LY-503,430

LY-503,430
Clinical data
Routes of
administration
oral
Legal status
Legal status
  • Investigational New Medicine
Identifiers
Synonyms LY-503,430; (R)-4'-[1-fluoro-1-methyl-2-(propane-2-sulfonylamino)-ethyl]-biphenyl-4-carboxylic acid methylamide
CAS Number 625820-83-9 YesY
PubChem (CID) 9952446
ChemSpider 8128056
Chemical and physical data
Formula C20H25FN2O3S
Molar mass 392.49 g/mol
3D model (Jmol) Interactive image
  (verify)

LY-503,430 is an ampakine drug developed by Eli Lilly.[1]

LY-503,430 produces both nootropic and neuroprotective effects, reducing brain damage caused by 6-hydroxydopamine or MPTP and also increasing levels of the neurotrophic factor BDNF in the brain, particularly in the substantia nigra, hippocampus and striatum.[2][3] It is orally active and the main application it is currently being developed for is treatment of Parkinson's Disease although it has also been proposed to be useful in the treatment of Alzheimer's Disease, depression and schizophrenia.[4][5]

References

  1. O'neill, MJ; Murray, TK; Clay, MP; Lindstrom, T; Yang, CR; Nisenbaum, ES (2005). "LY503430: pharmacology, pharmacokinetics, and effects in rodent models of Parkinson's disease". CNS Drug Reviews. 11 (1): 77–96. doi:10.1111/j.1527-3458.2005.tb00037.x. PMID 15867954.
  2. Murray, TK; Whalley, K; Robinson, CS; Ward, MA; Hicks, CA; Lodge, D; Vandergriff, JL; Baumbarger, P; et al. (2003). "LY503430, a novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor potentiator with functional, neuroprotective and neurotrophic effects in rodent models of Parkinson's disease". The Journal of Pharmacology and Experimental Therapeutics. 306 (2): 752–62. doi:10.1124/jpet.103.049445. PMID 12730350.
  3. Ryder, JW; Falcone, JF; Manro, JR; Svensson, KA; Merchant, KM (2006). "Pharmacological characterization of cGMP regulation by the biarylpropylsulfonamide class of positive, allosteric modulators of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors". The Journal of Pharmacology and Experimental Therapeutics. 319 (1): 293–8. doi:10.1124/jpet.106.105734. PMID 16803862.
  4. O'neill, MJ; Bleakman, D; Zimmerman, DM; Nisenbaum, ES (2004). "AMPA receptor potentiators for the treatment of CNS disorders". Current drug targets. CNS and neurological disorders. 3 (3): 181–94. doi:10.2174/1568007043337508. PMID 15180479.
  5. O'neill, MJ; Witkin, JM (2007). "AMPA receptor potentiators: application for depression and Parkinson's disease". Current drug targets. 8 (5): 603–20. doi:10.2174/138945007780618517. PMID 17504104.



This article is issued from Wikipedia - version of the 5/9/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.