LY-503430

LY-503430 is an AMPA receptor positive allosteric modulator developed by Eli Lilly.[1]

LY-503430
Clinical data
Other namesLY-503430; (R)-4'-[1-fluoro-1-methyl-2-(propane-2-sulfonylamino)-ethyl]-biphenyl-4-carboxylic acid methylamide
Routes of
administration		Oral
Legal status
Legal status
Identifiers
IUPAC name
  • 4'-{(1S)-1-fluoro-2-[(isopropylsulfonyl)amino]-1-methylethyl}-N-methylbiphenyl-4-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC20H25FN2O3S
Molar mass392.49 g·mol−1
3D model (JSmol)
SMILES
  • CC(C)S(=O)(=O)NCC(F)(C)c(cc2)ccc2-c(cc1)ccc1C(=O)NC
InChI
  • InChI=1S/C20H25FN2O3S/c1-14(2)27(25,26)23-13-20(3,21)18-11-9-16(10-12-18)15-5-7-17(8-6-15)19(24)22-4/h5-12,14,23H,13H2,1-4H3,(H,22,24)/t20-/m0/s1 N
  • Key:MFJKNXILEXBWNQ-FQEVSTJZSA-N N
 NY (what is this?)  (verify)

LY-503430 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]

See also

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. PMC 6741716. PMID 15867954.
  2. Murray TK, Whalley K, Robinson CS, Ward MA, Hicks CA, Lodge D, et al. (August 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 (October 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 (June 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 (May 2007). "AMPA receptor potentiators: application for depression and Parkinson's disease". Current Drug Targets. 8 (5): 603–20. doi:10.2174/138945007780618517. PMID 17504104.


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