LY-503,430
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LY-503,430
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| Systematic (IUPAC) name | |
| (R)-4'-[1-fluoro-1-methyl-2-(propane-2-sulfonylamino)-ethyl]-biphenyl-4-carboxylic acid methylamide | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | ? |
| Chemical data | |
| Formula | C20H25FN2O3S |
| Mol. mass | 392.49 g/mol |
| SMILES | & |
| Synonyms | LY-503,430 |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status |
Investigational New Medicine |
| Routes | oral |
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]
[edit] References
- ^ O'Neill MJ, Murray TK, Clay MP, Lindstrom T, Yang CR, Nisenbaum ES. LY503430: pharmacology, pharmacokinetics, and effects in rodent models of Parkinson's disease. CNS Drug Reviews. 2005 Spring;11(1):77-96. PMID 15867954
- ^ Murray TK, Whalley K, Robinson CS, Ward MA, Hicks CA, Lodge D, Vandergriff JL, Baumbarger P, Siuda E, Gates M, Ogden AM, Skolnick P, Zimmerman DM, Nisenbaum ES, Bleakman D, O'Neill MJ. 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. Journal of Pharmacology and Experimental Therapeutics. 2003 Aug;306(2):752-62. PMID 12730350
- ^ Ryder JW, Falcone JF, Manro JR, Svensson KA, Merchant KM. Pharmacological characterization of cGMP regulation by the biarylpropylsulfonamide class of positive, allosteric modulators of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors. Journal of Pharmacology and Experimental Therapeutics. 2006 Oct;319(1):293-8. PMID 16803862
- ^ O'Neill MJ, Bleakman D, Zimmerman DM, Nisenbaum ES. AMPA receptor potentiators for the treatment of CNS disorders. Current Drug Targets. CNS and Neurological Disorders. 2004 Jun;3(3):181-94. PMID 15180479
- ^ O'Neill MJ, Witkin JM. AMPA receptor potentiators: application for depression and Parkinson's disease. Current Drug Targets. 2007 May;8(5):603-20. PMID 17504104
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