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142477-34-7

中文名稱 142477-34-7
英文名稱 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 結(jié)構(gòu)式 142477-34-7 結(jié)構(gòu)式

基本信息

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

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色White to off-white
142477-34-7價(jià)格(試劑級)
報(bào)價(jià)日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價(jià)格
2024/11/08HY-100290142477-34-7
5-HT1A modulator 1
142477-34-71mg3200元

常見問題列表

生物活性
5-HT1A modulator 1 對 5HT1A,腎上腺素能 α1 和多巴胺 D2 受體具有非常高的親和力,IC50 分別為 2±0.3 nM,10±3 nM 和 40±9 nM。
靶點(diǎn)

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 )

體外研究

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.

體內(nèi)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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