LY-503430

Last updated
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
  • 4'-{(1S)-1-fluoro-2-[(isopropylsulfonyl)amino]-1-methylethyl}-N-methylbiphenyl-4-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
Formula C20H25FN2O3S
Molar mass 392.49 g·mol−1
3D model (JSmol)
  • CC(C)S(=O)(=O)NCC(F)(C)c(cc2)ccc2-c(cc1)ccc1C(=O)NC
  • 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 X mark.svgN
  • Key:MFJKNXILEXBWNQ-FQEVSTJZSA-N X mark.svgN
 X mark.svgNYes check.svgY  (what is this?)    (verify)

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

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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. S2CID   86751458.
  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. S2CID   11732324.
  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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