Basmisanil

Basmisanil (INN; developmental codes RG-1662 and 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.[1][2][3] As of June 2016, it is no longer studied.[4] It is studied with schizophrenia patients.[5]

Basmisanil
Clinical data
Other namesRG-1662; RO5186582
ATC code
  • None
Identifiers
IUPAC name
  • (1,1-Dioxo-1,4-thiazinan-4-yl)-[6-[[3-(4-fluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]pyridin-3-yl]methanone
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC21H20FN3O5S
Molar mass445.47 g·mol−1
3D model (JSmol)
SMILES
  • CC1=C(C(=NO1)C2=CC=C(C=C2)F)COC3=NC=C(C=C3)C(=O)N4CCS(=O)(=O)CC4
InChI
  • 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
  • Key:VCGRFBXVSFAGGA-UHFFFAOYSA-N



See also

References
  1. Froestl W, Muhs A, Pfeifer A (2012). "Cognitive enhancers (nootropics). Part 1: drugs interacting with receptors". J. Alzheimers Dis. 32 (4): 793–887. doi:10.3233/JAD-2012-121186. PMID 22886028.
  2. Hurley, Dan (2013). "Investigators Silence Trisomy 21 Chromosome in Human Down Syndrome Cells". Neurology Today. 13 (17): 14–15. doi:10.1097/01.NT.0000434604.55014.fd. ISSN 1533-7006.
  3. Rudolph, Uwe; Jensen, Henrik Sindal; Nichol, Kathryn; Lee, Deborah; Ebert, Bjarke (2014). "Clobazam and Its Active Metabolite N-desmethylclobazam Display Significantly Greater Affinities for α2- versus α1-GABAA–Receptor Complexes". PLOS ONE. 9 (2): e88456. Bibcode:2014PLoSO...988456J. doi:10.1371/journal.pone.0088456. ISSN 1932-6203. PMC 3922815. PMID 24533090.
  4. Marly Chevrette. "Response to the Roche Clinical Trial for CLEMATIS". Retrieved 2016-06-28.
  5. "A Study to Evaluate the Effects of Basmisanil in Participants With Cognitive Impairment Associated With Schizophrenia (CIAS) Treated With Antipsychotics". 21 January 2021. Retrieved 2021-07-02. {{cite journal}}: Cite journal requires |journal= (help)CS1 maint: url-status (link)


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