951650-22-9
951650-22-9 structure
- Name: NS-11394
- Chemical Name: 2-[3-[5-(2-hydroxypropan-2-yl)benzimidazol-1-yl]phenyl]benzonitrile
- CAS Number: 951650-22-9
- Molecular Formula: C23H19N3O
- Molecular Weight: 353.417
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
- Create Date: 2016-09-28 10:03:33
- Modify Date: 2024-01-03 00:32:17
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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.IC50 value:Target: GABA A receptor modulatorin 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]. 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].
| Name | 2-[3-[5-(2-hydroxypropan-2-yl)benzimidazol-1-yl]phenyl]benzonitrile |
|---|---|
| Synonyms |
[1,1'-Biphenyl]-2-carbonitrile, 3'-[5-(1-hydroxy-1-methylethyl)-1H-benzimidazol-1-yl]-
NS-11394 3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile 3'-[5-(2-Hydroxy-2-propanyl)-1H-benzimidazol-1-yl]-2-biphenylcarbonitrile NS11394 |
| 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.IC50 value:Target: GABA A receptor modulatorin 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]. 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]. |
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| Related Catalog | |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 623.7±65.0 °C at 760 mmHg |
| Molecular Formula | C23H19N3O |
| Molecular Weight | 353.417 |
| Flash Point | 331.0±34.3 °C |
| Exact Mass | 353.152802 |
| PSA | 61.84000 |
| LogP | 4.16 |
| Appearance | white solid |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Index of Refraction | 1.637 |
| Storage condition | -20℃ |