Basmisanil

Basmisanil
Clinical data
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	1159600-41-5;
PubChem CID	57336276;
ChemSpider	34500832;
CompTox Dashboard (EPA)	DTXSID201032402 ;
Chemical and physical data
Formula	C21H20FN3O5S
Molar mass	445.464003 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	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;

Basmisanil (INN) (developmental code names RG-1662, RO5186582) is a highly selective inverse agonist/negative allosteric modulator of α₅ subunit-containing GABA_A receptors which is under development by Roche for the treatment of cognitive impairment associated with Down syndrome.^[1]^[2]^[3] As of August 2015, it is in phase II clinical trials for this indication.^[4]

References

^ 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.
^ 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.
^ 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. doi:10.1371/journal.pone.0088456. ISSN 1932-6203.{{cite journal}}: CS1 maint: unflagged free DOI (link)
^ AdisInsight. "Basmisanil". Retrieved 2015-06-10.

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