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LY-503430

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
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
  • 4'-{(1S)-1-fluoro-2-[(isopropylsulfonyl)amino]-1-methylethyl}-N-methylbiphenyl-4-carboxamide
CAS Number
PubChemCID
ChemSpider
UNII
Chemical and physical data
FormulaC20H25FN2O3S
Molar mass392.49 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 ☒N
  • Key:MFJKNXILEXBWNQ-FQEVSTJZSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

LY-503430 is anAMPA receptorpositive allosteric modulator developed byEli Lilly.[1]

LY-503430 produces bothnootropic andneuroprotective effects, reducing brain damage caused by6-hydroxydopamine orMPTP and also increasing levels of the neurotrophic factorBDNF in the brain, particularly in thesubstantia nigra,hippocampus, andstriatum.[2][3] It is orally active and the main application it is currently being developed for is treatment ofParkinson's disease, although it has also been proposed to be useful in the treatment ofAlzheimer's disease,depression, andschizophrenia.[4][5]

See also

[edit]

References

[edit]
  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.
AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KARTooltip Kainate receptor
NMDARTooltip N-Methyl-D-aspartate receptor


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