L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki=0.45 nM).
靶点:
GABA Receptor;GABAReceptor
体内研究:
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.
参考文献:
1. Saab BJ, et al. Short-term memory impairment after isoflurane in mice is prevented by the α5 γ-aminobutyric acid type A receptorinverse agonist L-655708. Anesthesiology. 2010 Nov;113(5):1061-1071.