GR-159897
Identifiers
  • 5-fluoro-3-(2-(4-methoxy-4-([(R)-phenylsulphinyl]methyl)-1-piperidinyl)ethyl)-1H-indole
CAS Number
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC23H27FN2O2S
Molar mass414.54 g·mol−1
3D model (JSmol)
  • c4ccccc4S(=O)CC2(OC)CCN(CC2)CCc(c1cc3F)c[nH]c1cc3
  • InChI=1S/C23H27FN2O2S/c1-28-23(17-29(27)20-5-3-2-4-6-20)10-13-26(14-11-23)12-9-18-16-25-22-8-7-19(24)15-21(18)22/h2-8,15-16,25H,9-14,17H2,1H3
  • Key:BANYJBHWTOJQDU-UHFFFAOYSA-N
  (verify)

GR-159897 is a potent and selective NK2 receptor antagonist drug.[1] It has anxiolytic effects in animal models,[2] and also inhibits bronchoconstriction of the airways, which may potentially make it useful in the treatment of asthma.[3][4]

See also

References

  1. ^ Beresford IJ, Sheldrick RL, Ball DI, Turpin MP, Walsh DM, Hawcock AB, et al. (January 1995). "GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors". European Journal of Pharmacology. 272 (2–3): 241–8. doi:10.1016/0014-2999(94)00655-q. PMID 7713168.
  2. ^ Walsh DM, Stratton SC, Harvey FJ, Beresford IJ, Hagan RM (September 1995). "The anxiolytic-like activity of GR159897, a non-peptide NK2 receptor antagonist, in rodent and primate models of anxiety". Psychopharmacology. 121 (2): 186–91. doi:10.1007/bf02245629. PMID 8545524. S2CID 7662905.
  3. ^ Advenier C (July 1995). "Tachykinin NK2 receptors further characterized in the lung with nonpeptide receptor antagonists". Canadian Journal of Physiology and Pharmacology. 73 (7): 878–84. doi:10.1139/y95-121. PMID 8846425.
  4. ^ Mizuta K, Gallos G, Zhu D, Mizuta F, Goubaeva F, Xu D, et al. (March 2008). "Expression and coupling of neurokinin receptor subtypes to inositol phosphate and calcium signaling pathways in human airway smooth muscle cells". American Journal of Physiology. Lung Cellular and Molecular Physiology. 294 (3): L523-34. doi:10.1152/ajplung.00328.2007. PMC 3650481. PMID 18203813.
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