Details
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
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/28232865Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/27466376 | https://www.ncbi.nlm.nih.gov/pubmed/28236228 | http://www.roche.com/media/store/statements.htm | https://www.ncbi.nlm.nih.gov/pubmed/26635554
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28232865
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/27466376 | https://www.ncbi.nlm.nih.gov/pubmed/28236228 | http://www.roche.com/media/store/statements.htm | https://www.ncbi.nlm.nih.gov/pubmed/26635554
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.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL5112 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27466376 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02024789
120 or 240 mg (80 or 160 mg for subjects 12 and 13 years of age) orally twice daily, 26 weeks
Route of Administration:
Oral
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300000034034
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1646183-13-2
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DTXSID201032402
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9936
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DB11877
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C167009
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RG 1662
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57336276
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CD-101
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1159600-41-5
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788PET5SUA
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CHEMBL3681419
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ACTIVE MOIETY