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200940-22-3

中文名稱 SB 243213
英文名稱 1H-Indole-1-carboxamide, 2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-
CAS 200940-22-3
分子式 C22H19F3N4O2
分子量 428.41
MOL 文件 200940-22-3.mol
更新日期 2023/03/20 15:41:27
200940-22-3 結構式 200940-22-3 結構式

基本信息

英文別名
SB 243213
1H-Indole-1-carboxamide, 2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-

物理化學性質(zhì)

儲存條件-20°C儲存
形態(tài)Solid
顏色White to off-white
SB 243213價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-103112BSB 243213200940-22-35mg900元
2024/11/08HY-103112BSB 243213200940-22-310mM * 1mLin DMSO990元
2024/11/08HY-103112BSB 243213200940-22-310mg1500元

常見問題列表

生物活性
SB 243213 是一種口服有效的,選擇性的,高親和力的 5-HT2C 受體拮抗劑,對人 5-HT2C 受體的 pKi 為 9.37,pKb 為 9.8。SB 243213 對多種神經(jīng)遞質(zhì)受體、酶和離子通道具有超過 100 倍的選擇性。SB 243213 具有改善的抗焦慮特性,有用于精神分裂癥和運動障礙的潛力。
靶點

Human 5-HT 2C Receptor

9.37 (pKi)

human 5-HT 1A Receptor

<5.3 (pKi)

human 5-HT 1B Receptor

5.5 (pKi)

human 5-HT 1D Receptor

6.32 (pKi)

human 5-HT 1E Receptor

<5.4 (pKi)

human 5-HT 1F Receptor

5.35 (pKi)

Human 5-HT 2A Receptor

7.01 (pKi)

human 5-HT 2B Receptor

7.2 (pKi)

Human 5-HT 6 Receptor

6.5 (pKi)

Human 5-HT 7 Receptor

5.64 (pKi)

體外研究

SB 243213 shows little affinity (pK i <6) for cloned human 5-HT 1A , 5-HT 1B , 5-HT 1E , 5- HT 1F and 5-HT 7 receptors. It shows weak affinity (pK i <6.5) for the cloned human 5-HT 1D and D3 receptors and moderate affinity (pK i =6.7) for the cloned human D2 receptor.

體內(nèi)研究

SB 243213 (0.1-10 mg/kg, p.o. 1 h pre-test) dose-dependently and significantly increases the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.
SB 243213 (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction.

Animal Model: Male Sprague-Dawley experimentally naive rats (220-300 g)
Dosage: 0.1, 0.3, 1, 3, 10 mg/kg
Administration: PO; 1 hour pre-test
Result: Dose-dependently and significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.
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