LY-503430
{{Short description|Chemical compound}}
{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 424901917
| IUPAC_name = 4'-{(1S)-1-fluoro-2-[(isopropylsulfonyl)amino]-1-methylethyl}-N-methylbiphenyl-4-carboxamide
| image = LY503430.svg
| width = 150px
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| legal_US = Investigational New Drug
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| routes_of_administration = Oral
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| CAS_number_Ref = {{cascite|correct|CAS}}
| CAS_number = 625820-83-9
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 3NKZ7DGF3R
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| PubChem = 9952446
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
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| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = 8128056
| C=20 | H=25 | F=1 | N=2 | O=3 | S=1
| SMILES = CC(C)S(=O)(=O)NCC(F)(C)c(cc2)ccc2-c(cc1)ccc1C(=O)NC
| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| StdInChIKey = MFJKNXILEXBWNQ-FQEVSTJZSA-N
| synonyms = LY-503430; (R)-4'-[1-fluoro-1-methyl-2-(propane-2-sulfonylamino)-ethyl]-biphenyl-4-carboxylic acid methylamide
}}
LY-503430 is an AMPA receptor positive allosteric modulator developed by Eli Lilly.{{cite journal | vauthors = O'Neill MJ, Murray TK, Clay MP, Lindstrom T, Yang CR, Nisenbaum ES | title = LY503430: pharmacology, pharmacokinetics, and effects in rodent models of Parkinson's disease | journal = CNS Drug Reviews | volume = 11 | issue = 1 | pages = 77–96 | year = 2005 | pmid = 15867954 | pmc = 6741716 | doi = 10.1111/j.1527-3458.2005.tb00037.x }}
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.{{cite journal | vauthors = 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 | display-authors = 6 | title = 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 = The Journal of Pharmacology and Experimental Therapeutics | volume = 306 | issue = 2 | pages = 752–62 | date = August 2003 | pmid = 12730350 | doi = 10.1124/jpet.103.049445 | s2cid = 86751458 }}{{cite journal | vauthors = Ryder JW, Falcone JF, Manro JR, Svensson KA, Merchant KM | title = 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 = The Journal of Pharmacology and Experimental Therapeutics | volume = 319 | issue = 1 | pages = 293–8 | date = October 2006 | pmid = 16803862 | doi = 10.1124/jpet.106.105734 | s2cid = 11732324 }} 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.{{cite journal | vauthors = O'Neill MJ, Bleakman D, Zimmerman DM, Nisenbaum ES | title = AMPA receptor potentiators for the treatment of CNS disorders | journal = Current Drug Targets. CNS and Neurological Disorders | volume = 3 | issue = 3 | pages = 181–94 | date = June 2004 | pmid = 15180479 | doi = 10.2174/1568007043337508 }}{{cite journal | vauthors = O'Neill MJ, Witkin JM | title = AMPA receptor potentiators: application for depression and Parkinson's disease | journal = Current Drug Targets | volume = 8 | issue = 5 | pages = 603–20 | date = May 2007 | pmid = 17504104 | doi = 10.2174/138945007780618517 }}
See also
References
{{Reflist|2}}
{{Ionotropic glutamate receptor modulators}}
Category:AMPA receptor positive allosteric modulators
Category:Drugs developed by Eli Lilly and Company
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