Ganaxolone 是 GABAA 受体作用的正向变构调节剂,具有抗焦虑和抗惊厥作用。
产品描述
Ganaxolone is a positive allosteric modulator of the action of the GABAA receptor, acts on well-characterized targets in the brain known to have anxiolytic and anticonvulsant effects.
体内活性
Ganaxolone, may improve anxiety, aggression, and other PTSD-like behaviors in the SI mouse model. Ganaxolone (3.75-30 mg/kg, s.c.) injected 60 min before testing of SI mice, induced a dose-dependent reduction in aggression toward a same-sex intruder and anxiety-like behavior in an elevated plus maze.?The EC50 dose of ganaxolone used in these tests also normalized exaggerated contextual fear conditioning and, remarkably, enhanced fear extinction retention in SI mice.?At these doses, ganaxolone failed to change locomotion in an open field test.
动物实验
Adult male Swiss–Webster mice , 18–20 g body weight, were maintained under a 12-h dark/light cycle and provided food and water ad libitum in a vivarium with temperature and humidity kept near 24°C and 65%, respectively.?SI mice were housed individually in a 24 × 17 × 12 cm cage for 3–4 weeks, while group-housed control mice were housed in groups of 5.Inc^2.?Ganaxolone, pregnanolone, or vehicle (corn oil) in a volume of 100 μl/10 g was injected subcutaneously 60 min before behavioral tests of locomotor activity, anxiety-like behavior, and aggressive behavior toward an intruder in the home cage.?In a study of ganaxolone effects on fear extinction and retention, ganaxolone or vehicle was administered just once, immediately after the first session in which the mice were reexposed to the context in which fear conditioning was performed the day before[1]
Cas No.
38398-32-2
分子式
C22H36O2
分子量
332.52
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years