Stereochemistry | ACHIRAL |
Molecular Formula | C21H20FN3O5S |
Molecular Weight | 445.464 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(COC2=CC=C(C=N2)C(=O)N3CCS(=O)(=O)CC3)C(=NO1)C4=CC=C(F)C=C4
InChI
InChIKey=VCGRFBXVSFAGGA-UHFFFAOYSA-N
InChI=1S/C21H20FN3O5S/c1-14-18(20(24-30-14)15-2-5-17(22)6-3-15)13-29-19-7-4-16(12-23-19)21(26)25-8-10-31(27,28)11-9-25/h2-7,12H,8-11,13H2,1H3
Molecular Formula | C21H20FN3O5S |
Molecular Weight | 445.464 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Basmisanil (INN) (developmental code names RG-1662, RO5186582) is a highly selective inverse agonist/negative allosteric modulator of α5 subunit-containing GABAA receptors which is under development by Roche for the treatment of cognitive impairment associated with Down syndrome. The phase II trials were recently terminated due to lack of efficacy. This outcome suggests either that the α5-NAM was insufficiently effective to restore neuronal plasticity or alternatively that the hypothesis of excessive GABAergic inhibition obstructing neuronal plasticity does not extend to individuals with DS.