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SSD114 is a novel GABAB receptor positive allosteric modulator.
分子量
387.83
纯度
98%
可溶性
DMSO:45 mg/mL (116.03 mM)
In vitro(体外研究)
In the presence of 10 μM GABA, SSD114 hydrochloride at 25 μM significantly increases (to approximately 170% above basal levels) the [35S]GTPγS stimulation induced by GABA alone. SSD114 hydrochloride (15 or 30 μM) induces a leftward shift of the GABA concentration-response curve with a slight concomitant increase of maximal GABA stimulation at the highest concentration. In the presence of both 15 and 30 μM SSD114 hydrochloride, the EC50 for GABA decreases by 2 and 2.5 fold, respectively, while the maximal stimulation (Emax) is potentiated only at the concentration of 30 μM, reaching 161±5.09% over the basal value [1].
In vivo(体内研究)
The onset of loss of righting reflex (LORR) is reduced by pretreatment with SSD114 hydrochloride [F(5,30)=4.55, P<0.005]. Post hoc analysis indicates that the onset of LORR is significantly lower in mouse groups pretreated with doses of SSD114 hydrochloride equal to or higher than 10 mg/kg than in vehicle-treated mice. The duration of LORR is increased by pretreatment with SSD114 hydrochloride [F(5,30)=4.81, P<0.005]. Post hoc analysis indicates that the duration of LORR is significantly longer in mouse groups pretreated with 10 and 100 mg/kg SSD114 hydrochloride than in vehicle-treated mice [1].
背景
分子式
C18H21ClF3N3O
CAS号
2319790-02-6
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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