GR-159897

Из Википедије, слободне енциклопедије
GR-159897
GR-159,897 chemical structure.png
IUPAC ime
5-fluoro-3-(2-(4-methoxy-4-([(R)-phenylsulphinyl]methyl)-1-piperidinyl)ethyl)-1H-indole
Identifikatori
CAS broj 158848-32-9 ДаY
PubChem CID 9555764
Hemijski podaci
Formula C23H27FN2O2S
Molarna masa 414.535 g/mol

GR-159,897 je potentni i selektivni antagonist NK2 receptora.[1] On ima anksiolitičko dejstvo u životinjskim modelima,[2] i takođe inhibira bronhokonstrikciju plućnih kanala, iz kog razloga on možda može da bude koristan u tretmanu astme.[3][4]

Reference[уреди]

  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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