Molecular Formula | C18H19N3O4
|
Molar Mass | 341.36 |
Density | 1.42±0.1 g/cm3(Predicted) |
Melting Point | 175-176 °C |
Boling Point | 584.4±50.0 °C(Predicted) |
Flash Point | 307.2°C |
Solubility | DMSO: 6mg/mL |
Vapor Presure | 1.21E-13mmHg at 25°C |
Appearance | powder |
pKa | 1.49±0.20(Predicted) |
Storage Condition | Desiccate at +4°C |
Refractive Index | 1.675 |
Physical and Chemical Properties | Solubility: DMSO: 6 mg/ml WGK Germany:3 |
In vitro study | L655708 is a potent, selective inverse agonist for the benzodiazepine site of GABAA receptors containing the α5 subunit (Ki = 0.45 nM). Displays 50-100-fold selectivity over GABAA receptors containing α1, α2, α3 orα6 subunits in combination with β3 and γ2. Enhances LTP in a mouse hippocampal slice model and increases spatial learning, without displaying proconvulsant activity. |
In vivo study | L-655708 at 0.7 mg/kg, administered intraperitoneally, would result in 60-70% occupancy of α5 GABAA receptors with limited binding to α1, α2, and α3 subunit-containing GABAA receptors and no significant off-target behavioral effects, such as sedation and motor impairment. |