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GR-159,897
Systematic (IUPAC) name
5-Fluoro-3-(2-(4-methoxy-4-([(R)-phenylsulphinyl]methyl)-1-piperidinyl)ethyl)-1H-indole
Identifiers
CAS number 158848-32-9
ATC code  ?
PubChem 9555764
Chemical data
Formula C 23H27FN2O2S 
Mol. mass 414.535 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

GR-159,897 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]

References

  1. ^ Beresford IJ, Sheldrick RL, Ball DI, Turpin MP, Walsh DM, Hawcock AB, Coleman RA, Hagan RM, Tyers MB. GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors. European Journal of Pharmacology. 1995 Jan 16;272(2-3):241-8. PMID 7713168
  2. ^ Walsh DM, Stratton SC, Harvey FJ, Beresford IJ, Hagan RM. The anxiolytic-like activity of GR159897, a non-peptide NK2 receptor antagonist, in rodent and primate models of anxiety. Psychopharmacology (Berlin). 1995 Sep;121(2):186-91. PMID 8545524
  3. ^ Advenier C. Tachykinin NK2 receptors further characterized in the lung with nonpeptide receptor antagonists. Canadian Journal of Physiology and Pharmacology. 1995 Jul;73(7):878-84. PMID 8846425
  4. ^ Mizuta K, Gallos G, Zhu D, Mizuta F, Goubaeva F, Xu D, Panettieri RA Jr, Yang J, Emala CW Sr. 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. 2008 Mar;294(3):L523-34. PMID 18203813
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