Basmisanil

A novel selective negative allosteric modulator of the GABAA receptor α5-subtype, which is under development for the treatment of cognitive impairment associated with Down syndrome.Schizophrenia Phase 2 Clinical (In Vitro) :Basmisanil (0.1 nM-100 μM) has high affinity for bounding to recombinant human GABAA-α5 receptors with a Ki value of 5 nM and more than 90-fold selectivity versus α1 (Ki = 1031 nM), α2 (Ki = 458 nM), and α3 (Ki = 510 nM) subunit-containing receptors.Basmisanil (1 nM-1 μM) shows a highly selective inhibition of GABAA-α5 with a IC50 value of 8 nM.Basmisanil (1 μM) inhibits GABA-induced currents at GABAA-α5 yet had little or no effect at the other receptor subtypes. (In Vivo) :Basmisanil (3-100 mg/kg, p.o.) occupies GABAA-α receptor in dose-dependent in rat brain.Basmisanil (3-600 mg/kg p.o.) improves cognition in rats and non.human primates and not show anxiogenic or proconvulsant effects.

1159600-41-5

RG-1662 | RO5-186582

>98% (HPLC)

DMSO: ≥ 32 mg/mL

O=C (N1CCS (CC1) (=O) =O) C2=CC=C (OCC3=C (C) ON=C3C4=CC=C (F) C=C4) N=C2

C21H20FN3O5S

445.464

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.