LY 404187 - CAS 211311-95-4
Category: Inhibitor
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Molecular Formula:
C19H22N2O2S
Molecular Weight:
342.46
COA:
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Targets:
AMPAR
Description:
LY 404187 is an allosteric modulator of AMPA receptors (IC50 = 0.15μM, 0.21μM, 1.66μM and 5.65 μM for GluA2i, GluA4i, GluA3i and GluA1i, respectively).
Purity:
≥98% by HPLC
Synonyms:
LY-404187; LY 404187; LY404187. N-[2-(4'-Cyano[1,1'-biphenyl]-4-yl)propyl]-2-propanesulfonamide
MSDS:
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InChIKey:
HOQAVGZLYRYHSO-UHFFFAOYSA-N
InChI:
InChI=1S/C19H22N2O2S/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/h4-11,14-15,21H,13H2,1-3H3
Canonical SMILES:
CC(C)S(=O)(=O)NCC(C)C1=CC=C(C=C1)C2=CC=C(C=C2)C#N
1.AMPA receptor potentiators: application for depression and Parkinson's disease.
O'Neill MJ;Witkin JM Curr Drug Targets. 2007 May;8(5):603-20.
Alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors mediate most of the excitatory neurotransmission and play a key role in synaptic plasticity in the mammalian central nervous system (CNS). In recent years several classes of AMPA receptor potentiators have been reported in the literature, including pyrrolidones (piracetam, aniracetam), benzothiazides (cyclothiazide), benzylpiperidines (CX-516, CX-546) and biarylpropylsulfonamides (LY392098, LY404187, LY450108, LY451395 and LY503430). Clinical and preclinical data have suggested that positive modulation of AMPA receptors may be therapeutically effective in the treatment of cognitive deficits. However, recent evidence has shown that in addition to modulating fast synaptic plasticity and memory processes, AMPA receptor potentiators alter downstream signalling pathways and may thereby have utility in other CNS disorders. The present review summarises studies into the effects of AMPA receptor potentiators (with a focus on the biarylpropylsulfonamides) in rodent models of depression and Parkinson's disease.
2.Potentiation of responses to AMPA on central neurones by LY392098 and LY404187 in vivo.
Vandergriff J;Huff K;Bond A;Lodge D Neuropharmacology. 2001 Jun;40(8):1003-9.
Enhancement of AMPA receptor mediated synaptic excitation has the potential to aid in the treatment of several psychiatric conditions. To test such claims there is a need to develop more potent compounds than those presently available and to demonstrate that they cross the blood-brain barrier to affect responses at central AMPA receptors. We have now completed in vivo tests with two such compounds, the newly discovered biarylpropylsulfonamides, LY392098 and LY404187, on spinal and hippocampal neurones in anaesthetised rats. In the initial study on spinal neurones, LY392098 (30-1000 microg/kg i.v.) dose-dependently increased responses to iontophoretically administered AMPA but not those to NMDA. Subsequently in a more detailed follow-up study on hippocampal neurones, LY392098 (1-100 microg/kg i.v.) and LY404187 (1-100 microg/kg i.v.) enhanced in a dose-dependent manner responses to AMPA. Responses to NMDA were also enhanced but to a less extent. Such enhanced responses to NMDA, but not those to AMPA, were reduced by the NMDA antagonist, ketamine (0.5-1 mg/kg i.v.) whereas the selective AMPA antagonist, LY300168 (GYKI53655; 1 mg/kg i.v.), reduced responses to both NMDA and AMPA. LY392098 also potentiated the synaptic excitation of dentate granule cells following perforant path stimulation.
3.AMPA receptor potentiators for the treatment of CNS disorders.
O'Neill MJ;Bleakman D;Zimmerman DM;Nisenbaum ES Curr Drug Targets CNS Neurol Disord. 2004 Jun;3(3):181-94.
Glutamate alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors mediate most of the excitatory neurotransmission in the mammalian central nervous system and also participate in forms of synaptic plasticity thought to underlie memory and learning, and the formation of neural networks during development. Molecular cloning techniques have shown that the AMPA receptor family is composed of four different subunits named GluR1-4 or GluRA-D (newly termed as Glu(A1)-Glu(A4)) and native AMPA receptors are most likely tetramers generated by the assembly of one or more of these subunits, yielding homomeric or heteromeric receptors. Additional complexity among AMPA receptors is conferred by alternative splicing of RNA for each subunit giving rise to flip and flop variants. Clinical and experimental data have suggested that positive modulation of AMPA receptors may be therapeutically effective in the treatment of cognitive deficits. Several classes of AMPA receptor potentiators have been reported, including pyrroliddones (piracetam, aniracetam), benzothiazides (cyclothiazide), benzylpiperidines (CX-516, CX-546) and more recently biarylpropylsulfonamides (LY392098, LY404187 and LY503430).
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CAS 211311-95-4 LY 404187

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