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 (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. PMID 15867954.
- ^ Murray, TK; Whalley, K; Robinson, CS; Ward, MA; Hicks, CA; Lodge, D; Vandergriff, JL; Baumbarger, P et al. (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.
- ^ Ryder, JW; Falcone, JF; Manro, JR; Svensson, KA; Merchant, KM (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.
- ^ O'neill, MJ; Bleakman, D; Zimmerman, DM; Nisenbaum, ES (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.
- ^ O'neill, MJ; Witkin, JM (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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Agonists: Glutamate/acite site competitive agonists: Aspartate • Glutamate • Homoquinolinic acid • Ibotenic acid • NMDA • Quinolinic acid • Tetrazolylglycine; Glycine site agonists: ACBD • ACPC • ACPD • Alanine • CCG • Cycloserine • DHPG • Fluoroalanine • Glycine • HA-966 • L-687,414 • Milacemide • Sarcosine • Serine • Tetrazolylglycine; Polyamine site agonists: Acamprosate • Spermidine • Spermine
Antagonists: Competitive antagonists: AP5 (APV) • AP7 • CGP-37849 • CGP-39551 • CGP-39653 • CGP-40116 • CGS-19755 • CPP • LY-233,053 • LY-235,959 • LY-274,614 • MDL-100,453 • Midafotel (d-CPPene) • NPC-12,626 • NPC-17,742 • PBPD • PEAQX • Perzinfotel • PPDA • SDZ-220581 • Selfotel; Noncompetitive antagonists: ARR-15,896 • Caroverine • Dexanabinol • FPL-12495 • FR-115,427 • Hodgkinsine • Magnesium • MDL-27,266 • NPS-1506 • Psychotridine • Zinc; Uncompetitive pore blockers: 2-MDP • 3-MeO-PCP • 8A-PDHQ • Alaproclate • Amantadine • Aptiganel • ARL-12,495 • ARL-15,896-AR • ARL-16,247 • Budipine • Delucemine • Dexoxadrol • Dextrallorphan • Dieticyclidine • Dizocilpine • Endopsychosin • Esketamine • Etoxadrol • Eticyclidine • Gacyclidine • Ibogaine • Indantadol • Ketamine • Ketobemidone • Loperamide • Memantine • Meperidine (Pethidine) • Methadone • Methorphan ( Dextromethorphan, Levomethorphan) • Methoxetamine • Milnacipran • Morphanol ( Dextrorphan, Levorphanol) • NEFA • Neramexane • Nitrous oxide • Noribogaine • Orphenadrine • PCPr • Phencyclamine • Phencyclidine • Propoxyphene • Remacemide • Rhynchophylline • Riluzole • Rimantadine • Rolicyclidine • Sabeluzole • Tenocyclidine • Tiletamine • Tramadol • Xenon; Glycine site antagonists: ACEA-1021 • ACEA-1328 • ACPC • Carisoprodol • CGP-39653 • CKA • DCKA • Felbamate • Gavestinel • GV-196,771 • Kynurenic acid • L-689,560 • L-701,324 • Lacosamide • Licostinel • LU-73,068 • MDL-105,519 • Meprobamate • MRZ 2/576 • PNQX • ZD-9379; NR2B subunit antagonists: Besonprodil • CO-101,244 (PD-174,494) • CP-101,606 • Eliprodil • Haloperidol • Ifenprodil • Isoxsuprine • Nylidrin • Ro8-4304 • Ro25-6981 • Traxoprodil; Polyamine site antagonists: Arcaine • Co 101676 • Diaminopropane • Acamprosate • Diethylenetriamine • Huperzine A • Putrescine • Ro 25-6981; Unclassified/unsorted antagonists: Chloroform • Diethyl ether • Enflurane • Ethanol (Alcohol) • Halothane • Isoflurane • Methoxyflurane • Toluene • Trichloroethane • Trichloroethanol • Trichloroethylene • Xylene
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Transporter
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