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{{Short description|Chemical compound}} |
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{{Drugbox |
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{{Drugbox |
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| verifiedrevid = 424670500 |
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| verifiedrevid = 449869240 |
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| IUPAC_name = ''N''-propane-2-sulfonamide |
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| IUPAC_name = ''N''-propane-2-sulfonamide |
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| image = LY404187.png |
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| image = LY-404187.svg |
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| width = 200 |
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| width = 250px |
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<!--Clinical data--> |
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<!--Clinical data--> |
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| tradename = |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| pregnancy_category = |
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| pregnancy_category = |
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| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> |
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| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> |
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| legal_CA = <!-- Schedule I --> |
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| legal_CA = <!-- Schedule I --> |
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| legal_UK = <!-- Class A --> |
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| legal_UK = <!-- Class A --> |
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| legal_US = |
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| legal_US = Investigational New Drug |
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| legal_status = Investigational New Medicine |
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<!--Pharmacokinetic data--> |
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<!--Pharmacokinetic data--> |
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| bioavailability = |
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<!--Identifiers--> |
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<!--Identifiers--> |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = 211311-95-4 |
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| CAS_number = 211311-95-4 |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| ATC_prefix = |
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| UNII = 75W6I8W6OU |
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| ATC_prefix = none |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} |
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| ChemSpiderID = 18962921 |
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<!--Chemical data--> |
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<!--Chemical data--> |
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| C=19 | H=22 | N=2 | O=2 | S=1 |
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| C=19 | H=22 | N=2 | O=2 | S=1 |
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| SMILES = N#Cc2ccc(cc2)-c1ccc(C(C)CNS(=O)(=O)C(C)C)cc1 |
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| molecular_weight = 342.45 g/mol |
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| smiles = N#Cc2ccc(cc2)-c1ccc(C(C)CNS(=O)(=O)C(C)C)cc1 |
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| synonyms = <small>LY-404,187; ''N''-2-propyl-2-propanesulfonamide</small> |
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| synonyms = <small>LY-404,187; ''N''-2-propyl-2-propanesulfonamide</small> |
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| StdInChI_Ref = {{stdinchicite|changed|chemspider}} |
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| StdInChI = 1S/C19H28N2O2S/c1-14(2)24(22,23)21-13-15(3)17-8-10-19(11-9-17)18-6-4-16(12-20)5-7-18/h4-7,14-15,17,19,21H,8-11,13H2,1-3H3 |
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| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} |
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| StdInChIKey = AIALBPYHYGYYRB-UHFFFAOYSA-N |
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'''LY-404,187''' (or '''LY404187''') is an ] (or "AMPA receptor potentiator") developed by ].<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> |
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'''LY-404187''' is an ] ] which was developed by ].<ref name="pmid15864556">{{ cite journal |vauthors=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 | year = 2005 | volume = 180 | issue = 4 | pages = 743–751 | pmid = 15864556 | doi = 10.1007/s00213-005-2254-y | s2cid = 37727259 }}</ref> It is a member of the ] class of AMPA receptor potentiators.<ref name="pmid16803862">{{ 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 α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid Receptors | journal = Journal of Pharmacology and Experimental Therapeutics | year = 2006 | volume = 319 | issue = 1 | pages = 293–298 | pmid = 16803862 | doi = 10.1124/jpet.106.105734 | s2cid = 11732324 | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=16803862 }}</ref> |
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LY-404,187 has been demonstrated to enhance cognitive function in animal studies, and has also shown effects suggesting ] action as well as having possible application in the treatment of ], ] and ]. 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 ] 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> |
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LY-404187 has been demonstrated to enhance cognitive function in animal studies, and has also shown effects suggesting ] action as well as having possible application in the treatment of ], ] and ]. 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 ] in the brain.<ref>{{ cite journal |vauthors=Quirk JC, Nisenbaum ES | title = LY404187: A Novel Positive Allosteric Modulator of AMPA Receptors | journal = CNS Drug Reviews | year = 2002 | volume = 8 | issue = 3 | pages = 255–282 | doi = 10.1111/j.1527-3458.2002.tb00228.x | pmid = 12353058 | pmc = 6741690 }}</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>{{ 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 | year = 2004 | volume = 3 | issue = 3 | pages = 181–194 | doi = 10.2174/1568007043337508 | pmid = 15180479 }}</ref><ref>{{ cite journal |vauthors=O'Neill MJ, Witkin JM | title = AMPA Receptor Potentiators: Application for Depression and Parkinson's Disease | journal = Current Drug Targets | year = 2007 | volume = 8 | issue = 5 | pages = 603–620 | doi = 10.2174/138945007780618517 | pmid = 17504104 }}</ref> |
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==See also== |
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==References== |
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==References== |
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{{Ionotropic glutamate receptor modulators}} |
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{{Glutamate receptor ligands}} |
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