LY-404,187

LY-404,187
IUPAC ime
	N-[2-(4'-cianobifenil-4-il)propil]propan-2-sulfonamid
Pravni status
Pravni status	Lek u razvoju;
Identifikatori
CAS broj	211311-95-4
ATC kod	none
Sinonimi	N-2-[4-(4-cijanofenil)fenil]propil-2-propanesulfonamid
Hemijski podaci
Formula	C19H22N2O2S
Molarna masa	342,45 g/mol
	SMILES N#Cc2ccc(cc2)-c1ccc(C(C)CNS(=O)(=O)C(C)C)cc1; ;

LY-404,187 (LY404187) je ampakinski lek (potencijator AMPA receptora) koji je razvila kompanija Eli Lili.^[1] On je član biarilpropilsulfonamidne klase ampakina.^[2]

LY-404,187 poboljšava kognitivne funkcije u životinjskim studijama, a isto tako ispoljava efekte koji sugerišu antidepresantno dejstvo. On potencijalno može da nađe primenu u tretiranju šizofrenije, Parkinsonove bolesti i ADHD-a. Njegovo dejstvo je posredovano višestrukim mehanizmima akcije pored potencijacije AMPA receptor. Prominentni efekat zapažen u istraživanjima je povišeni novo BDNF-a u mozgu.^[3]^[4]^[5]

Reference

^ Jones N, O'Neill MJ, Tricklebank M, Libri V, Williams SC (2005). „Examining the neural targets of the AMPA receptor potentiator LY404187 in the rat brain using pharmacological magnetic resonance imaging”. Psychopharmacology (Berl.). 180 (4): 743—51. PMID 15864556. doi:10.1007/s00213-005-2254-y.
^ 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”. J. Pharmacol. Exp. Ther. 319 (1): 293—8. PMID 16803862. doi:10.1124/jpet.106.105734.
^ Quirk JC, Nisenbaum ES. LY404187: a novel positive allosteric modulator of AMPA receptors. CNS Drug Reviews. 2002 Fall;8(3):255-82. PMID 12353058
^ 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
^ 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

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[pmid15864556-1] Jones N, O'Neill MJ, Tricklebank M, Libri V, Williams SC (2005). „Examining the neural targets of the AMPA receptor potentiator LY404187 in the rat brain using pharmacological magnetic resonance imaging”. Psychopharmacology (Berl.). 180 (4): 743—51. PMID 15864556. doi:10.1007/s00213-005-2254-y.

[pmid16803862-2] 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”. J. Pharmacol. Exp. Ther. 319 (1): 293—8. PMID 16803862. doi:10.1124/jpet.106.105734.

[3] Quirk JC, Nisenbaum ES. LY404187: a novel positive allosteric modulator of AMPA receptors. CNS Drug Reviews. 2002 Fall;8(3):255-82. PMID 12353058

[4] 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

[5] 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

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