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142477-34-7

中文名称 142477-34-7
英文名称 5-HT1A modulator 1
CAS 142477-34-7
分子式 C21H25N3O2S
分子量 383.51
MOL 文件 142477-34-7.mol
更新日期 2023/03/20 15:41:17
142477-34-7 结构式 142477-34-7 结构式

基本信息

中文别名
化合物 T10168
化合物5-HT1A MODULATOR 1
英文别名
5-HT1A modulator 1
2(3H)-Benzothiazolone, 6-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-3-methyl-

物理化学性质

储存条件-20°C储存
溶解度溶于二甲基亚砜
形态Solid
颜色White to off-white
142477-34-7价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/08/19HY-100290142477-34-7
5-HT1A modulator 1
142477-34-71mg3200元

常见问题列表

生物活性
5-HT1A modulator 1 对 5HT1A,肾上腺素能 α1 和多巴胺 D2 受体具有非常高的亲和力,IC50 分别为 2±0.3 nM,10±3 nM 和 40±9 nM。
靶点

sPLA2

2 nM (IC 50 )

5-HT 2A Receptor

500 nM (IC 50 )

5-HT 2C Receptor

4000 nM (IC 50 )

α1 receptor

10 nM (IC 50 )

D2 receptor

40 nM (IC 50 )

体外研究

5-HT1A modulator 1 (Compound 24) also displays affinities for the 5HT 1B , 5-HT 2A and 5-HT 2C receptor with IC 50 s of 300±55 nM, 500±75 nM, and 4000±440 nM, respectively.

体内研究

5-HT1A modulator 1 (Compound 24) shows clear antagonist action at 5HT 2A receptor subtype in mice. The antagonism is nearly complete at the dose of 1 mg/kg ip for 5-HT1A modulator 1 (94% of antagonism, p<0.01). 5-HT1A modulator 1 completely blocks the stereotypies and the climbing at the dose of 1 mg/kg ip (100% of antagonism). 5-HT1A modulator 1 is also tested in rats, using the same paradigm. After oral administration, 5-HT1A modulator 1 significantly (p<0.05) reduces the hyperactivity by 50% at the doses of 2 and 4 mg/kg po, respectively 63% and 58% of antagonism for 5-HT1A modulator 1; the antagonism is complete (103% and 108%) at the respective doses of 8 and 16 mg/kg po for 5-HT1A modulator 1 (p<0.01).

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