| Stereochemistry | RACEMIC |
| Molecular Formula | C19H22N2O2S |
| Molecular Weight | 342.455 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)S(=O)(=O)NCC(C)C1=CC=C(C=C1)C2=CC=C(C=C2)C#N
InChI
InChIKey=HOQAVGZLYRYHSO-UHFFFAOYSA-N
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
| Molecular Formula | C19H22N2O2S |
| Molecular Weight | 342.455 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
LY404187 (or LY-404,187) is a selective, potent and centrally active positive allosteric modulator of AMPA receptors. LY404187 preferentially acts at recombinant human homomeric GluR2 and GluR4 versus GluR1 and GluR3 AMPA receptors. This drug, developed by Eli Lilly and Company, is a member of biarylpropylsulfonamides. LY404187 has been shown to enhance performance in animal models of cognitive function requiring different mnemonic processes and may be therapeutically beneficial for treating cognitive deficits in a variety of disorders, particularly those that are associated with reduced glutamatergic signaling such as schizophrenia. In addition, LY404187 has been demonstrated to be efficacious in animal models of behavioral despair that possess considerable predictive validity for antidepressant activity and Parkinson's disease.
CNS Activity
Originator
Approval Year
PubMed
Sample Use Guides
in mice: Acute treatment by LY404187: 2.0, 5.0, or 10 mg/kg subcutaneously
Route of Administration:
Other
LY404187 enhance glutamate (100 uM) stimulated ion influx through recombinant homomeric human AMPA receptor ion channels, GluR1-4, with estimated EC(50) values of 5.65 uM (GluR1(i)), 0.15 uM (GluR2(i)), 1.44 uM (GluR2(o)), 1.66 uM (GluR3(i)) and 0.21 uM (GluR4(i)) for LY404187. Neither compound affected ion influx in untransfected HEK293 cells or GluR transfected cells in the absence of glutamate. This compound was selective for activity at AMPA receptors, with no activity at human recombinant kainate receptors. Electrophysiological recordings demonstrated that glutamate (1 mM)-evoked inward currents in human GluR4 transfected HEK293 cells was potentiated by LY404187 at low concentrations (3-10 nM). In addition, this compound removed glutamate-dependent desensitization of recombinant GluR4 AMPA receptors.
