SB-399885 hydrochlorideCAS号: 402713-81-9;402713-80-8(freebase)分子式: C18H21Cl2N3O4S·HCl分子量: 482.81描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vivo(体内研究)
产品描述 | |
描述 |
SB399885 盐酸盐是一种有效的 SR 6 拮抗剂。它显示 > 200-fold SR-6 (pKi 值分别为 9.11,8.81 和重组人、 本机大鼠和本机人类 SR-6 受体,9.02) 其他 5-羟色胺受体的选择性。 |
纯度 |
98%
|
储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
|
基本信息 | |
别名 |
SB-399885 HCl
|
外观 |
Off-white solid
|
可溶性/溶解性 |
DMSO : 100 mg/mL (207.12 mM; Need ultrasonic)
H2O : 6.67 mg/mL (13.81 mM; ultrasonic and warming and heat to 60°C) |
生物活性 | |
靶点 |
5-HT6 receptor
|
In vivo(体内研究) |
Compare with the control vehicle SB-399885 hydrochloride 10 mg/kg significantly increases wakefulness (W) (F(3,15)=3.32, P<0.05) while slow wave sleep (SWS), rapid-eye-movement sleep (REMS) and the number of REM periods are reduced (F(3,15)=4.0, P<0.01; F(3,15)=3.14, P<0.05 and F(3,15)=2.62, P<0.05, respectively). Analysis of sleep variables in 2-h blocks shows that SB-399885 hydrochloride 10 mg/kg increases W (F(3,15)=5.48, P<0.01) and reduces SWS (F(3,15)=5.42, P<0.01) and REMS (F(3,15)= 4.05, P<0.01) during the first 2-h period. SB-399885 hydrochloride 5 and 10 mg/kg augment light sleep over the first (F(3,15)=3.46,P<0.01 and F(3,15)= 3.65, P<0.01, respectively) and the second (F(3,15)=3.23, P<0.05 and F(3,15)=3.08, P<0.05, respectively) 2-h recording periods. SB-399885 hydrochloride 10 mg/kg significantly increases REMS latency (F(3,15)=3.60, P<0.01) and reduces the number of REM periods during the first 2-h of recording (F(3,15)=3.88, P<0.01).
|
分子结构图