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LY-503430

LY-503430
LY503430.svg
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
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC20H25FN2O3S
Molar mass392.49 g/mol g·mol−1
3D model (JSmol)
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LY-503430 is an AMPA receptor positive allosteric modulator developed by Eli Lilly.[1]

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. 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.