1 and 2 antagonists in metastatic breast carcinoma cells; Effects independent of Substance P. | Nizam, E. and Erin, N. 2018. Biomed Pharmacother. 108: 263-270. PMID: 30223097
- Prokinetic effects of the neurokinin NK2 receptor agonist [Lys5,MeLeu9,Nle10]-NKA(4-10) on bladder and colorectal activity in minipigs. | Rupniak, NMJ., et al. 2019. Neuropeptides. 77: 101956. PMID: 31324387
- NK1R antagonist decreases inflammation and metastasis of breast carcinoma cells metastasized to liver but not to brain; phenotype-dependent therapeutic and toxic consequences. | Nizam, E., et al. 2020. Cancer Immunol Immunother. 69: 1639-1650. PMID: 32322911
Inhibitor of:
NK-2R.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GR 159897, 5 mg | sc-361193 | 5 mg | $190.00 | |||
GR 159897, 25 mg | sc-361193A | 25 mg | $632.00 |