Cas No.: | 951650-22-9 |
Chemical Name: | 3'-(5-(2-hydroxypropan-2-yl)-1H-benzo[d]imidazol-1-yl)biphenyl-2-carbonitrile |
Synonyms: | NS 11394,NS-11394,NS11394 |
SMILES: | CC(C)(C1=CC2=C(C=C1)N(C=N2)C3=CC=CC(=C3)C4=CC=CC=C4C#N)O |
Formula: | C23H19N3O |
M.Wt: | 353.42 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors. |
In Vivo: | Oral administration of NS11394 (1-30 mg/kg) to rats attenuated spontaneous nociceptive behaviors in response to hindpaw injection of formalin and capsaicin, effects that were blocked by the benzodiazepine site antagonist flumazenil [1]. NS11394 impairs memory in both rats and mice, which is possibly attributable to its efficacy at GABA(A)-alpha(5) receptors, albeit activity at this receptor might be relevant to its antinociceptive effects [2]. |
In Vitro: | NS11394 is unique in having superior efficacy at GABA(A)-alpha(3) receptors while maintaining low efficacy at GABA(A)-alpha(1) receptors. NS11394 has an excellent pharmacokinetic profile, which correlates with pharmacodynamic endpoints (CNS receptor occupancy), yielding a high level of confidence in deriving in vivo conclusions anchored to an in vitro selectivity profile and allowing for translation to higher species [2]. |