| 词条 | LY-503430 |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 424901917 | IUPAC_name = 4'(1S)-1-fluoro-2-[(isopropylsulfonyl)amino]-1-methylethylN-methylbiphenyl-4-carboxamide | image = LY503430.svg | width = 150px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = Investigational New Drug | legal_status = | routes_of_administration = Oral | bioavailability = | protein_bound = | metabolism = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 625820-83-9 | ATC_prefix = | ATC_suffix = | PubChem = 9952446 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 8128056 | C=20 | H=25 | F=1 | N=2 | O=3 | S=1 | molecular_weight = 392.49 g/mol | 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.[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
References1. ^{{cite journal |doi=10.1111/j.1527-3458.2005.tb00037.x |pmid=15867954 |year=2005 |last1=O'neill |first1=MJ |last2=Murray |last3=Clay |last4=Lindstrom |last5=Yang |last6=Nisenbaum |title=LY503430: pharmacology, pharmacokinetics, and effects in rodent models of Parkinson's disease |volume=11 |issue=1 |pages=77–96 |journal=CNS Drug Reviews |first2=TK |first3=MP |first4=T |first5=CR |first6=ES}} {{Nootropics}}{{Ionotropic glutamate receptor modulators}}{{nervous-system-drug-stub}}2. ^{{cite journal |pmid=12730350 |year=2003 |last1=Murray |first1=TK |last2=Whalley |last3=Robinson |last4=Ward |last5=Hicks |last6=Lodge |last7=Vandergriff |last8=Baumbarger |last9=Siuda |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 |volume=306 |issue=2 |pages=752–62 |doi=10.1124/jpet.103.049445 |journal=The Journal of Pharmacology and Experimental Therapeutics |first2=K |first3=CS |first4=MA |first5=CA |first6=D |first7=JL |first8=P |first9=E|last10=Gates |first10=M |last11=Ogden |first11=A. M. |last12=Skolnick |first12=P |last13=Zimmerman |first13=D. M. |last14=Nisenbaum |first14=E. S. |last15=Bleakman |first15=D |last16=O'Neill |first16=M. J. |display-authors=8 }} 3. ^{{cite journal |pmid=16803862 |year=2006 |last1=Ryder |first1=JW |last2=Falcone |last3=Manro |last4=Svensson |last5=Merchant |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 |volume=319 |issue=1 |pages=293–8 |doi=10.1124/jpet.106.105734 |journal=The Journal of Pharmacology and Experimental Therapeutics |first2=JF |first3=JR |first4=KA |first5=KM}} 4. ^{{cite journal |pmid=15180479 |year=2004 |last1=O'neill |first1=MJ |last2=Bleakman |last3=Zimmerman |last4=Nisenbaum |title=AMPA receptor potentiators for the treatment of CNS disorders |volume=3 |issue=3 |pages=181–94 |journal=Current Drug Targets. CNS and Neurological Disorders |doi=10.2174/1568007043337508 |first2=D |first3=DM |first4=ES}} 5. ^{{cite journal |pmid=17504104 |year=2007 |last1=O'neill |first1=MJ |last2=Witkin |title=AMPA receptor potentiators: application for depression and Parkinson's disease |volume=8 |issue=5 |pages=603–20 |journal=Current Drug Targets |doi=10.2174/138945007780618517 |first2=JM}} 6 : AMPA receptor positive allosteric modulators|Benzamides|Eli Lilly and Company|Experimental drugs|Organofluorides|Sulfonamides |
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