LY-404187: Difference between revisions

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| legal_status = Investigational New Medicine

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| molecular_weight = 342.45 g/mol

| smiles = N#Cc2ccc(cc2)-c1ccc(C(C)CNS(=O)(=O)C(C)C)cc1

'''LY-404,187''' (or '''LY404187''') is an [[ampakine]] (or "AMPA receptor potentiator") developed by [[Eli Lilly and Company]].<ref name="pmid15864556">{{cite journal |author=Jones N, O'Neill MJ, Tricklebank M, Libri V, Williams SC |title=Examining the neural targets of the AMPA receptor potentiator LY404187 in the rat brain using pharmacological magnetic resonance imaging |journal=Psychopharmacology (Berl.) |volume=180 |issue=4 |pages=743–51 |year=2005 |month=August |pmid=15864556 |doi=10.1007/s00213-005-2254-y}}</ref> It is a member of the biarylpropylsulfonamide class of ampakines.<ref name="pmid16803862">{{cite journal |author=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=J. Pharmacol. Exp. Ther. |volume=319 |issue=1 |pages=293–8 |year=2006 |month=October |pmid=16803862 |doi=10.1124/jpet.106.105734 |url=http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=16803862}}</ref>

LY-404,187 has been demonstrated to enhance cognitive function in animal studies, and has also shown effects suggesting [[antidepressant]] action as well as having possible application in the treatment of [[schizophrenia]], [[Parkinson's disease]] and [[ADHD]]. These effects appear to be mediated through multiple mechanisms of action secondary to AMPA receptor potentiation, with a prominent effect seen in research being increased levels of [[BDNF]] in the brain.<ref>Quirk JC, Nisenbaum ES. LY404187: a novel positive allosteric modulator of AMPA receptors. ''CNS Drug Reviews''. 2002 Fall;8(3):255-82. PMID 12353058</ref> It may therefore be continued on to human trials, although Eli Lilly has developed a whole family of biarylpropylsulfonamide derivatives and it is unclear at this stage which compound is most likely to be selected for further development.<ref>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</ref><ref>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</ref>

{{reflist}}

{{Glutamate receptor ligands}}

[[Category:Eli Lilly and Company]]

[[Category:Ampakines]]